Entries |
Document | Title | Date |
20080200503 | Macrocylic Inhibitors Of Hepatitis C Virus - Inhibitors of HCV of formula (I). | 08-21-2008 |
20080207687 | Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I) | 08-28-2008 |
20080214604 | Medicinal Composition - A pharmaceutical composition comprising: an active ingredient consisting of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, salt thereof, or solvate of the foregoing; and (i) a compound, a 5% (w/w) aqueous solution or suspension of which has a pH of 8 or more, and/or (ii) silicic acid, salt thereof, or solvate of the foregoing is a highly stable pharmaceutical composition, wherein under humidified and heated storage conditions, the decomposition of said compound is sufficiently reduced, or the gelation on the surface of the pharmaceutical composition is sufficiently inhibited. | 09-04-2008 |
20080214605 | Alkyl Sulfoxide Quinolines as Nk-3 Receptor Ligands - Compounds of Formula I | 09-04-2008 |
20080221158 | Novel 14 and 15 Membered Ring Compounds - The present invention relates to 15-membered macrolides substituted at the 4″ position of formula (I) | 09-11-2008 |
20080221159 | Inhibitors of human immunodeficiency virus replication - Compounds of formula I: | 09-11-2008 |
20080221160 | SULFONYLATED HETEROCYCLES USEFUL FOR MODULATION OF THE PROGESTERONE RECEPTOR - Compounds of the following structure are provided, wherein n, R | 09-11-2008 |
20080227811 | Spiro Substituted Compounds As Angiogenesis Inhibitors - The present invention relates to spiro (tetracarbon) substituted compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans. | 09-18-2008 |
20080242700 | Methods and Compositions for Selectin Inhibition - The present teachings relate to compounds of formula I: | 10-02-2008 |
20080249129 | Compositions and Methods for Treatment of Protein Misfolding Diseases - Disclosed are compounds and conditions that either suppress or enhance toxicity in yeast cells expressing alpha synuclein or huntingtin. These compounds and conditions can be used in the development of compositions that suppress toxicity, fibril formation, and/or diseases mediated at least in part by alpha synuclein or huntingtin. | 10-09-2008 |
20080255190 | 8-Cyanoquinolonecarboxylic Acid Derivative - To provide a quinolone antibacterial drug and a therapeutic agent for infectious diseases, which exhibit potent antibacterial activity on Gram-positive and Gram-negative bacteria and which is highly safe. | 10-16-2008 |
20080255191 | BENZYLIMIDAZOLYL SUBSTITUTED 2-QUINOLINE AND QUINAZOLINE DERIVATIVES FOR USE AS FARNESYL TRANSFERASE INHIBITORS - This invention comprises the novel compounds of formula (I) | 10-16-2008 |
20080255192 | Methods and Compositions for Selectin Inhibition - The present teachings relate to novel compounds of formula I: | 10-16-2008 |
20080255193 | Pharmaceutical Composition - A novel pharmaceutical composition comprising the NK | 10-16-2008 |
20080262034 | LIPOIC ACID DERIVATIVES - Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives. | 10-23-2008 |
20080275082 | Pharmaceutical Composition - A novel pharmaceutical composition comprising the NK | 11-06-2008 |
20080306110 | Alkylnitrile Quinolines as Nk-3 Receptor Ligands - Compounds of Formula I | 12-11-2008 |
20080319008 | Compounds Having Activity in Increasing Ion Transport by Mutant-Cftr and Uses Thereof - The invention provides compositions, pharmaceutical preparations and methods for increasing activity (e.g., ion transport) of the mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR), e.g., ΔF508 CFTR, G551D-CFTR, G1349D-CFTR, or D1152H-CFTR, that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more phenylglycine-containing compounds or sulfonamide-containing compounds of the invention, or an analog or derivative thereof. | 12-25-2008 |
20080319009 | Methylene-bridged selective androgen receptor modulators and methods of use thereof - This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell. | 12-25-2008 |
20090012118 | Kynurenic Acid Amide Derivatives as Nr2b Receptor Antagoni - The new kynurenic acid amide derivatives of formula (I): and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. | 01-08-2009 |
20090012119 | FLUOROALKYLPYRROLIDINE DERIVATIVE - This invention relates to a compound represented by the following formula (1): | 01-08-2009 |
20090023773 | COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS - Disclosed are compounds that modulate the activity of the gated ion channels. Compounds that modulate these gated ion channels are useful in the treatment of diseases and disorders related to pain, inflammation, the neurological system, the gastrointestinal system and genitourinary system. Preferred compounds include compounds of the Formulae 1, 2, 3, 4, and 5. | 01-22-2009 |
20090023774 | Pyridine analogs as C5A antagonists - The present invention provides novel compounds of Formula I which are antagonists of the C5a receptor. Compounds of the present invention are useful for the treatment of various C5a-mediated diseases and disorders; accordingly the present invention provides a method for the treatment of C5a-mediated diseases using the novel compounds described herein, as well as pharmaceutical compositions containing them. | 01-22-2009 |
20090030038 | Novel 8-Sulfonylamino-3 Aminosubstituted Chroman or Tetrahydronaphtalene Derivatives Modulating the 5Ht6 Receptor - The present invention relates to new compounds of formula I. (I) wherein R | 01-29-2009 |
20090036485 | Quinoline derivatives - The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R | 02-05-2009 |
20090042932 | ANTIMICROBIAL PARENTERAL FORMULATION - This invention relates to a parenteral formulation containing an effective amount of the compound of the following formula I: | 02-12-2009 |
20090042933 | Derivatives of 4-(2-amino -1-hydroxyethyl)phenol as agonists of the Beta2 adrenergic receptor - A compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R | 02-12-2009 |
20090042934 | Sulfonyl-Quinoline Derivatives - The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in treatment and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors. | 02-12-2009 |
20090042935 | NOVEL IV FORMULATION OF TIPIFARNIB - This invention concerns compositions of tipifarnib, mannitol, and hydroxypropyl-β-cyclodextrin and, suitable for intravenous (IV) administration. The invention further concerns the use of such formulation and processes for preparing such formulations and methods of treating by administering said formulations. | 02-12-2009 |
20090048293 | METHODS FOR TREATING BACILLUS INFECTION - The present invention provides compositions and methods for detecting, treating, and preventing microbial infection, especially infection caused by | 02-19-2009 |
20090048294 | HIF-1 ALPHA ACTIVATING AGENT - The present invention relates to a HIF-1α activator containing clioquinol and its derivatives as an active ingredient. Clioquinol and its derivatives of the invention inhibit HIF-1α (hypoxia-inducible factor-1α) ubiquitination in normoxic cells and thus accumulate HIF-1α. In the meantime, CQ inhibits FIH-I activity and thereby induces transcription activity of the accumulated HIF-1α, resulting in the induction of expressions of HIF-1α target genes VEGF (vascular endothelial growth factor) and EPO (erythropoietin). Therefore, clioquinol and its derivatives can be effectively used as a therapeutic agent for ischemic disease. | 02-19-2009 |
20090048295 | SUBSTITUTED 5,6,7,8-TETRAHYDROQUINOLINE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE THEREOF - Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C5 | 02-19-2009 |
20090048296 | HIGH CONCENTRATION LOCAL ANESTHETIC FORMULATIONS - A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit neuropathic pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours. | 02-19-2009 |
20090062337 | Treatment of Microbial Infections - The present invention provides methods for treating various microbial infections using a compound of the formula: | 03-05-2009 |
20090069372 | ANTITUMOR AGENTS - The invention provides compounds of formula I: | 03-12-2009 |
20090076072 | DEUTERIUM-ENRICHED TAFENOQUINE - The present application describes deuterium-enriched tafenoquine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090076073 | THERAPEUTIC AMIDES - The invention provides compounds of the formula: | 03-19-2009 |
20090076074 | QUINOLINE DERIVATIVES - The invention concerns quinoline derivatives of Formula I | 03-19-2009 |
20090076075 | QUINOLINE DERIVATIVES - The invention concerns quinoline derivatives of Formula I | 03-19-2009 |
20090099230 | Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof. | 04-16-2009 |
20090105299 | c-MET MODULATORS AND METHODS OF USE - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 04-23-2009 |
20090111850 | Amino-Substituted Ethylamino Beta2 Adrenergic Receptor Agonists - The invention provides novel β | 04-30-2009 |
20090111851 | Antimicrobial Quinolones, Their Compositions and Uses - Compounds having the general structure: | 04-30-2009 |
20090131474 | SCREENING METHODS FOR PROTEIN KINASE B INHIBITORS EMPLOYING VIRTUAL DOCKING APPROACHES AND COMPOUNDS AND COMPOSITIONS DISCOVERED THEREBY - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions. | 05-21-2009 |
20090137626 | Pharmaceutical Composition Containing PPARgamma Agonist - [Object] To provide a highly safe method for treating diabetes that demonstrates superior effects and is capable of inhibiting adverse side effects. | 05-28-2009 |
20090137627 | Method for Treating Chronic Pain - A method for the treatment of chronic pain in a mammal is provided. The method comprises administering to a mammal (e.g., a human) suffering from chronic pain a pain relieving amount of a diarylureido-dihalokynurenate compound. Preferred diarylureido-dihalokynurenate compounds are esters (e.g., ethyl esters). Particularly preferred are diphenylureido-dichlorokynurenate compounds. | 05-28-2009 |
20090143426 | Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments - The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR | 06-04-2009 |
20090143427 | 4-Oxoquinoline derivatives - This invention relates to novel compounds that are 4-oxoquinoline derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 4-oxoquinoline derivatives that are derivatives of elvitegravir. This invention also provides pyrogen-free compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor, such as elvitegravir. | 06-04-2009 |
20090156636 | THERAPEUTIC AGENT FOR GLOMERULAR DISEASE - The present invention relates to a preventive and/or therapeutic agent for a glomerular disease containing, as active ingredients pitavastatin or a salt thereof and candesartan cilexetil or a salt thereof. The agent of the present invention exhibits an excellent effect in the prevention and/or therapy of a glomerular disease. | 06-18-2009 |
20090163544 | Use of NK-3 Receptor Antagonists for the Treatment of Nausea and Vomiting - This invention relates to the treatment or prevention of nausea and/or vomiting by the administration of a NK-3 receptor antagonist. | 06-25-2009 |
20090163545 | Method For Altering The Lifespan Of Eukaryotic Organisms - A method for altering the lifespan of a eukaryotic organism. The method comprises the steps of providing a lifespan altering compound, and administering an effective amount of the compound to a eukaryotic organism, such that the lifespan of the organism is altered. In one embodiment, the compound is identified using the DeaD assay. | 06-25-2009 |
20090170896 | c-Met modulators and methods of use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 07-02-2009 |
20090176826 | COMBINATION DRUG CONTAINING PROBUCOL AND A TETRAZOLYLALKOXY-DIHYDROCARBOSTYRIL DERIVATIVE WITH SUPEROXIDE SUPRESSANT EFFECTS - This invention relates to a combination drug comprising a combination of a tetrazolylalkoxy-dihydrocarbostyril derivative of the formula: | 07-09-2009 |
20090197913 | SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR - The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′: | 08-06-2009 |
20090209580 | ANTITUMOR AGENT FOR THYROID CANCER - The objective of the present invention is to provide a pharmaceutical composition and a therapeutic method that are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. | 08-20-2009 |
20090221635 | QUINOLINYL AND BENZOTHIAZOLYL MODULATORS - Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ. In particular, the compounds of the invention modulate the function of PPARγ. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis. | 09-03-2009 |
20090239904 | COMPOUNDS HAVING BETA2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY - This invention provides compounds of formula I: | 09-24-2009 |
20090247576 | ANTI-TUMOR AGENT FOR MULTIPLE MYELOMA - The object of the invention is to provide a pharmaceutical composition and a therapeutic method which can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3. The compound represented by General Formula (I), a pharmacologically acceptable salt thereof or a solvate thereof can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3. | 10-01-2009 |
20090247577 | PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS - Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula I, | 10-01-2009 |
20090247578 | 5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE-DERIVATIVES AND THEIR USES AS ANTIBACTERIALS - The invention relates to novel chimeric antibiotics of formula I | 10-01-2009 |
20090253739 | Amine Derivatives - The invention relates to compounds of formula (1) | 10-08-2009 |
20090264464 | ANTITUMOR AGENT FOR UNDIFFERENTIATED GASTRIC CANCER - The present invention relates to a therapeutic agent represented by the General formula (I), or a pharmacologically acceptable salt thereof, or a solvate of the compound or the salt thereof: | 10-22-2009 |
20090281140 | Macrocyclic inhibitors of hepatitis c virus - Inhibitors of HCV replication of formula (I) | 11-12-2009 |
20090281141 | MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I) | 11-12-2009 |
20090298874 | BACTERIAL ATP SYNTHASE BINDING DOMAIN - This invention provides an isolated mutant atpE protein and departing from said mutant atpE protein the identification of an ATPase binding domain. This invention also provides related nucleic acids, vectors, host cells, pharmaceutical compositions and articles of manufacture. This invention further provides methods for determining whether a test compound interacts with an atpE protein, i.e. with the ATPase binding domain of the present invention, as well as pharmaceuticals compositions comprising said test compound, in particular as antimicrobials, more particular as antimycobacterial agent, even more particular for treating tuberculosis in a subject. | 12-03-2009 |
20090298875 | A Combination of Compounds, Which Can be Used in the Treatment of Respiratory Diseases, Especially Chronic Obstructive Pulmonary Disease (COPD) and Asthma - The present invention provides pharmaceutical compositions comprising a β | 12-03-2009 |
20090298876 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 12-03-2009 |
20090326008 | NF-kappa B Inhibitor - The present invention provides an NF-κB inhibitor. The NF-κB inhibitor of the present invention contains a carbostyril compound represented by General Formula (1) | 12-31-2009 |
20100004282 | TREATMENT OF ANTIBIOTIC-RESISTANT BACTERIA INFECTION - This invention relates to a method of treating infection by methicillin-nonsusceptibale bacteria, vancomycin-nonsusceptibale bacteria, penicillin-nonsusceptibale bacteria, clarithromycin-nonsusceptibale bacteria, or metronidazole-nonsusceptibale bacteria by administering to a subject in need thereof an effective amount of a compound of the following formula: | 01-07-2010 |
20100010039 | POLYMORPHIC CRYSTAL FORM OF A INDAN-2-YLAMINO-HYDROXYETHYL-QUINOLINONE MALEATE DERIVATIVE AS BETA-ADRENOCEPTOR AGONIST - New polymorphic crystal form of (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one maleate designated crystal form Qalpha that is useful in the treatment of inflammatory or obstructive airways diseases. A method for preparing crystal form Qalpha is also described. | 01-14-2010 |
20100010040 | Triazol Derivatives Useful For The Treatment of Diseases - The invention relates to compounds of formula (1) | 01-14-2010 |
20100016352 | COMPOUNDS AND METHODS FOR TREATING ESTROGEN RECEPTOR-RELATED DISEASES - Provided herein in certain embodiments are compounds, pharmaceutical compositions and methods for modulating the functions of estrogen receptor alpha 36, for preventing and/or treating diseases mediated by estrogen receptor alpha 36, for preventing and/or treating osteoporosis, for inducing cell death and/or inhibiting cell proliferation and for preventing and/or treating diseases involving abnormal cell proliferation such as cancers. | 01-21-2010 |
20100022585 | BETA- AND GAMMA-AMINO-ISOQUINOLINE AMIDE COMPOUNDS AND SUBSTITUTED BENZAMIDE COMPOUNDS - Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds. | 01-28-2010 |
20100022586 | BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PD E4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. | 01-28-2010 |
20100022587 | DERIVATIVES OF 2-PHENYL-3-HYDROXYQUINOLINE-4(1H)-ONE AND METHODS OF THEIR PREPARATION AND UTILIZATION - Derivatives of 2-phenyl-3-hydroxyquinoline-4(1H)-one of the general formula (II), where X represents a nitro group, amino group, and Y represents an atom of halogen, oxygen or sulphur substituted by C | 01-28-2010 |
20100029714 | AQUEOUS PHARMACEUTICAL SUSPENSIONS CONTAINING REBAMIPIDE AND MANUFACTURING PROCESS THEREOF - The invention provides a rebamipide-containing aqueous pharmaceutical suspension which can be prepared by a simple process and keep the dispersed fine-particle state of rebamipide stable without having the fine particle agglutinated. The rebamipide-containing aqueous pharmaceutical suspension of the invention is prepared by mixing polyvinyl alcohol and additionally a sodium salt compound with rebamipide. | 02-04-2010 |
20100029715 | POLYMORPHIC FORMS OF A MACROCYCLIC INHIBITOR OF HCV - Provided are crystalline forms of the compound of formula (I), which is a macrocyclic inhibitor of HCV, processes for the preparation thereof, and pharmaceutical compositions comprising these crystalline forms. | 02-04-2010 |
20100041697 | PNEUMONIA TREATMENT - This invention relates to a method of treating pneumonia by orally administering to a subject in need thereof a quinolone compound of formula (I), shown in the disclosure, at a daily dose of 2-30 mg/kg. | 02-18-2010 |
20100048620 | COMPOSITION FOR TREATMENT OF UNDIFFERENTIATED GASTRIC CANCER - Disclosed are: a therapeutic agent, a kit and a treatment method for undifferentiated gastric cancer; and a pharmaceutical composition, a kit and a treatment method which are more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. A combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on undifferentiated gastric cancer. The combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. | 02-25-2010 |
20100048621 | MEDICAMENT FOR TREATING CHRONIC OBSTRUCTIVE PULMONARY DISEASE - The invention relates to a medicament for treating chronic obstructive pulmonary disease comprising as active ingredients a carbostyril derivative of formula (1): wherein A is a lower alkylene group, R is a cycloalkyl group, the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond, or a salt thereof; and probucol. | 02-25-2010 |
20100069434 | Compositions of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein. | 03-18-2010 |
20100069435 | METHOD OF SELECTIVELY INTRODUCING AMINO SUBSTITUENT - Provided are a technique for position-selectively introducing an amino group into a difluorobenzoic acid, a novel process for producing a quinolonecarboxylic acid derivative serving as an antibacterial agent, and intermediates in the production. The process comprises treating a compound represented by formula (6): | 03-18-2010 |
20100087481 | ORAL PHARMACEUTICAL FORMULATIONS FOR ANTIDIABETIC COMPOUNDS - Oral pharmaceutical preparations of salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. The oral pharmaceutical preparation is useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation. | 04-08-2010 |
20100093791 | Therapeutic Compositions - There is provided the use of a 5-HT | 04-15-2010 |
20100093792 | CRYSTALLINE FORMS OF A POTENT HCV INHIBITOR - This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: | 04-15-2010 |
20100105728 | DIHYDRO-[1H]-QUINOLIN-2-ONE DERIVATIVES AS RXR AGONISTS FOR THE TREATMENT OF DYSLIPIDEMIA, HYPERCHOLESTEROLEMIA AND DIABETES - The present invention relates to compounds of Formula (I), | 04-29-2010 |
20100113514 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula : | 05-06-2010 |
20100113515 | PTEN INHIBITOR OR MAXI-K CHANNELS OPENER - A new PTEN opener or a new opener of a large conductance Ca | 05-06-2010 |
20100120849 | Compositions for Treating Hyperproliferative Vascular Disorders and Cancers - The present invention relates to a pharmaceutical composition for preventing or treating hyperproliferative vascular disorders, and a pharmaceutical anticancer composition comprising the compound represented by the Formula 1. The present compounds exhibit IC | 05-13-2010 |
20100120850 | Quinoline Derivatives, Pharmaceutical Compositions Comprising Them, and Their Use in Treating Central Nervous System and Peripheral Diseases - Compounds of Formula (I) wherein R | 05-13-2010 |
20100120851 | PRENYLTRANSFERASE INHIBITORS FOR OCULAR HYPERTENSION CONTROL AND THE TREATMENT OF GLAUCOMA - The invention concerns in one embodiment a method of treating glaucoma or elevated intraocular pressure comprising administering a pharmaceutically effective amount of a composition comprising at least one prenyltransferase inhibitor. In another embodiment, the invention concerns a composition for the treatment of elevated intraocular pressure and glaucoma comprising a pharmaceutically effective amount of a prenyltransferase inhibitor. | 05-13-2010 |
20100120852 | AROYL-PIPERIDINE DERIVATIVES AND METHOD OF TREATING DISORDERS INDUCED BY SUBSTANCE P - The invention relates to a method of administering N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(quinoloylamino)-piperidines of the formula | 05-13-2010 |
20100130546 | QUINOLONE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a quinolone compound represented by General Formula (1) | 05-27-2010 |
20100130547 | SOLID FORMS OF N-(4-(7-AZABICYCLO[2.2.1]HEPTAN-7-YL)-2-(TRIFLUORORMETHYL)PHENYL)-4-OXO-5- -(TRIFLUOROMETHYL)-1,4-DIHYROQUINOLINE-3-CARBOXAMIDE - The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith. | 05-27-2010 |
20100130548 | BIPHENYL DERIVATIVES AS MODULATORS OF VOLTAGE GATED ION CHANNELS - Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions. | 05-27-2010 |
20100137361 | Tetrahydro-Quinolinylurea Derivatives - This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. | 06-03-2010 |
20100144786 | QUINOLINE DERIVATIVES AS CRTH2 RECEPTOR LIGANDS - Specific quinoline derivatives are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component. | 06-10-2010 |
20100144787 | Quinolines and Their Therapeutic Use - Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R | 06-10-2010 |
20100160372 | TREATMENT OF PROTEINOPATHIES USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA antagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant. | 06-24-2010 |
20100168161 | DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR - The present relates to compounds of formula (I): | 07-01-2010 |
20100168162 | SELECTIVE INHIBITORS OF AKT AND METHODS OF USING SAME - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions. | 07-01-2010 |
20100173939 | ANTIVIRAL COMPOUNDS - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infection. | 07-08-2010 |
20100184803 | Treatment of Lysosomal Storage Diseases - Methods and compositions useful in the treatment or prevention of lysosomal storage diseases, such as Pompe's disease, Fabry's disease, Gaucher's disease, and Niemann-Pick disease, are provided. The treatment includes administering to a subject a farnesyl transferase inhibitor compound. The treatment may also include enzyme replacement therapy or gene therapy. | 07-22-2010 |
20100184804 | METHODS FOR THE PREVENTION OR TREATMENT OF BACTERIAL AND FUNGAL INFECTIONS - The present invention features improved methods for treating, stabilizing, or preventing a bacterial or a fungal infection in a plant or an animal, such as a mammal. In particular, these methods involve the use of a compound, that is controlled by MvfR, and that affects the expression of an MvfR protein or that promotes its modification or inactivation, or a compound produced by | 07-22-2010 |
20100197727 | Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) | 08-05-2010 |
20100197728 | CRYSTALLINE FORM OF A QUINOLINONE-CARBOXAMIDE COMPOUND - The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT | 08-05-2010 |
20100204270 | Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof. Several of these compounds are also claimed as such. Further the combination of the above compounds with other antibacterial agents is described | 08-12-2010 |
20100204271 | STABLE CRYSTAL OF 4-OXOQUINOLINE COMPOUND - Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2θ(°) as measured by X-ray powder diffractometry. | 08-12-2010 |
20100204272 | Compounds which have activity at M1 receptor and their uses in medicine - Compounds of formula (I) or a salt thereof are provided: | 08-12-2010 |
20100210684 | Amine salt of carbostyril derivative - The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects. | 08-19-2010 |
20100222381 | Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors - Compounds represented by Formula (I): | 09-02-2010 |
20100234421 | SUBSTITUTED 3-AMINO-2-MERCAPTOQUINOLINES AS KCNQ2/3 MODULATORS - The invention relates to substituted 3-amino-2-mercaptoquinolines, to processes for their preparation, to medicaments containing these compounds and to the use of these compounds in the preparation of medicaments. | 09-16-2010 |
20100234422 | Sulfonylated Heterocycles Useful for Modulation of the Progesterone Receptor - Compounds of the following structure are provided, wherein n, R | 09-16-2010 |
20100249182 | AMINOQUINOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Provided are a novel aminoquinoline compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, preparation method thereof, and a pharmaceutical composition for preventing or treating cutaneous cancer, comprising the aminoquinoline compound or pharmaceutically acceptable salt thereof. Since the compound of Formula 1 exhibits excellent anti-proliferative effect on melanoma tumor cells, it is useful for preventing or treating cutaneous cancer. | 09-30-2010 |
20100249183 | THERAPEUTIC USE OF N-(ARYLALKYL)-1H-PYRROLOPYRIDINE-2-CARBOXAMIDE DERIVATIVES - The invention concerns therapeutic use of compounds of general formula (I), wherein n, the pyrrolopyridine ring, X | 09-30-2010 |
20100267768 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 10-21-2010 |
20100280069 | CONTROLLED RELEASE LOCAL ANESTHETIC FOR POST DENTAL SURGERY AND METHOD OF USE - The present invention relates to a method of delivering local anesthetic after dental extraction surgery. The present invention relates to packing the tooth socket with a tinned release local anesthetic which is coordinated with an initial local anesthetic and which lasts up to 5 days. The socket can be surgically sealed or the implant can act as the sealing means. | 11-04-2010 |
20100280070 | NOVEL TETRAHYDROQUINOLINES AS AROMATASE INHIBITORS - The invention relates to synthesis and biological screening of novel tetrahydroquinolines of formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them for aromatase inhibition: (I). The present invention also relates to a process for the preparation of the novel tetrahydroquinolines, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in for aromatase inhibition, particularly in the treatment and/or prevention of cancer, particularly breast cancer, more particularly hormone dependent breast cancer. | 11-04-2010 |
20100292270 | TREATMENT OF CACHEXIA - The present invention provides a means for prevention and treatment of cachexia and other chronic illnesses including but not limited to the promotion of weight gain, reduction or prevention of weight loss by administration of a substance that both reduces the sensitivity of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propranolol, tertatolol or bopindolol are preferred for this purpose. | 11-18-2010 |
20100292271 | Quinoline Compounds Suitable for Treating Disorders that Respond to Modulation of the Serotonin-5-HT6 Receptor - The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin | 11-18-2010 |
20100298375 | MEDICAMENT COMPRISING A CARBOSTYRIL DERIVATIVE AND DONEPEZIL FOR TREATING ALZHEIMER'S DISEASE - The invention relates to a medicament for treating Alzheimer's disease comprising as active ingredients a carbostyril derivative of the general formula: wherein A is a lower alkylene group, R is a cycloalkyl group, the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond, or a salt thereof; and donepezil or a salt thereof. | 11-25-2010 |
20100317692 | Quinolone M1 Receptor Positive Allosteric Modulators - The present invention is directed to quinolone compounds of general formula (I) | 12-16-2010 |
20100317693 | 3,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE - To provide a compound which has a potent agonistic activity on GHS-R and which is useful as a therapeutic agent for systemic wasting diseases such as cachexia. | 12-16-2010 |
20100324087 | COMBINED USE OF ANGIOGENESIS INHIBITOR AND TAXANE - The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with taxane. | 12-23-2010 |
20100324088 | Fused Pyridone M1 Receptor Positive Allosteric Modulators - The present invention is directed to fused pyridone compounds of formula (I) (I) that are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 12-23-2010 |
20100331363 | TREATMENT OF MITOCHONDRIAL DISORDERS USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject an amount of a farnesyl transferase inhibitor, wherein the amount administered is sufficient to cause an improvement in mitochondrial health in said subject. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant. | 12-30-2010 |
20110015224 | COMBINATION OF A CARBOSTYRIL AND CARNITINE - The present invention relates to a medicament for treating occlusive and/or ischemic vascular disorder comprising a carbostyril derivative and carnitine. | 01-20-2011 |
20110021561 | QUINOLINE COMPOUND AND PHARMACEUTICAL COMPOSITION, PREPARATION METHOD AND USES THEREOF - The present invention discloses a quinoline compound represented by the formula A or pharmaceutically acceptable solvate, optical isomer or polymorph thereof, | 01-27-2011 |
20110034508 | Treatment of BDNF-related disorders using laquinimod - This application provides for a method of increasing brain-derived neurotrophic factor (BDNF) serum level in a human subject comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to increase BDNF serum level in the human subject. The method can further comprise periodically administering to the subject an amount of a second BDNF-increasing agent. This application also provides for a method for treating a human subject suffering from a BDNF-related disease comprising periodically administering laquinimod or a pharmaceutically acceptable salt thereof in an amount effective to treat the human subject. This application additionally provides for use of laquinimod in the manufacture of a medicament for increasing BDNF serum level in a human subject. This application further provides for a pharmaceutical composition comprising an amount of laquinimod effective for use in increasing BDNF serum level in a human subject. This application also provides for a pharmaceutical preparation comprising an amount of laquinimod and an amount of a second BDNF-increasing agent effective for use in increasing BDNF serum level in a human subject. | 02-10-2011 |
20110034509 | Beta-2-Adrenoreceptor Agonists - Compounds of formula | 02-10-2011 |
20110039887 | CARBOSTYRIL DERIVATIVES INCLUDING CILOSTAZOL FOR TREATING FATTY LIVER - The invention relates to a medicament for preventing and/or treating fatty liver which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof. | 02-17-2011 |
20110060005 | TREATMENT OF MITOCHONDRIAL DISORDERS USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies and mitochondrial disorders are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject an amount of a farnesyl transferase inhibitor, wherein the amount administered is sufficient to stimulate mitophagy in said subject. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant. | 03-10-2011 |
20110077269 | DERIVATIVES FOR MODULATION OF ION CHANNELS - Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions. | 03-31-2011 |
20110098318 | FARNESYL PROTEIN TRANSFERASE INHIBITORS FOR TREATING BREAST CANCER - The present invention relates to the use of farnesyl protein transferase inhibitors for preparing pharmaceutical compositions for treating advanced breast cancer. | 04-28-2011 |
20110105557 | FARNESYL PROTEIN TRANSFERASE INHIBITOR COMBINATIONS WITH ANTIESTROGEN AGENTS - The present invention is concerned with combinations of a farnesyl transferase inhibitor and an antiestrogen agent for inhibiting the growth of tumor cells, useful in the treatment of cancer. | 05-05-2011 |
20110105558 | EYE-DROP PREPARATION AND USE THEREOF - Disclosed is a technique for preventing the decomposition of latanoprost (a thermally unstable substance) contained in an eye-drop solution to stabilize the eye-drop solution. Specifically disclosed is an eye-drop preparation comprising latanoprost and carteolol hydrochloride. By adding carteolol hydrochloride to an eye-drop solution containing latanoprost which is a thermally unstable substance and is likely to be adhered on the surface of a container, it becomes possible to prevent the decomposition of latanoprost in the eye-drop solution and also prevent the loss of latanoprost caused by the adsorption of latanoprost on the surface of a container. | 05-05-2011 |
20110112141 | CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF - Disclosed is a process for the preparation of laguinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics. | 05-12-2011 |
20110118308 | CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF - Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics. | 05-19-2011 |
20110118309 | USE OF HDAC INHIBITORS FOR THE TREATMENT OF HODGKIN'S DISEASE - The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I): | 05-19-2011 |
20110124682 | PHARMACEUTICAL COMPOSITION COMPRISING REBAMIPIDE - An object of the present invention is to provide a pharmaceutical composition containing rebamipide, which is unnecessary to be re-dispersed, has an enough transparency, and exhibits neutral to weakly acidic pH not to injure the keratoconjunctiva of a patient suffering from dry eye. The present pharmaceutical composition comprises (1) rebamipide, (2) an amino sugar, and (3) an buffer agent, which has no inorganic cation. | 05-26-2011 |
20110136861 | QUINOLONE INHIBITORS OF LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 - The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof. | 06-09-2011 |
20110136862 | NOVEL TETRAMETHYL SUBSTITUTED PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel tetramethyl substituted pipehdine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 06-09-2011 |
20110136863 | N-Heterocyclic M1 Receptor Positive Allosteric Modulators - The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 06-09-2011 |
20110152316 | 3,4-SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS - The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position Isoqumolone and having the Formula (I): The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency. | 06-23-2011 |
20110166179 | ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or formula (Ib): | 07-07-2011 |
20110172268 | MECHANISM-BASED SMALL-MOLECULE PARASITE INHIBITORS - Methods for preventing or treating an Apicomplexan parasite infection in a patient administering to a patient in need thereof an effective amount of a compound of Formulas I-IV. | 07-14-2011 |
20110172269 | ANTIOXIDANT COMBINATIONS FOR USE IN FEED RATIONS TO INCREASE MILK PRODUCTION AND MILK FAT - The present invention provides a combination of antioxidants that effectively stabilize different types of fats utilized in a ruminant diet. When included in a ruminant feed ration or water source, the antioxidant combination typically increases nutrient digestion, such as fiber and protein, improves rumen fermentation, improves microbial growth, improves microbial efficiency, increases milk production and/or milk fat, improves antioxidant status of the ruminant, and attenuates the negative effects of some fats in the ruminant animal. | 07-14-2011 |
20110190342 | GLYCINE B ANTAGONIST - The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders. | 08-04-2011 |
20110212993 | MEDICAMENT FOR TREATING GLAUCOMA COMPRISING AS AN ACTIVE INGREDIENT CYCLODEXTRIN-CLATHRATE COMPOUND OF CILOSTAZOL - The invention relates to an ophthalmic medicament for treating glaucoma which comprises a clathrate compound prepared by dissolving cilostazol or a salt thereof in a cyclodextrin. | 09-01-2011 |
20110230519 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 09-22-2011 |
20110230520 | NITRATE DERIVATIVES OF CILOSTAZOL FOR THE TREATMENT OF VASCULAR AND METABOLIC DISEASES - Nitrate derivatives of cilostazol are described. They have superior properties and clinical advantages compared to cilostazol in the treatment of vascular and metabolic diseases. | 09-22-2011 |
20110251234 | MESYLATE SALT OF 5-(2--1-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2(1H)-ONE AS AGONIST OF THE BETA2 ADRENERGIC RECEPTOR - The present disclosure relates to a mesylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 receptor. | 10-13-2011 |
20110251235 | STABLE LAQUINIMOD PREPARATIONS - The invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable salt of N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, N-methylglucamine, and a pharmaceutically acceptable carrier. | 10-13-2011 |
20110269794 | External Preparation for Athlete's Foot Treatment - External preparations for athlete's foot treatment capable of enhancing patient's compliance and capable of reducing the symptom of rubefaction, comprising an anti-trichophyton drug mixed with at least one compound selected from among 1-menthol, menthol analogue compounds and bactericidal compounds. | 11-03-2011 |
20110288121 | Processes for Producing Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to the process for producing modulators of cystic fibrosis transmembrane conductance regulator (CFTR). | 11-24-2011 |
20110288122 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 11-24-2011 |
20110288123 | FORMULATIONS FOR THE TREATMENT OF ACUTE HERPES ZOSTER PAIN - The present invention provides compositions and methods that are useful for treatment of pain associated with acute herpes zoster. The aqueous compositions are non-stinging and non-irritating. | 11-24-2011 |
20110306634 | Amorphous Salt of a Macrocyclic Inhibitor of HCV - The amorphous form of the sodium salt of the macrocyclic inhibitor of HCV of formula: | 12-15-2011 |
20110312994 | BIPHENYL DERIVATIVES - This invention provides biphenyl derivatives of formula I: | 12-22-2011 |
20110312995 | BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS - This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. | 12-22-2011 |
20110319446 | BICYCLO[2.2.1]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES - Compounds of formula (I) have muscarinic M3 receptor modulating activity; | 12-29-2011 |
20120010237 | COMPOUNDS HAVING ANTIPARASITIC OR ANTI-INFECTIOUS ACTIVITY - A method for inhibiting a parasitic or infectious disease in a subject, wherein the parasitic or infectious disease is selected from one caused by | 01-12-2012 |
20120010238 | DEUTERATED N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQ- UINOLINE-3-CARBOXAMIDE, SALTS AND USES THEREOF - The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses. | 01-12-2012 |
20120010239 | 5-CHLORO-4-HYDROXY-1-METHYL-2-OXO-N-PHENYL-1,2-DIHYDROQUINOLINE-3-CARBOXAM- IDE, SALTS AND USES THEREOF - The subject invention provides 5-chloro-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide, its salts and uses. | 01-12-2012 |
20120015977 | QUINOLINONE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS - The present invention relates to novel quinolinone derivatives (I), efficacious in animal models of CNS disorders and, as such, valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders. In other aspects the invention relates to pharmaceutical compositions comprising the quinolinone derivatives of the invention and to the use of these compounds for therapeutic applications. | 01-19-2012 |
20120029014 | 5-(2--1-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2 (1H)-ONE FOR THE TREATMENT OF LUNG FUNCTION - A compound which is a hydroxyquinolinone derivative of formula (I), | 02-02-2012 |
20120029015 | Novel medical use of kynurenic acid, its precursors and derivatives - The invention relates to the use of kynurenic acid derivatives of general formula (I), | 02-02-2012 |
20120035212 | (L)-Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide - Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane- | 02-09-2012 |
20120046313 | SILOXANE POLYMER CONTAINING TETHERED FLUOROQUINOLONE - A polymer that is a polysiloxane polymer has fluoroquinolone antibiotic groups, or pharmaceutically acceptable salts thereof, attached via linkers. The linkers may be hydrolytically labile thereby providing a manner of releasing the fluoroquinolone antibiotic from the polymer. | 02-23-2012 |
20120059033 | Crystalline Salts of a Potent HCV Inhibitor - This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: | 03-08-2012 |
20120071504 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - This invention relates to a compound of Formula I: | 03-22-2012 |
20120071505 | SUBSTITUTED PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE TO TREAT OXIDATIVE STRESS - Substituted pyridine derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted pyridine derivative, and methods of use in treating inflammation are provided. The substituted pyridine derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase. | 03-22-2012 |
20120071506 | METHODS FOR TREATING CNS DISORDERS WITH BICYCLO-SUBSTITUTED 2-IMIDAZOLINE AND 2-IMIDAZOLES - The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I | 03-22-2012 |
20120077842 | QUINOLINE DERIVATIVE-CONTAINING PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof; and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor: | 03-29-2012 |
20120108631 | Sulfonamides for the Modulation of PKM2 - The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder. | 05-03-2012 |
20120108632 | PRENYLTRANSFERASE INHIBITORS FOR OCULAR HYPERTENSION CONTROL AND THE TREATMENT OF GLAUCOMA - The invention concerns in one embodiment a method of treating glaucoma or elevated intraocular pressure comprising administering a pharmaceutically effective amount of a composition comprising at least one prenyltransferase inhibitor. In another embodiment, the invention concerns a composition for the treatment of elevated intraocular pressure and glaucoma comprising a pharmaceutically effective amount of a prenyltransferase inhibitor. | 05-03-2012 |
20120115904 | COMPOUNDS HAVING ANTIPARASITIC OR ANTI-INFECTIOUS ACTIVITY - Compounds of formula I: | 05-10-2012 |
20120122921 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 05-17-2012 |
20120122922 | COMPOSITIONS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein. | 05-17-2012 |
20120136025 | QUINOLONE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R | 05-31-2012 |
20120142729 | KAT ll INHIBITORS - The present invention relates to compounds 3-amino-1-hydroxy-2-oxo-1,2,3,4-tetrahydroquinoline-7-carbonitrile, 3-amino-1-hydroxy-7-(2-methoxyethoxy)-3,4-dihydroquinolin-2(1H)-one, and 3-amino-1-hydroxy-7-[(1S)-2-methoxy-1-methylethoxy]-3,4-dihydroquinolin-2(1H)-one, including racemic mixtures and resolved enantiomers thereof, to pharmaceutically acceptable salts thereof, and to the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans. | 06-07-2012 |
20120142730 | USE OF LAQUINIMOD FOR REDUCING FATIGUE, IMPROVING FUNCTIONAL STATUS, AND IMPROVING QUALITY OF LIFE IN MULTIPLE SCLEROSIS PATIENTS - The subject invention provides methods for reducing or inhibiting progression of the level of fatigue in a multiple sclerosis human patient, for improving or inhibiting deterioration of the functional status of a multiple sclerosis human patient, and for improving or inhibiting deterioration of the general health of a multiple sclerosis human patient, comprising orally administering to the human patient laquinimod or a pharmaceutically acceptable salt thereof. The subject invention also provides a method for providing neuroprotection to a human subject, the method comprising orally administering to the human subject laquinimod or a pharmaceutically acceptable salt thereof. | 06-07-2012 |
20120157492 | ANTIBIOTIC DRUG - This invention relates to a malic acid salt of (3S,5R)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid. Also disclosed is a method of treating bacterial infection by an effective amount of this salt. | 06-21-2012 |
20120165369 | 3-SUBSTITUTED QUINOLINIUM AND 7H-INDOLO[2,3-c]QUINOLINIUM SALTS AS NEW ANTIINFECTIVES - The present invention relates to quinolinium antiinfective agents in which the qunolinium nucleus is fused to an indole ring or the qunolinium nucleus is linked to a cyclic structure through an opened indole or a benzothiophene or benzofuran ring. The compound is further substituted with various substituent groups. | 06-28-2012 |
20120165370 | QUINOLINE DERIVATIVES AS ANTI-CANCER AGENTS - Quinoline derivatives showing anticancer activities against cancer cell lines of hepatocellular carcinoma (Hep3B), lung carcinoma (A549), esophageal squamous cell carcinoma (HKESC-1, HKESC-4 and KYSE150). The quinoline derivatives have a backbone structure of the following formulas: | 06-28-2012 |
20120165371 | SPIRO SUBSTITUTED COMPOUNDS AS ANGIOGENESIS INHIBITORS - The present invention relates to spiro (tetracarbon) substituted compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans. | 06-28-2012 |
20120165372 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof. | 06-28-2012 |
20120172394 | PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING RHEUMATOID ARTHRITIS, CONTAINING REBAMIPIDE - The present invention provides a pharmaceutical composition for preventing or treating rheumatoid arthritis comprising rebamipide as an active ingredient and a pharmaceutically acceptable carrier. The pharmaceutical composition may be for oral administration, for example an oral solid dosage form of a tablet or capsule form. The pharmaceutical composition may be formulated into a unit dosage form suitable for orally administering rebamipide in a dose ranging from 0.5 to 50 mg/kg, preferably from 0.6 to 6 mg/kg. | 07-05-2012 |
20120172395 | SLOW-RELEASE CILOSTAZOL TABLET HAVING AN IMPROVED ELUTION RATE AND MINIMAL SIDE EFFECTS - Provided is a slow-release tablet including cilostazol as a pharmacologically active component, which is efficacious in suppressing aggregation of blood platelets and promoting vascular relaxation by inhibiting phosphodiesterase types. The slow-release cilostazol tablet has an extended elution time so that the slow-release cilostazol tablet can be taken once daily for convenience of drug use, and minimizes the manifestation of headache which is one side effect caused when women, the elderly and children take conventional cilostazol preparations so that the convenience of drug use can be improved. Also, the slow-release cilostazol tablet exhibits a stable elution pattern with no variation in elution rate according to changes in pH in the stomach and intestines, as well as an effect of delaying the release of a drug, using a mixture of hydroxypropyl methylcellulose and a carbomer as a release-controlling polymer. | 07-05-2012 |
20120184579 | Quinolines and Their Therapeutic Use - Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R | 07-19-2012 |
20120196894 | NOVEL TRPA1 ANTAGONISTS - The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels. | 08-02-2012 |
20120202848 | THERAPY OF AUTOIMMUNE COLITIS USING A TIP60 INHIBITOR - This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases. | 08-09-2012 |
20120208843 | Method of Using GPR35 to Identify Metabolic-Stabilizing Compounds - The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to a method for treating or preventing a metabolic-related disorder, comprising administering to an individual in need thereof an effective amount of a GPR35 modulator. | 08-16-2012 |
20120214841 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 08-23-2012 |
20120220625 | PHARMACEUTICAL COMPOSITION AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention. | 08-30-2012 |
20120220626 | NOVEL QUINOLINE COMPOUND, AND COMPOSITION CONTAINING CENTIPEDE EXTRACT OR COMPOUNDS ISOLATED THEREFROM FOR PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASE - The present invention relates to a composition for the prevention and treatment of cardiovascular diseases containing the novel quinoline compound, the centipede extracts or compounds isolated from the extracts. The novel quinoline compound, the centipede extracts or a quinoline compound and a phenol compound isolated from the extracts of the invention exhibit excellent LDL-antioxidant activity, ACAT inhibiting activity, and anti-inflammatory activities, so that they can be included as an effective ingredient in a composition for the prevention and treatment of cardiovascular disease including hyperlipidemia, atherosclerosis, coronary heart disease, and myocardial infarction mediated by LDL-oxidation, cholesteryl ester synthesis and accumulation, and inflammation. | 08-30-2012 |
20120252840 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1. | 10-04-2012 |
20120252841 | Substituted 2-mercaptoquinoline-3-carboxamides as KCNQ2/3 modulators - The invention relates to substituted 2-mercaptoquinoline-3-carboxamides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments. | 10-04-2012 |
20120258983 | Pharmaceutical Composition and Administrations Thereof - The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention. | 10-11-2012 |
20120270899 | Compositions and Methods for Treating Cardiovascular Diseases - The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions. | 10-25-2012 |
20120277264 | ANTITHROMBOTIC AGENT - An object of the present invention is to provide an antithrombotic agent that has fewer side effects and that is highly effective. The present invention provides an antithrombotic agent comprising (±)-[2-[4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl]ethyl]dimethylsulfonium p-toluenesulfonate represented by Formula (1) as an active ingredient. | 11-01-2012 |
20120283289 | CRYSTALLINE FORM OF A BIPHENYL COMPOUND - The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder. | 11-08-2012 |
20120302600 | STABLE LAQUINIMOD PREPARATIONS - The invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable salt of N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, N-methylglucamine, and a pharmaceutically acceptable carrier. | 11-29-2012 |
20120329829 | Dopamine Transporter Inhibitors for Use in Treatment of Movement Disorders and Other CNS Indications - The invention provides a class of dopamine transporter inhibitors of formula (I) (DAS inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses treating, or the manufacturing medicaments for treating disease conditions, including Parkinson's disease, Hoehn and Yahr Staging of Parkinson's Disease. Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided. | 12-27-2012 |
20130005765 | Methods and Compositions for Controlling Ectoparasites - A method for inhibiting hatching of an ectoparasite egg, the method comprising exposing the ectoparasite egg to at least one metal chelating agent and/or metalloprotease inhibitor, wherein the metal chelating agent is a compound comprising at least two heteroatoms able to simultaneously coordinate with a metal ion, at least one of the two heteroatoms being selected from nitrogen, sulfur, oxygen and phosphorus, wherein the compound comprises at least one carbocyclic ring substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom, or the compound comprises at least one heterocyclic ring containing at least one heteroatom, wherein said heterocyclic ring is optionally substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom is provided. Methods of treating ectoparasite infestations and compositions for use in such methods are also provided. | 01-03-2013 |
20130005766 | 5-[(3,3,3-TRIFLUORO-2-HYDROXY-1-ARYLPROPYL)AMINO]-1H-QUINOLIN-2-ONES, A PROCESS FOR THEIR PRODUCTION AND THEIR USE AS ANTI-INFLAMMATORY AGENTS - The present invention relates to compounds of formula I, | 01-03-2013 |
20130005767 | THERAPEUTIC COMPOUNDS - Disclosed herein are compounds of the formula | 01-03-2013 |
20130012537 | 3,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE - A method for treatment of a systemic wasting disease, by administering, to a subject in need thereof, an effective amount of a 3,8-diaminotetrahydroquinoline derivative represented by formula (Ia) (wherein X represents CH | 01-10-2013 |
20130018071 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 01-17-2013 |
20130030016 | QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS - Method of treating a bacterial infection other than a Mycobacterial infection, using a compound of formula (Ia) or (Ib) | 01-31-2013 |
20130030017 | QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS - Method of treating a bacterial infection other than a Mycobacterial infection, using a compound of formula (Ia) or (Ib) | 01-31-2013 |
20130040989 | 1-CYCLOPROPYL-8-METHYL-7-[5-METHYL-6-(METHYLAMINO)-3-PYRIDINYL]-4-OXO-1,4-- DIHYDRO-3-QUINOLINECARBOXYLIC ACID SALTS - There is provided a salt of 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid selected from the group consisting of citrate, hemi-fumarate, maleate, L-tartrate, mesylate, hydrochloride, potassium, and sodium salts. | 02-14-2013 |
20130045989 | STABILIZED CRYSTAL OF 2-ETHYL-3,7-DIMETHYL-6-(4-(TRIFLUOROMETHOXY)PHENOXY)QUINOLINE-4-YL METHYL CARBONATE, PROCESS FOR PRODUCING THE CRYSTAL, AND AGRICULTURAL CHEMICAL COMPOSITION COMPRISING THE CRYSTAL - An objective of the present invention is to provide a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate having stable physicochemical properties. | 02-21-2013 |
20130065920 | PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR TREATMENT OF OSTEOARTHRITIS CONTAINING REBAMIPIDE AS AN ACTIVE INGREDIENT - The present invention provides a pharmaceutical composition for preventing or treating osteoarthritis comprising rebamipide as an active ingredient and a pharmaceutically acceptable carrier. The pharmaceutical composition may be for oral administration, for example an oral solid dosage form of a tablet or capsule form. The pharmaceutical composition may be formulated into a unit dosage form suitable for orally administering rebamipide in a dose ranging from 0.5 to 50 mg/kg, preferably from 0.6 to 6 mg/kg. | 03-14-2013 |
20130065921 | PTEN INHIBITOR OR MAXI-K CHANNELS OPENER - A new PTEN opener or a new opener of a large conductance Ca | 03-14-2013 |
20130065922 | NOVEL AMIDES AS FUNGICIDES - Compounds of the general formula (I), wherein the substituents are as defined in claim | 03-14-2013 |
20130072522 | Process for Making Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The invention provides a process for the preparation of a compound of Formula 1, | 03-21-2013 |
20130079367 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 03-28-2013 |
20130085158 | SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 04-04-2013 |
20130090354 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 04-11-2013 |
20130096157 | QUINOLINE DERIVATIVES AND USES OF THE SAME - Provided is a quinoline derivative of Chemical Formula (I): | 04-18-2013 |
20130096158 | Treatment Of Multiple Sclerosis With Combination Of Laquinimod And Fingolimod - This invention provides a method of treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome comprising administering to the subject laquinimod as an add-on therapy to or in combination with fingolimod. This invention also provides a package and a pharmaceutical composition comprising laquinimod and fingolimod for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention also provides laquinimod for use as an add-on therapy or in combination with fingolimod in treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention further provides use of laquinimod and fingolimod in the preparation of a combination for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. | 04-18-2013 |
20130102630 | Derivatives of the Aminated Hydroxyquinoline Class For Treating Cancers - The invention relates to compounds of the aminated hydroxyquinoline type capable of preventing the migration of metastases or tumoral cells. Such compounds are useful for treating cancers. | 04-25-2013 |
20130102631 | NOVEL MICROBIOCIDAL DIOXIME ETHER DERIVATIVES - The present invention provides compounds of formula (I) wherein R | 04-25-2013 |
20130109717 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE | 05-02-2013 |
20130116279 | BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. | 05-09-2013 |
20130116280 | Fusion protein comprising C-terminal domain of RET protein and use thereof as a diagnosing marker - A fusion protein including N-terminal domain of a fusion partner at N-terminal and C-terminal domain of RET protein at C-terminal, a fusion gene encoding the fusion protein, and a use of the fusion protein or the fusion gene as a diagnosing marker for a cancer, are provided. | 05-09-2013 |
20130123301 | CRYSTALLINE SALTS OF QUINOLINE COMPOUNDS AND METHODS FOR PREPARING THEM - A stable solid pharmaceutical composition consisting essentially of an effective amount of a crystalline salt of formula (II) | 05-16-2013 |
20130131107 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 05-23-2013 |
20130137722 | SOLID FORMS OF N-(4-(7-AZABICYCLO[2.2.1]HEPTAN-7-YL)-2-TRIFLUOROMETHYL)PHENYL)-4-OXO-5-(- TRIFLUOROMETHYL)-1,4-DIHYDROQUINOLINE-3-CARBOXAMIDE - The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith. | 05-30-2013 |
20130137723 | CRYSTAL OF ANTI-BACTERIAL COMPOUND - It is intended to provide a salt of a compound and crystals thereof useful as a therapeutic and/or preventive agent for infectious diseases which has wide and excellent antibacterial activity and has excellent safety. | 05-30-2013 |
20130143918 | Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl-6-F- luoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxa- mide - The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith. | 06-06-2013 |
20130143919 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 06-06-2013 |
20130150404 | BIPHENYL DERIVATIVES - This invention provides biphenyl derivatives of formula I: | 06-13-2013 |
20130165479 | ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF - The present application is directed to compounds that are TRPV1 antagonictc and have formula (I) | 06-27-2013 |
20130178498 | BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. | 07-11-2013 |
20130178499 | Novel Substituted Quinoline Compounds as S-Nitrosoglutathione Reductase Inhibitors - The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same. | 07-11-2013 |
20130184310 | TREATMENT OF LUPUS ARTHRITIS USING LAQUINIMOD - This invention provides a method of treating a subject afflicted with active lupus arthritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus arthritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with lupus arthritis. | 07-18-2013 |
20130203806 | CILOSTAZOL COCRYSTALS AND COMPOSITIONS - The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of cilostazol. Disclosed herein are several new compositions and cocrystals of cilostazol, including: a 1:1 cilostazol gentisic acid cocrystal, a 1:1:1 cilostazol gentisic acid H | 08-08-2013 |
20130203807 | USE OF LAQUINIMOD FOR TREATING CROHN'S DISEASE PATIENTS WHO FAILED FIRST-LINE ANTI-TNF THERAPY - This application provides for a method of treating a human patient afflicted with anti-TNFα refractory Crohn's disease, of treating a human patient afflicted with non-fibrostenotic Crohn's disease, and of treating a human patient whose Crohn's disease had not been surgically treated, the method comprising periodically administering to the patient an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the patient. This application also provides for a method of inducing or maintaining clinical remission in a human patient afflicted with Crohn's disease comprising periodically administering to the patient an amount of laquinimod effective to induce or maintain clinical remission in the patient, which amount of laquinimod is less than 0.5 mg/day. | 08-08-2013 |
20130203808 | Drug for degradation and treatment of biofilms - The invention comprising decoquinate and one or both of a redox drug or macrolide drug for prophylaxis or treatment of certain biofilms and plaques in humans and animals. | 08-08-2013 |
20130217724 | N-ETHYL-N-PHENYL-1,2-DIHYDRO-4,5-DI-HYDROXY-1-METHYL-2-OXO-3-QUINOLINECARB- OXAMIDE, PREPARATION AND USES THEREOF - The subject invention provides a pharmaceutical composition containing laquinimod or a pharmaceutically acceptable salt thereof, and a compound of N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide or a salt thereof. | 08-22-2013 |
20130217725 | Macrocyclic Inhibitors Of Hepatitis C Virus - Inhibitors of HCV replication of formula (I) | 08-22-2013 |
20130231367 | BETA2-ADRENORECEPTOR AGONISTS - Compounds of formula | 09-05-2013 |
20130231368 | Solid Forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluorormethyl)phenyl)-4-oxo-5- -(trifluoromethyl)-1,4-dihyroquinoline-3-carboxamide - The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith. | 09-05-2013 |
20130237564 | Combinations of Glycopyrrolate and Beta2 Adrenoceptor Agonists - A medicament comprising, separately or together (A) glycopyrrolate; and
| 09-12-2013 |
20130237565 | Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinoli- necarboxamide - A pharmaceutical composition comprising: an active ingredient consisting of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, salt thereof, or solvate of the foregoing; and (i) a compound, a 5% (w/w) aqueous solution or suspension of which has a pH of 8 or more, and/or (ii) silicic acid, salt thereof, or solvate of the foregoing is a highly stable pharmaceutical composition, wherein under humidified and heated storage conditions, the decomposition of said compound is sufficiently reduced, or the gelation on the surface of the pharmaceutical composition is sufficiently inhibited. | 09-12-2013 |
20130245065 | INTERMEDIATE COMPOUNDS AND PROCESSES FOR THE PREPARATION OF QUINOLINE DERIVATIVES SUCH AS LAQUINIMOD SODIUM - The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes. | 09-19-2013 |
20130253006 | 2-SELENOPHENE-4-QUINOLONES AS ANTICANCER AGENTS - 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na | 09-26-2013 |
20130253007 | Compounds That Modulate Oxidative Stress - The present invention provides methods of identifying compounds that selectively induce an oxidative stress response in a biological sample. The present invention further provides methods of treating a subject having a disease associated with oxidative stress using compounds that selectively induce an oxidative stress response in the subject. The invention further provides methods of selectively inducing an oxidative stress response in a cell. | 09-26-2013 |
20130267558 | PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING ALCOHOLIC LIVER DISEASES, CONTAINING CILOSTAZOL AS ACTIVE INGREDIENT - Provided is a pharmaceutical composition for the treatment and prevention of alcoholic liver diseases, including cilostazol as an active ingredient. Cilostazol inhibits expression levels of TNF-α and FAS (fatty acid synthase) gene in a concentration-dependent manner, and also significantly inhibits the activity of caspase-3. Accordingly, cilostazol shows superior effects for the treatment or prevention of alcoholic liver diseases, in particular, alcoholic hepatitis compared to pentoxifylline which is conventionally used as a therapeutic agent for the treatment for alcoholic hepatitis. Thus, cilostazol is suitable for use as a drug for the treatment or prevention of alcoholic hepatitis. | 10-10-2013 |
20130267559 | Quinolinone Derivatives - The present invention relates to compounds which are quinolinone derivatives of general formula (I) capable of modulating the activity, in particular of inducing the differentiation, of stem and progenitor cells; these compounds are of use in the treatment of disorders related to a stem differentiation defect; the invention also relates to novel compounds among these quinolinone derivatives and to pharmaceutical compositions containing the same. | 10-10-2013 |
20130281487 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith. | 10-24-2013 |
20130296365 | QUINOLINE DERIVATIVE-CONTAINING PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof, and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor: | 11-07-2013 |
20130303569 | USE OF HIGH DOSE LAQUINIMOD FOR TREATING MULTIPLE SCLEROSIS - Disclosed herein are methods of treating a human patient afflicted with multiple sclerosis (MS) or presenting a clinically isolated syndrome (CIS), for treating a human subject by providing neuroprotection, and of treating a human patient afflicted with MS or presenting a CIS by increasing the time to confirmed disease progression and/or confirmed relapse or reducing brain atrophy, comprising orally administering a daily dose of about 1.2 mg laquinimod or a pharmaceutically acceptable salt thereof. Also disclosed is a pharmaceutical oral unit dosage form of about 1.2 mg laquinimod or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier for use in treating a human patient afflicted with MS or presenting a CIS, in treating a human subject by providing neuroprotection, or in treating a human patient afflicted with MS or presenting a CIS by increasing the time to confirmed disease progression and/or confirmed relapse or reducing brain atrophy. | 11-14-2013 |
20130303570 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 11-14-2013 |
20130317060 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to solid state forms of N—[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 11-28-2013 |
20130317061 | Crystalline Salts of a Potent HCV Inhibitor - This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: | 11-28-2013 |
20130324574 | TREATMENT OF OCULAR INFLAMMATORY DISEASES USING LAQUINIMOD - Disclosed is a method for treating an ocular inflammatory disease (OID), e.g., uveitis or conjunctivitis, comprising periodic administration of a therapeutically effective amount of laquinimod or a pharmaceutically acceptable salt thereof. Also provided is a pharmaceutical composition comprising laquinimod or a pharmaceutically acceptable salt thereof for use in treating a subject suffering from an OID, uveitis, bacterial conjunctivitis, viral conjunctivitis, an inflammation of the orbital tissue, the lacrimal apparatus, the eyelid, the cornea, the retina or the optic pathway. This application also provides a method for treating a subject suffering from an autoimmune disease-associated ocular inflammation comprising periodic ocular administration to the subject a therapeutically effective amount of laquinimod or a pharmaceutically acceptable salt, and an ocular pharmaceutical composition comprising laquinimod or a pharmaceutically acceptable salt thereof for use in treating an autoimmune disease-associated ocular inflammation. | 12-05-2013 |
20130331412 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 12-12-2013 |
20130338188 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 12-19-2013 |
20130338189 | CRYSTAL OF ANTI-BACTERIAL COMPOUND - It is intended to provide a salt of a compound and crystals thereof useful as a therapeutic and/or preventive agent for infectious diseases which has wide and excellent antibacterial activity and has excellent safety. | 12-19-2013 |
20130345256 | N-ETHYL-4-HYDROXYL-1-METHYL-5-(METHYL(2,3,4,5,6-PENTAHYDROXYHEXYL)AMINO)-2- -OXO-N-PHENYL-1,2-DIHYDROQUINOLINE-3-CARBOXAMIDE - The subject invention provides pharmaceutical compositions containing laquinimod or a pharmaceutically acceptable salt thereof, an isolated compound of N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide or a salt thereof, compositions containing N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide and methods of preparing the same. | 12-26-2013 |
20130345257 | COMPOSITION FOR LUPUS NEPHRITIS AND METHODS OF MAKING AND USING THE SAME - Provided herein are compositions and methods associated with the prevention and treatment of lupus nephritis. In particular, provided herein is a method for delaying onset of active lupus nephritis in a subject at risk for developing active lupus nephritis, comprising periodically administering to the subject an amount of laquinimod effective to delay onset of active lupus nephritis in the subject. Also provided herein are laquinimod (LAQ) and a pharmaceutical composition comprising an amount of LAQ for use in delaying onset of active lupus nephritis in a subject at risk for developing active lupus nephritis. | 12-26-2013 |
20140018385 | Identification Of PCNA Targeting Compounds For Cancer Therapy And PCNA Function Regulation - Pharmaceutical compositions and methods for inhibiting cell growth, modulating function of PCNA, treating prostate cancer, and enhancing PCNA trimer formation are disclosed. The methods include administering an effective amount of a compound of Formula (I), Formula (II) | 01-16-2014 |
20140018386 | LAQUINIMOD FORMULATIONS WITHOUT ALKALIZING AGENT - The subject invention provides a stable pharmaceutical composition comprising a therapeutically effective amount of laquinimod, an amount of a filler, and an amount of a lubricant, wherein the stable pharmaceutical composition is free of an alkalizing agent or an oxidation reducing agent. Also provided are processes for making the stable pharmaceutical composition and sealed packages comprising the stable pharmaceutical composition. Also provided is a method for treating a subject afflicted with a form of multiple sclerosis (MS) or for alleviating a symptom of MS in a subject afflicted with a form of MS comprising administering to the subject a stable pharmaceutical composition as described herein. Also provided is use of a stable pharmaceutical composition as described herein for treating a subject afflicted with a form of MS or for alleviating a symptom of MS in a subject afflicted with a form of multiple MS. | 01-16-2014 |
20140018387 | OINTMENT WITH EXCELLENT FORMULATION STABILITY - Provided is an ointment which has excellent drug stability and excellent drug uniformity. The ointment, which comprises 1 to 5% by weight of 1-[2-[(4S)-4-hydroxy-1,2,3,4-tetrahydroquinolin-1-yl]-4-pyridyl]-2,3-bis(hydroxymethyl)-6,7-dimethoxynaphthalene•3/2 hydrate, 3 to 7% by weight of a separation inhibitor, 15 to 50% by weight of a hydrocarbon gel, a pH controller and 0.05 to 0.4% by weight of an antioxidant, has excellent drug stability and excellent drug dispersibility. In the present ointment, polyoxyethylene (196) polyoxypropylene (67) glycol is preferred as the separation inhibitor, diisopropanolamine is preferred as the pH controller, and dibutylhydroxytoluene is preferred as the antioxidant. | 01-16-2014 |
20140024677 | METHODS FOR INDUCING MITOCHONDRIAL BIOGENESIS - Methods and compositions for inducing mitochondrial biogenesis are provided. In some aspects, methods for the treatment of diseases such as acute kidney disease (AKI) or a muscle wasting disease by administering tomoxetine, nisoxetine, fenoterol, formoterol, or procaterol to an individual are provided. | 01-23-2014 |
20140024678 | STABLE LAQUINIMOD PREPARATIONS - The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5- chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4 -hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido) benzoic acid, 1H,3H-spiro[5-chloro- | 01-23-2014 |
20140039005 | NOVEL REBAMIPIDE COMPLEXES AND COCRYSTALS - New rebamipide complexes and new rebamipide cocrystals are disclosed, specifically a 1:1 rebamipide nicotinamide complex, a 1:1 rebamipide nicotinamide cocrystal, a 1:1 rebamipide 2,4-dihydroxybenzolc acid complex, and a 1:1 rebamipide 2,4-dihydroxybenzoic acid cocrystal. Pharmaceutical compositions containing a rebamipide complex or cocrystal of the invention and a pharmaceutically acceptable carrier and methods of treatment are also disclosed. | 02-06-2014 |
20140045885 | Decoquinate, 4-hydroxyquinolones and napthoquinones combined with levamisole, Imidazothiazole, for the prevention and treatment of sarcocystosis and equine protozoal myeloencephalitis caused by Sarcocystis and Neospora and other apicomplexan protozoans. - Apicomplexan parasites that infect horses such as | 02-13-2014 |
20140045886 | LAQUINIMOD FOR TREATMENT OF GABA MEDIATED DISORDERS - This invention provides a method of treating a subject suffering from a GABA related disorder comprising periodically administering to the subject an effective amount of laquinimod or pharmaceutically acceptable salt thereof in an amount effective to treat the subject. | 02-13-2014 |
20140045887 | LAQUINIMOD FOR TREATMENT OF CANNABINOID RECEPTOR TYPE 1(CB1) MEDIATED DISORDERS - This invention provides a method of treating a human subject suffering from a CB1 receptor related disorder comprising periodically administering to the subject an effective amount of laquinimod or pharmaceutically acceptable salt thereof in an amount effective to treat the subject. | 02-13-2014 |
20140045888 | COMPOUNDS HAVING ANTIPARASITIC OR ANTI-INFECTIOUS ACTIVITY - Compounds of formula I: | 02-13-2014 |
20140045889 | Combination Drug Containing Probucol and a Tetrazolyalkoxy-Dihydrocarbostyril Derivative With Superoxide Supressant Effects - This invention relates to a combination drug comprising a combination of a tetrazolylalkoxy-dihydrocarbostyril derivative of the formula: | 02-13-2014 |
20140051723 | DEUTERATED N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQ- UINOLINE-3-CARBOXAMIDE, SALTS AND USES THEREOF - The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses. | 02-20-2014 |
20140051724 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 02-20-2014 |
20140057943 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF. | 02-27-2014 |
20140066478 | Beta2-Adrenoreceptor Agonists - Compounds of formula | 03-06-2014 |
20140073667 | DEUTERATED CFTR POTENTIATORS - This invention relates to compounds of Formula I: | 03-13-2014 |
20140080867 | Substituted 2-oxy-quinoline-3-carboxamides as KCNQ2/3 modulators - The invention relates to substituted 2-oxy-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 03-20-2014 |
20140088140 | COMBINATION OF LAQUINIMOD AND PRIDOPIDINE FOR TREATING NEURODEGENERATIVE DISORDERS, IN PARTICULAR HUNTINGTON'S DISEASE - This invention provides a method of treating a patient afflicted with a neurodegenerative disorder, e.g., Huntington's disease (HD), comprising administering to the patient laquinimod as an add-on therapy to or in combination with pridopidine. This invention also provides a package and a pharmaceutical composition comprising laquinimod and pridopidine for treating a patient afflicted with a neurodegenerative disorder, e.g., HD. This invention also provides laquinimod for use as an add-on therapy or in combination with pridopidine in treating a patient afflicted with a neurodegenerative disorder, e.g., HD. This invention further provides use of laquinimod and pridopidine in the preparation of a combination for treating a patient afflicted with a neurodegenerative disorder, e.g., HD. | 03-27-2014 |
20140088141 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 03-27-2014 |
20140088142 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - This invention relates to a compound of Formula I: | 03-27-2014 |
20140107154 | LAQUINIMOD FOR REDUCING THALAMIC DAMAGE IN MULTIPLE SCLEROSIS - This invention provides methods for inhibiting or reducing thalamic damage in a subject comprising administering to the subject an amount of laquinimod, wherein the subject is a human patient afflicted with a form of multiple sclerosis or presenting a clinically isolated syndrome who has been determined to have thalamic damage at baseline, a subject afflicted with a disease or disorder other than a form of multiple sclerosis or a clinically isolated syndrome, or a subject not afflicted with a form of multiple sclerosis or a presenting clinically isolated syndrome, and laquinimod and laquinimod pharmaceutical compositions for use thereof. This invention also provides methods for inhibiting or reducing tremor or spasticity in a subject afflicted by tremor or spasticity, comprising administering to the subject an amount of laquinimod, and laquinimod and laquinimod pharmaceutical compositions for use thereof. | 04-17-2014 |
20140113933 | Solid Forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-- (trifluoromethyl)-1,4-dihyroquinoline-3-carboxamide - The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith. | 04-24-2014 |
20140121239 | METHOD OF TREATING LUNG ADENOCARCINOMA - This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: | 05-01-2014 |
20140121240 | NOVEL PHARMACEUTICAL COMPOSITION - Provided is a novel pharmaceutical composition (antipruritic agent) that is useful for prophylaxis or treatment of itch in conditions such as dermal pruritus. More specifically, provided is a pharmaceutical composition (antipruritic agent) for treatment of itch comprising as an active ingredient a naphthalene compound of the following formula (I): | 05-01-2014 |
20140121241 | Carbostyril Derivatives Including Cilostazol for Treating Fatty Liver - The invention relates to a medicament for preventing and/or treating fatty liver which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof. | 05-01-2014 |
20140128429 | NEW IMIDAZOLYLKETONE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 05-08-2014 |
20140128430 | AMINE SALTS OF LAQUINIMOD - The subject invention provides a Laquinimod amine salt, which is laquinimod meglumine, laquinimod choline hydroxide, laquinimod L-lysine or laquinimod monoethanolamine. | 05-08-2014 |
20140142137 | HIV INTEGRASE INHIBITORS - Provided herein, inter alia, are novel compounds for the inhibition of HIV integrase. The compounds disclosed herein are useful for methods of treating HIV infection in a subject in need thereof. | 05-22-2014 |
20140142138 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 05-22-2014 |
20140148482 | METHOD FOR SCREENING ANTI-CANCER DRUGS AND METHOD OF CANCER TREATMENT - The present application provides a method for screening compounds for cancer treatment comprising treating cancer cells with a candidate compound for sufficient time for detectable expression of a gene selected from GADD45 family; and detecting the level of expression of the gene as compared to the level of expression in the absence of the candidate compound; wherein an increased level of expression in the presence of the candidate compound as compared to expression in the absence of the candidate compound indicates that the candidate compound acts as an inhibitor of the cancer cells. In some embodiments, the method can be used for screening compounds for treatment of sorafenib-resistant hepatocellular carcinoma. The present application further provides a method for treating hepatocellular carcinoma comprising administering to a subject having hepatocellular carcinoma a therapeutic effective amount of an agonist of GADD45 family. | 05-29-2014 |
20140148483 | Method For Predicting Effectiveness Of Angiogenesis Inhibitor - The purpose of the present invention is to provide a method for predicting the effectiveness of an angiogenesis inhibitor in a subject suffering from a tumor. Provided is a method comprising a step of testing for the presence or absence of an a mutation or loss of expression of B-Raf and PTEN in a sample of tumor tissue from the subject. By using the presence or absence of or a mutation or loss of expression of B-Raf and PTEN as an indicator, this method enables the antitumor effectiveness of the angiogenesis inhibitor to be predicted without administering the angiogenesis inhibitor to the subject. | 05-29-2014 |
20140155431 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 06-05-2014 |
20140163068 | Pharmaceutical Compositions for the Treatment of CFTR Mediated Diseases - Pharmaceutical compositions comprising 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1) in Form I and a solid dispersion comprising substantially amorphous N-(5-hydroxy-2,4-ditert-butyl-phenyl)-4-oxo-1H-quinoline-3-carboxamide (Compound 2), methods of treating, lessening the severity of, or symptomatically treating CFTR mediated diseases, such as cystic fibrosis, methods of manufacturing, methods of administering, and kits thereof are disclosed. | 06-12-2014 |
20140179736 | Method of Treating Cancer and Bone Cancer Pain - This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I. | 06-26-2014 |
20140187577 | BIOMARKERS FOR PREDICTING AND ASSESSING RESPONSIVENESS OF THYROID AND KIDNEY CANCER SUBJECTS TO LENVATINIB COMPOUNDS - Biomarkers are provided that are predictive of a subject's responsiveness to a therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate). The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having cancer (e.g., thyroid cancer, kidney cancer), suspected of having cancer, or at risk of developing cancer. | 07-03-2014 |
20140187578 | Pharmaceutical Topical Compositions - The invention provides pharmaceutical stable semisolid topical compositions comprising between 0.2 to 5% of a des-fluoroquinolone compound, and a suitable carrier to manufacture an ointment or a cream. | 07-03-2014 |
20140200242 | Processes for Preparing Quinoline Compounds and Pharmaceutical Compositions Containing Such Compounds - The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2. | 07-17-2014 |
20140200243 | TREATMENT OF CROHN'S DISEASE WITH LAQUINIMOD - This application provides for a method of treating a subject suffering from Crohn's disease, the method comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This application provides for use of laquinimod in the manufacture of a medicament for treating a subject suffering from Crohn's disease. This application also provides for a pharmaceutical composition comprising laquinimod for use in treating a subject suffering from Crohn's disease. | 07-17-2014 |
20140206720 | DOSAGE UNITS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith. | 07-24-2014 |
20140213612 | PPAR GAMMA AGONISTS FOR TREATMENT OF MULTIPLE SCLEROSIS - Methods of treatment of multiple sclerosis (MS) with PPARγ agonists, and in particular with the compound of formula (I) known as INT131: | 07-31-2014 |
20140213613 | Novel Crystal Form - A novel crystalline form of a compound is disclosed. | 07-31-2014 |
20140221423 | Agents And Methods For Treating Ischemic And Other Diseases - This invention relates to compounds that modulate TRPM7 protein activity and use of the same for treatment or prophylaxis of ischemia, cancer, pain or glaucoma. | 08-07-2014 |
20140221424 | PHARMACEUTICAL COMPOSITIONS FOR USE IN THE TREATMENT OF CYSTIC FIBROSIS - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide and pharmaceutical compositions thereof for the treatment of cystic fibrosis, in patients, including kits and/or products thereof. | 08-07-2014 |
20140221425 | Quinolyl-containing Hydroxamic Acid Compound and Preparation Method Thereof, and Pharmaceutical Composition Containing This Compound and Use Thereof - Provided in the present invention is a quinolyl-containing hydroxamic acid compound as shown in formula (I), at the same time also disclosed is the preparation method of the compound and the use thereof, and a pharmaceutical composition containing the quinolyl-containing hydroxamic acid compound. Such compounds are inhibitors of protein kinases and/or histone deacetylases, and can be used in the treatment of diseases caused by the abnormal activity of protein kinases and/or histone deacetylases, for example, tumors, etc. | 08-07-2014 |
20140235670 | TREATMENT OF PROGRESSIVE FORMS OF MULTIPLE SCLEROSIS WITH LAQUINIMOD - This invention provides a method for treating a human subject afflicted with a progressive form of multiple sclerosis, comprising periodically administering to the human subject an amount of laquinimod effective to treat the human subject. This invention also provides laquinimod for use in treating a human subject afflicted with a progressive form of multiple sclerosis. This invention further provides pharmaceutical compositions and packages comprising an effective amount of laquinimod for treating a progressive form of multiple sclerosis. | 08-21-2014 |
20140256770 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 09-11-2014 |
20140275163 | SOVAPREVIR POLYMORPHS AND METHODS OF MANUFACTURE THEREOF - The disclosure provides crystalline Sovaprevir forms. The crystalline forms of Sovaprevir comprise a Form A polymorph, a Form B polymorph, a Form C polymorph, a Form D polymorph, and a Form E polymorph. The Form A, B, C, D, and E polymorphs exhibit X-ray powder diffraction patterns having peak locations in accordance with FIGS. | 09-18-2014 |
20140303204 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 10-09-2014 |
20140303205 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - This invention relates to a compound of Formula I: | 10-09-2014 |
20140315948 | Pharmaceutical Composition and Administrations Thereof - The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention. | 10-23-2014 |
20140323521 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 10-30-2014 |
20140323522 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and bone metastases, with a dual inhibitor of MET and VEGF. | 10-30-2014 |
20140329855 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 11-06-2014 |
20140336219 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 11-13-2014 |
20140336220 | COMPOSITION FOR PREVENTING OR TREATING OBESITY COMPRISING REBAMIPIDE - The present disclosure relates to a composition and a health functional food for preventing or treating obesity comprising a rebamipide compound or its pharmaceutically acceptable salt as an active component. It is confirmed that when a rebamipide compound of the present disclosure is administered to a mouse model induced with obesity, it shows excellent effects of reducing weight, reducing adipocyte, and reducing a total cholesterol content in the body, as compared with a non-administered control group, and also, it shows an excellent effect of suppressing differentiation of cytotoxic Th17 cells that generate and secrets inflammatory cytokine and an excellent effect of improving activity of regulatory T cells (Treg) capable of suppressing a function of abnormally activated immune cells and controlling an inflammatory reaction. Thus, the rebamipide compound can be used for producing a medicine and a functional food which can effectively treat obesity caused by abnormality of immune modulation. | 11-13-2014 |
20140343096 | DEUTERATED N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQ- UINOLINE-3-CARBOXAMIDE, SALTS AND USES THEREOF - The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses. | 11-20-2014 |
20140343097 | 5-(2-1-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2(1H)-ONE FOR THE TREATMENT OF LUNG FUNCTION - A compound which is a hydroxyquinolinone derivative of formula (I), | 11-20-2014 |
20140343098 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 11-20-2014 |
20140350047 | ISOFORM-SELECTIVE INHIBITORS AND ACTIVATORS OF PDE3 CYCLIC NUCLEOTIDE PHOSPHODIESTERASES - The present invention concerns methods and compositions related to type 3 phosphodiesterases (PDE3). Certain embodiments concern isolated peptides corresponding to various PDE3A isoforms and/or site-specific mutants of PDE3A isoforms, along with expression vectors encoding such isoforms or mutants. In specific embodiments, methods for identifying isoform-selective inhibitors or activators of PDE3 are provided, along with methods of use of such inhibitors or activators in the treatment of dilated cardiomyopathy, pulmonary hypertension and/or other medical conditions related to PDE3 effects on cAMP levels in different intracellular compartments. | 11-27-2014 |
20150018387 | HIGH CONCENTRATION LOCAL ANESTHETIC FORMULATIONS - A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit neuropathic pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours. | 01-15-2015 |
20150025108 | 8-HYDROXY QUINOLINE DERIVATIVES - The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula | 01-22-2015 |
20150031722 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-29-2015 |
20150051244 | ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): | 02-19-2015 |
20150057310 | Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer - Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. | 02-26-2015 |
20150057311 | Heterocyclic GSK-3 Allosteric Modulators - The present invention relates to heterocyclic substituted quinoline derivatives as allosteric inhibitors of the glycogen synthase kinase-3 (GSK-3) enzyme. Therefore, these compounds are useful for the manufacturing of a medicament designed for the treatment and/or prevention of diseases wherein GSK-3 is involved, such as neurodegenerative diseases, inflammatory diseases, cancer, diabetes, and to promote various regenerative processes. | 02-26-2015 |
20150065539 | Methods for Increasing CFTR Activity - The present disclosure provides compounds effective in increasing mucociliary clearance in a subject. In one embodiment, the compounds are of the general formula I. The present disclosure further shows that such compounds are effective in increasing activation of the CFTR, thereby increasing mucociliary clearance in the subject. The present disclosure further shows that such compounds are effective in increasing the depth of ASL, thereby increasing mucociliary clearance in the subject. In one embodiment of each of the foregoing, the subject is free from congenital or genetic defect in the cellular mucociliary clearance apparatus and/or acquired abnormality in the cellular mucociliary clearance apparatus. | 03-05-2015 |
20150073015 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 03-12-2015 |
20150073016 | ROR MODULATORS AND THEIR USES - The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR. | 03-12-2015 |
20150080430 | USE OF JASMONATE ESTER DERIVATIVES FOR TREATING BENIGN HYPERPROLIFERATIVE SKIN DISORDERS - The present invention relates to methods of treating benign hyperproliferative diseases of the epidermis by administering a composition comprising at least one jasmonate ester derivative. In particular, the present invention provides jasmonate ester derivatives as potent compounds useful for the treatment of disorders such as actinic keratoses with reduced side effects. | 03-19-2015 |
20150080431 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CFTR-MEDIATED DISORDERS - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), solids forms, and pharmaceutical compositions thereof for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to the use of Compound 1 in combination with 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 2), and Compound 1 in combination with (S)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 3), for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to solid forms and formulations of Compound 2 or Compound 3 in combination with Compound 1, and pharmaceutical compositions thereof, for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 03-19-2015 |
20150094331 | QUINOLONE INHIBITORS OF LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 - The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof. | 04-02-2015 |
20150094332 | Laquinimod Combination Therapy For Treatment Of Multiple Sclerosis - The subject invention provides a method for treating a subject afflicted with a form of multiple sclerosis (MS) or presenting a clinically isolated syndrome (CIS) comprising periodically administering to the subject an amount of laquinimod and an amount of a compound of formula (I): | 04-02-2015 |
20150099779 | ROR MODULATORS AND THEIR USES - The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR. | 04-09-2015 |
20150099780 | DEUTERATED CFTR POTENTIATORS - This invention relates to compounds of Formula I: | 04-09-2015 |
20150099781 | Compounds and Methods for Treating Mammalian Gastrointestinal Microbial Infections - Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants. | 04-09-2015 |
20150119420 | Treatment of Multiple Sclerosis With Combination of Laquinimod and Dimethyl Fumarate - This invention provides a method of treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome comprising administering to the subject laquinimod as an add-on therapy to or in combination with DMF. This invention also provides a package comprising laquinimod and DMF for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention also provides laquinimod for use as an add-on therapy or in combination with DMF in treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention also provides a pharmaceutical composition comprising laquinimod and DMF for use in treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention further provides use of laquinimod and DMF in the preparation of a combination for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. | 04-30-2015 |
20150133493 | COUMARIN-BASED COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND CANCER - Compounds including those of the Formula I | 05-14-2015 |
20150133494 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF. | 05-14-2015 |
20150141457 | ELVITEGRAVIR SOLID DISPERSION - The present invention provides a novel amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In a preferred embodiment the process for the preparation of amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier comprises: preparing a solution comprising a mixture of elvitegravir and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol, span 20 or soluplus in a solvent; and removing the solvent from the solution obtained; adding hydrocarbon solvent to the residual solid; and isolating amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier. | 05-21-2015 |
20150141458 | Treatment of Glaucoma Using Laquinimod - The subject invention provides a method of treating a subject afflicted with glaucoma, suffering from retinal ganglion cell (RGC) loss or damage, or elevated intraocular pressure (IOP), or of reducing RGC loss or damage, or reducing IOP in a subject, comprising administering to the subject an amount of laquinimod effective to treat the subject, to reduce RGC loss or damage, or to reduce IOP in the subject. Provide also is a pharmaceutical composition, a package and a therapeutic package for treating a subject afflicted with glaucoma. | 05-21-2015 |
20150141459 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 05-21-2015 |
20150291531 | THERAPEUTIC HYDROXYQUINOLONES - The invention provides compounds of formula (I) and salts thereof wherein R | 10-15-2015 |
20150306088 | LAQUINIMOD FOR THE TREATMENT OF RELAPSING-REMITTING MULTIPLE SCLEROSIS (RRMS) PATIENTS WITH A HIGH DISABILITY STATUS - This invention provides a method for treating or for reducing ambulatory deterioration in a human patient diagnosed to be afflicted with relapsing-remitting multiple sclerosis (RRMS) and having a high baseline disability score according to the Kurtzke Expanded Disability Status Scale (EDSS), comprising periodically administering to only the patient diagnosed with RRMS and having a high baseline disability score an amount of laquinimod effective to treat the patient or to reduce ambulatory deterioration. This invention further provides pharmaceutical compositions and packages comprising an effective amount of laquinimod for treating a human patient diagnosed to be afflicted with RRMS and having a high baseline disability score according to the EDSS. | 10-29-2015 |
20150315151 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 11-05-2015 |
20150315152 | Pharmaceutical Compositions for the Treatment of CFTR-Mediated Disorders - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), solids forms, and pharmaceutical compositions thereof for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to the use of Compound 1 in combination with 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 2), and Compound 1 in combination with (S)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 3), for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to solid forms and formulations of Compound 2 or Compound 3 in combination with Compound 1, and pharmaceutical compositions thereof, for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 11-05-2015 |
20150328187 | USE OF PDE4 INHIBITORS AND COMBINATIONS THEREOF FOR THE TREATMENT OF CYSTIC FIBROSIS - Methods of treating cystic fibrosis by administering a PDE4 inhibitor in combination with one or more cystic fibrosis transmembrane conductance regulator (CFTR) potentiators, including ivacaftor, and/or one or more CFTR correctors, including lumacaftor. Pharmaceutical compositions, dosage forms, and kits suitable for use in methods of the invention are also disclosed. | 11-19-2015 |
20150336876 | PHENOXYALKYLAMINE COMPOUND - The invention provides a compound having a selective inhibitory activity against highly-expressed LAT-1 in tumor cell. The compound is represented by the formula (I): | 11-26-2015 |
20150344466 | METHOD FOR CONTROLLING ARTHROPOD PEST - An amide compound represented by formula (I): | 12-03-2015 |
20150351384 | AQUEOUS SUSPENDED AGRICULTURAL CHEMICAL COMPOSITION - The present invention provides an aqueous suspended agricultural chemical composition comprising an agricultural chemical active ingredient, an alkyl naphthalene sulfonate formalin condensate and one or two or more compounds selected from the group consisting of an alkyl sulfate, a polyoxyalkylene alkyl ether sulfate, an alkyl phosphoric acid and a salt thereof, a polyoxyalkylene alkyl ether phosphoric acid and a salt thereof, and a polyoxyalkylene alkyl ether acetic acid and a salt thereof. The aqueous suspended agricultural chemical composition suppresses the crystal growth of the agricultural chemical active ingredient, and has an excellent effect on pest control and an excellent storage stability. | 12-10-2015 |
20150359891 | NON-ADDICTIVE ANALGESIC SUSTAINED-RELEASE DRUG DELIVERY SYSTEM AND PREPARATION METHOD THEREOF - A non-addictive analgesic sustained-release drug delivery system, comprising: (1) a narcotic analgesic drug having a concentration of 1 mg/ml-160 mg/ml, the drug being selected from a group consisting of: a local analgesic drug, and the combination of the local analgesic drug and a nonsteroidal analgesic drug and/or an opioid analgesic drug; (2) a drug menstruum in a proportion of 1%-75% (v/v), the menstruum being selected from a group consisting of benzyl alcohol, ethanol, benzyl benzoate, ethyl lactate, and tetrahydrofurfuryl polyethylene glycol ether; and (3) a drug sustained-release formulation having a proportion of 25%-99% (v/v), the sustained-release formulation being selected from a group consisting of natural vegetable oil, synthetic lipid, artificially improved half-natural lipid and derivative thereof. Also disclosed are a preparation process and use of the sustained-release drug delivery system. | 12-17-2015 |
20150366859 | SOLID DISPERSION COMPRISING AMORPHOUS CILOSTAZOL - The present invention relates to a solid dispersion comprising cilostazol, and methacrylic acid copolymer S and/or methacrylic acid copolymer L, which is characterized in that cilostazol is retained in an amorphous state in a gastrointestinal tract for a certain period after oral administration. | 12-24-2015 |
20160008348 | PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR MILD COGNITIVE IMPAIRMENT | 01-14-2016 |
20160016909 | PROCESS FOR THE PREPARATION OF IVACAFTOR AND ITS INTERMEDIATES - The present invention provides novel intermediates of ivacaftor and process for its preparation. The present invention also provides process for the preparation of ivacaftor and pharmaceutically acceptable salt thereof using novel intermediates. | 01-21-2016 |
20160022664 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 01-28-2016 |
20160022665 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 01-28-2016 |
20160024065 | COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING CYSTIC FIBROSIS, CHRONIC OBSTRUCTIVE PULMONARY DISEASE, AND MISFOLDED PROTEIN DISORDERS - Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis and chronic obstructive pulmonary diseases). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided. | 01-28-2016 |
20160024105 | ALDOSTERONE SYNTHASE INHIBITORS - The present invention relates to compounds of formula I: | 01-28-2016 |
20160030338 | Pharmaceutical Topical Compositions - The invention provides pharmaceutical stable semisolid topical compositions comprising between 0.2 to 5% of a des-fluoroquinolone compound, and a suitable carrier to manufacture an ointment or a cream. | 02-04-2016 |
20160031818 | Metabolites of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide - The invention relates to metabolites of cabozantinib (I) as well as uses thereof. | 02-04-2016 |
20160031854 | ACTIVATION OR REACTIVATION OF ACHE - Disclosed herein is an in vitro or in vivo method of activating or reversing inactivation of acetylcholinesterase (AChE) or butyrylcholinesterase (BuchE) using compounds of the present disclosure. Also disclosed is a method of treating a subject exposed to a nerve agent using such compounds. Also disclosed is a method of treating organophosphate poisoning in a subject using such compounds. Also disclosed is a method of modulating neuronal signaling and transmission in a subject using such compounds. | 02-04-2016 |
20160038475 | COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING HYPERPROLIFERATIVE DISEASES - Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell. | 02-11-2016 |
20160039764 | DEUTERATED CFTR POTENTIATORS - This invention relates to compounds of Formula I: | 02-11-2016 |
20160045490 | USE OF CHEMOTHERAPEUTIC AGENTS - The use of chemotherapeutic agents for the preparation of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals. | 02-18-2016 |
20160051532 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1. | 02-25-2016 |
20160067185 | SOLID PHARMACEUTICAL COMPOSITION - [Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less. | 03-10-2016 |
20160067239 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 03-10-2016 |
20160068502 | FLAVONOID IL-17A INHIBITORS - The present invention describes compounds according to formula I: | 03-10-2016 |
20160074330 | SOLID PHARMACEUTICAL COMPOSITION - [Problem] To provide a novel pharmaceutical composition which contains a medically active component and which can suppress delays in the release of said component due to gelling. | 03-17-2016 |
20160074380 | Treatment Of Neurodegenerative Diseases With Combination Of Laquinimod And Fingolimod - This invention provides a method of treating a subject afflicted with a neurodegenerative disease comprising periodic administration of an amount of laquinimod and an amount of fingolimod, wherein the amounts when taken together are effective to treat the subject. Also provided are packages and pharmaceutical compositions comprising laquinimod and fingolimod for treating a subject afflicted with a neurodegenerative disease. Also provided is a pharmaceutical composition comprising laquinimod for use as an add-on therapy or in combination with fingolimod, and a pharmaceutical composition comprising fingolimod for use as an add-on therapy or in combination with laquinimod, for treating said subject. | 03-17-2016 |
20160075685 | Novel Crystal Form - A novel crystalline form of a compound is disclosed. | 03-17-2016 |
20160083367 | PYRIDINYL QUINOLINONE DERIVATIVES AS MUTANT-ISOCITRATE DEHYDROGENASE INHIBITORS - The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: | 03-24-2016 |
20160089365 | IMMUNOSTIMULATORY COMPOUND - An immunostimulatory compound is disclosed. | 03-31-2016 |
20160089366 | BIOMARKERS FOR PREDICTING AND ASSESSING RESPONSIVENESS OF ENDOMETRIAL CANCER SUBJECTS TO LENVATINIB COMPOUNDS - Biomarkers are provided that predict whether a subject having endometrial cancer will or will not respond to a therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate). The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for and treating a subject having, suspected of having, or at risk of developing an endometrial cancer. | 03-31-2016 |
20160096807 | CO-CRYSTALS OF MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present disclosure relates to co-crystals comprising N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and a co-former and methods for their preparation. The present disclosure further relates to pharmaceutical compositions comprising the co-crystal forms, as well as methods of treatment therewith and kits. | 04-07-2016 |
20160101097 | Combinations of Glycopyrrolate and Beta2 Adrenoceptor Agonists - A medicament comprising, separately or together (A) glycopyrrolate; and | 04-14-2016 |
20160101223 | Catheter Locking Solution Having Antimicrobial and Anticoagulation Properties - The present invention includes a catheter locking solution having both antimicrobial and anticoagulant properties including a local anesthetic and a viscosifying agent. The local anesthetic of the present invention may be an amino amide; an amino ester; an aminoacylanilide; an aminoalkyl benzoate; an amino carbonate; an N-phenylamidine compound; an N-aminoalkyl amid; an aminoketone, or combinations and mixtures thereof. In a particular embodiment of the present invention, the local anesthetic is tetracaine or dibucaine. | 04-14-2016 |
20160113918 | Heterocyclic GSK-3 Allosteric Modulators - The present invention relates to heterocyclic substituted quinoline derivatives as allosteric inhibitors of the glycogen synthase kinase-3 (GSK-3) enzyme. Therefore, these compounds are useful for the manufacturing of a medicament designed for the treatment and/or prevention of diseases wherein GSK-3 is involved, such as neurodegenerative diseases, inflammatory diseases, cancer, diabetes, and to promote various regenerative processes. | 04-28-2016 |
20160130231 | ROR MODULATORS AND THEIR USES - The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR. | 05-12-2016 |
20160143880 | Use of Glycopyrrolate for Treating Tachycardia - The invention relates to a novel use of the antimuscarinic agent glycopyrrolate, for example the salt glycopyrronium bromide. In particular, the invention relates to glycopyrrolate for use as a heart rate lowering agent and more particularly, but not exclusively, for use in patients suffering from respiratory conditions such as chronic obstructive pulmonary disease. | 05-26-2016 |
20160143898 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 05-26-2016 |
20160165888 | PEST CONTROL COMPOSITION INCLUDING NOVEL IMINOPYRIDINE DERIVATIVE | 06-16-2016 |
20160185767 | SOLID ORAL DOSAGE FORMULATION OF HCV INHIBITOR IN THE AMORPHOUS STATE - Described herein are solid oral dosage forms containing Compound (1) or a pharmaceutically acceptable salt thereof (Formula 1), wherein Compound (1) is in the amorphous state. Also described are solid oral dosage forms comprising a composition of Compound (1) in the amorphous state and one or more pharmaceutically acceptable excipients. Compound (1) is a specific inhibitor of the hepatitis C virus (HCV) NS3/4A serine protease. Thus, also described herein are methods for using the described solid oral dosage forms in the treatment of HCV infection. Also described are processes for the manufacture of the solid oral dosage forms. | 06-30-2016 |
20160200684 | Pharmaceutical Compositions for the Treatment of CFTR-Mediated Disorders | 07-14-2016 |
20160201132 | GENE EXPRESSION BIOMARKERS OF LAQUINIMOD RESPONSIVENESS | 07-14-2016 |
20160251345 | Amorphous Salt of a Macrocyclic Inhibitor of HCV | 09-01-2016 |
20160376239 | N-Acylalkyl Prodrugs of Multi-Tyrosine Kinase Inhibitors and Methods of Use - The present invention is directed to N-acylalkyl prodrugs of nitrogen-containing multi-tyrosine kinase inhibitors. The present invention is further directed to compositions comprising compounds of the invention. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention. | 12-29-2016 |
20160376255 | QUINOLONE INHIBITORS OF LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 - The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof | 12-29-2016 |
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