| Entries |
| Document | Title | Date |
|---|
| 20120010241 | HSP90 INHIBITING INDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF - The invention relates to novel products having formula (I), wherein: R4 represents H, CH3, CH2CH3, CF3, F, Cl, Br, I; Het represents a heterocycle optionally substituted by one or more R1 or R′1 radicals selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalkoxy, alkylthio, carboxy that is free or sterified with an alkyl radical, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, S(O2)-N(alkyl)2, all of the alkyl, alkoxy and alkylthio radicals being optionally substituted; R being selected from the group comprising (A′), (B), (C), (D) and (F), wherein W1, W2, W3 represent independently CH or N, X represents O, S, NR2, C(O), S(O) or S(O)2; V represents H, Hal, —O—R2 or —NH—R2 with R2 representing H, alkyl, cycloalkyl or heterocycloalkyl, optionally substituted; said products being in all isomer forms, as well as the salts and intended for use as drugs. | 01-12-2012 |
| 20100120854 | TGF-BETA INHIBITORS - The present invention provides crystalline 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole monohydrate. | 05-13-2010 |
| 20110207773 | NOVEL PHENYL-QUINOLINE-CARBOXYLIC ACID PYRIDINE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel phenyl-quinoline-carboxylic acid pyridine derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 08-25-2011 |
| 20100016354 | NOVEL OXADIAZOLE DERIVATIVES AND THIADIAZOLE DERIVATIVES HAVING NEOVASCULARIZATION INHIBITORY ACTIVITY - The present invention relates to Compounds represented by the formula (I) or salts thereof. In the formula (I), the ring A represents a benzene ring, a thiophene ring, or a pyridine ring; R | 01-21-2010 |
| 20090253740 | SUBSTITUTED N-BICYCLICALKYL BICYCLICCARBOXYAMIDE COMPOUNDS - This invention provides a compound of the formula (I): And their use for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound. | 10-08-2009 |
| 20110124683 | Use of CRTH2 Antagonist Compounds - The invention relates to compounds of general formula (I): | 05-26-2011 |
| 20090306133 | New Acetyl Coenzyme A Carboxylase (ACC) Inhibitors And Uses In Treatments Of Obesity And Diabetes Mellitus - 087 - The present invention relates to Acetyl Coenzyme A Carboxylase (ACC) inhibitors according to formula (I), | 12-10-2009 |
| 20150148377 | Quinoline Derivatives - The invention relates to quinoline compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, W, U, Q, R | 05-28-2015 |
| 20100056571 | NOVEL PYRAZOLE COMPOUNDS AS TRANSFORMING GROWTH FACTOR (TGF) INHIBITORS - Novel pyrazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)- | 03-04-2010 |
| 20110053977 | SMALL MOLECULE E2F INHIBITOR - A small molecular inhibitor of E2F (HLM006474) was identified using a computer-based virtual screen and the known crystal structure of the DNA bound E2F4/DP2 heterodimer. Treatment of multiple cell lines resulted in the loss of intracellular E2F4 DNA-binding activity. Overnight exposure to HLM006474 resulted in down regulation of total E2F4 protein as well as several known E2F targets. The effects of treatment on different cell lines included a reduction in cell proliferation and an increase in apoptosis. Apoptosis was induced in a manner distinct from cisplatin and doxorubicin. E2F4-null MEFs were less sensitive than wildtype counterparts to the apoptosis-inducing activity of the compound revealing its biological specificity. A375 cells were extremely sensitive to the apoptosis-inducing activity of the compound in two-dimensional culture and HLM006474 was a potent inhibitor of melanocytes proliferation and subsequent invasion in a three-dimensional tissue culture model system. | 03-03-2011 |
| 20110224255 | TRIPEPTIDYL PEPTIDASE INHIBITORS - The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. | 09-15-2011 |
| 20130203809 | PHARMACEUTICAL COMPOSITIONS COMPRISING 7-(1H-IMIDAZOL-4-YLMETHYL)-5,6,7,8-TETRAHYDRO-QUINOLINE FOR TREATING SKIN DISEASES AND CONDITIONS - The present invention relates to a method for treating skin diseases and skin conditions in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1H-Imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, or its individual enantiomers or the tautomers thereof, or a pharmaceutically acceptable salt thereof. | 08-08-2013 |
| 20090286829 | QUINOLYNYLMETHYLIMIDIZOLES AS THERAPEUTIC AGENTS - Disclosed herein are methods for treating a disorder associated with selective subtype modulation of alpha 2B and alpha 2C adrenergic receptors. Such methods can be performed, for example, by administering to a subject in need thereof a pharmaceutical composition containing a therapeutically effective amount of at least one compound having the structure: | 11-19-2009 |
| 20120015978 | THERAPEUTIC AGENTS FOR OCULAR HYPERTENSION - This invention provides well defined 6-alkyl or hydroxyalkyl- | 01-19-2012 |
| 20100168164 | Antidiabetic Oxazolidinediones and Thiazolidinediones - Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes. | 07-01-2010 |
| 20110039888 | ASYMMETRIC ALPHA FUNCTIONALIZATION AND ALPHA, ALPHA BISFUNCTIONALIZATION OF ALDEHYDES AND KETONES - The present invention relates, generally, to asymmetric α-functionalization and to asymmetric α,α-bisfunctionalization of ketones and aldehydes and, in particular, to chiral auxiliaries suitable for use in effecting such functionalizations and to methods of using same. | 02-17-2011 |
| 20100113516 | QUINOLYNYLMETHYLIMIDIZOLES AS THERAPEUTIC AGENTS - Disclosed herein is a compound of the formula (I):(I). Therapeutic methods, compositions and medicaments related thereto are also disclosed. | 05-06-2010 |
| 20100267769 | Substituted Bicyclocarboxyamide Compounds - This invention provides a compound of the formula | 10-21-2010 |
| 20110021563 | INSULIN-REGULATED AMINOPEPTIDASE (IRAP) INHIBITORS AND USES THEREOF - The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions. | 01-27-2011 |
| 20110112142 | NOVEL ESTROGEN RECEPTOR LIGANDS - The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R | 05-12-2011 |
| 20090253741 | ALKENE PIPERIDINE DERIVATIVES AS ANTIVIRAL AGENTS - This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS. | 10-08-2009 |
| 20130096159 | INHIBITORS OF HUMAN 12-LIPOXYGENASE - Disclosed are inhibitors of human 12-lipoxygenase of Formula (I) or (II), wherein R | 04-18-2013 |
| 20100160373 | DIHYDROPYRIDONE AMIDES AS P2X7 MODULATORS - Compounds of the formula I: | 06-24-2010 |
| 20110039889 | COMPOUNDS - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 02-17-2011 |
| 20100041700 | Substituted 1-(Azolin-2-yl)-Amino-1,2-Heterocyclyl-Ethane Compounds For Combating Pests - The present invention relates to 1-(Azolin-2-yl)-amino-1,2-heterocyclyl-ethane compounds, which are useful for combating insects, arachnids and nematodes. The present invention also relates to methods for combating animal pests and to compositions for combating animal pests. It has been found that animal pests can be combated by 1-(Azolin-2-yl)-amino-1,2-heterocyclyl-ethane compounds of the general formula (I): wherein A is a radical of the formulae A | 02-18-2010 |
| 20140073668 | N-QUINOLIN-BENZENSULFONAMIDES AND RELATED COMPOUNDS FOR THE TREATMENT OF CANCER, AUTOIMMUNE DISORDERS AND INFLAMMATION - The present invention relates to the NQBS class of molecules. It is based, at least in part, on the discovery that a representative group of compounds have been observed to inhibit nuclear translocation of NF-κB subunits. Without being bound by any particular theory, this inhibition of nuclear translocation may be mediated by either (i) binding of the NQBS or related compound to the C-terminus of the RHD, which specifically mediates the nuclear internalization; or (ii) NQBS-mediated stabilization of the dimer/IκB complex, disallowing dissociation of the active NF-κB monomers, and thus, inhibiting the generation of the subunits necessary to enter the nucleus. The NQBS class of molecules, and related molecules, may be used in therapeutic applications where inhibition of NF-κB translocation is beneficial, including but not limited to the treatment of cancer, autoimmune disorders, and inflammatory states. | 03-13-2014 |
| 20110060007 | Novel NIP Thiazole Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydroge-Nase-1 - The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions. | 03-10-2011 |
| 20140011840 | Compounds of Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 01-09-2014 |
| 20140073669 | 4'-O-SUBSTITUTED ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 03-13-2014 |
| 20110224253 | SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR - The present invention provides tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof. The present invention provides a method of using tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof. | 09-15-2011 |
| 20160115131 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 04-28-2016 |
| 20110105559 | Compositions and Methods for Treating, Controlling, Reducing, Ameliorating, or Preventing Allergy - A composition for treating, controlling, reducing, ameliorating, or preventing allergy comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an anti-allergic medicament and/or an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. The anti-allergic medicament can comprise an antihistamine, a mast-cell stabilizer, a leukotriene inhibitor, an immunomodulator, an anti-IgE agent, or a combination thereof. | 05-05-2011 |
| 20120029016 | Indoles Useful in the Treatment of Inflammation - There is provided compounds of formula I, wherein ring R | 02-02-2012 |
| 20110060006 | Functionally Selective Alpha2C Adrenoreceptor Agonists - In its many embodiments, the present invention provides a novel class of heterocyclic derivatives as a2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions. | 03-10-2011 |
| 20100249185 | METHOD FOR INHIBITING TOPOISOMERASE II - The present invention relates to compounds that inhibit the activity of Hsp90 and inhibit topoisomerase II. | 09-30-2010 |
| 20130217726 | INSULIN-REGULATED AMINOPEPTIDASE (IRAP) INHIBITORS AND USES THEREOF - The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions. | 08-22-2013 |
| 20100222382 | Esters of Compounds in the Leptomycin Family - Esters of compounds in the leptomycin family, having a structure according to formula I | 09-02-2010 |
| 20100234423 | TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE - The present invention relates to compound 1, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising Compound 1 and methods of using the compositions in the treatment of proliferative disorders. | 09-16-2010 |
| 20140031391 | Novel 5-aminotetrahydroquinoline-2-carboxylic acids and their use - The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders. | 01-30-2014 |
| 20100210685 | Novel Substituted Indoles | 08-19-2010 |
| 20100298376 | USE OF NOVEL NEUROPROTECTIVE 3-SUBSTITUTED INDOLONE COMPOSITIONS - The present invention provides compositions and methods of synthesizing optionally substituted 3-substituted indolin-2-ones and methods to employ the resultant compounds to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke. | 11-25-2010 |
| 20110224254 | NOVEL INHIBITORS - Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water. | 09-15-2011 |
| 20090281142 | THIAZOLE DERIVATIVE - [Problem] To provide a compound which is useful as a GK activator. | 11-12-2009 |
| 20100305156 | INHIBITORS OF C-MET PROTEIN KINASE - The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 12-02-2010 |
| 20110251237 | 2,5-Disubstituted Piperidine Orexin Receptor Antagonists - The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 10-13-2011 |
| 20100197730 | METHODS FOR TREATING ANXIETY - Disclosed are methods of treating anxiety by administering to a patient in need of such treatment a compound having the following formula (I). | 08-05-2010 |
| 20100197729 | THERAPEUTIC ((PHENYL)IMIDAZOLYL)METHYLQUINOLINYL COMPOUNDS - Disclosed herein is a compound of the formula (I) therapeutic methods, compositions, and medicaments related thereto are also disclosed. | 08-05-2010 |
| 20110212995 | COMPOSITIONS AND METHODS FOR TREATING SPASTICITY - Disclosed are methods of treating spasticity by administering to a patient in need of such treatment a compound having the following formula: | 09-01-2011 |
| 20110212994 | Small Molecule Choline Kinase Inhibitors, Screening Assays, and Methods for Safe and Effective Treatment of Neoplastic Disorders - Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided. | 09-01-2011 |
| 20100305155 | SUBSTITUTED PYRAZOLE INHIBITORS OF C-MET PROTEIN KINASE - The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 12-02-2010 |
| 20150038532 | Pharmaceutical Composition Of A Potent HCV Inhibitor For Oral Administration - A pharmaceutical composition of the following Compound (1), a potent hepatitis C viral (HCV) inhibitor, or a pharmaceutically acceptable salt thereof, for oral administration. | 02-05-2015 |
| 20110015225 | Heterocyclic compound - The present invention provides to a compound having melanin-concentrating hormone receptor antagonistic action and low toxicity, and useful as a agent for the prophylaxis or treatment of obesity and the like. | 01-20-2011 |
| 20150329524 | FATTY ACID SYNTHASE INHIBITORS - This invention relates to triazolones and triazolones for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer. | 11-19-2015 |
| 20130331413 | DEFENSIN-LIKE MOLECULES AS NOVEL ANTIMICROBIAL AGENTS - Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal. | 12-12-2013 |
| 20120316199 | COMPOSITIONS AND METHODS FOR TREATING, CONTROLLING, REDUCING, OR AMELIORATING INFLAMMATORY PAIN - A composition for treating, controlling, reducing, or ameliorating inflammatory pain comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. It may be used in a method of managing post-surgical ocular pain such that it has lower risk of eliciting adverse side effects seen with other therapeutic agents. | 12-13-2012 |
| 20160037773 | DIINDOL-3-YLMETHANES AS POTENT NON-TOXIC ANTIFOULING COMPOUNDS - The present invention provides high potency 3,3′-diindolylmethane (DIM) and analogue compounds as antifouling agents. The present invention further provides methods of preventing or reducing settlement and/or fouling of marine fouling organisms on surfaces of submerged objects by coating the surfaces with the 3,3′-diindolylmethane (DIM) and analogue compounds provided. | 02-11-2016 |
| 20100190823 | Therapeutic ((Bicylicheteroaryl)Imidazolyl) Methylheteroaryl Compounds - Disclosed herein is a compound of the formula (I) therapeutic methods, compositions, and medicaments related thereto are also disclosed. | 07-29-2010 |
| 20140194465 | COMPOSITIONS FOR TREATMENT OF CANCER - Compounds that are specifically toxic to cancer stem cells are disclosed. | 07-10-2014 |
| 20130072523 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R1, R | 03-21-2013 |
| 20120108634 | 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. | 05-03-2012 |
| 20140275165 | COMPOUNDS THAT INHIBIT NFkB AND BACE1 ACTIVITY - The present invention relates to compounds with activity as BACE1 and NFκB modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds. | 09-18-2014 |
| 20140296287 | METHODS FOR TREATING COGNITIVE DISORDERS USING 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS - Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 | 10-02-2014 |
| 20110224252 | NOVEL IMIDAZOLE DERIVATIVES - The present invention relates to novel imidazole derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R | 09-15-2011 |
| 20110046178 | Thiazolylpiperidine Derivatives as Fungicides - Thiazolylpiperidine derivatives of the formula (I), | 02-24-2011 |
| 20090326009 | Novel 1-2-Dihydroquinoline Derivative Having Glucocorticoid Receptor Binding Activity - An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; R | 12-31-2009 |
| 20140315949 | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF - Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein. | 10-23-2014 |
| 20120309787 | INSULIN-REGULATED AMINOPEPTIDASE (IRAP) INHIBITORS AND USES THEREOF - The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions. | 12-06-2012 |
| 20100120855 | MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I), the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by | 05-13-2010 |
| 20110124684 | AMINOPYRAZOLE TRIAZOLOTHIADIAZOLE INHIBITORS OF C-MET PROTIEN KINASE - The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 05-26-2011 |
| 20100041699 | MICROCRYSTALLINE (5-FLUORO-2-METHYL-3-QUINOLIN-2-YLMETHYL-INDOL-1-YL) ACETIC ACID - The invention relates to a microcrystalline form of a compound which is an inhibitor of PGD | 02-18-2010 |
| 20120214842 | METHODS FOR TREATING DISEASES OF THE RETINA - Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of Formula I | 08-23-2012 |
| 20110152318 | NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME - This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on. | 06-23-2011 |
| 20130012538 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example. | 01-10-2013 |
| 20100216837 | GLYCINE TRANSPORT INHIBITORS - The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof. | 08-26-2010 |
| 20140213614 | Imaging Beta-Amyloid Peptides and Inhibition of Beta-Amyloid Peptide Aggregation - The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro by using carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using carbazole-based fluorophores. | 07-31-2014 |
| 20130197029 | CHEMICAL COMPOUNDS - The use of a compound of formula I | 08-01-2013 |
| 20100056569 | Heterocyclic Non-Nucleoside Compounds, Their Preparation, Pharmaceutical Composition And Their Use As Antiviral Agents - The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on. | 03-04-2010 |
| 20120322823 | HETEROCYCLIC SULFONAMIDES, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: | 12-20-2012 |
| 20140187579 | TIP60 INHIBITORS - This invention is in the fields of immunology and autoimmunity. More particularly it concerns pharmaceutical compositions comprising compounds which are useful agents for inhibiting the functions of TIP60 and the use of such compounds in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases. | 07-03-2014 |
| 20140128431 | PHARMACEUTICAL COMPOSITION WITH IMPROVED BIOAVAILABILITY, SAFETY AND TOLERABILITY - The invention relates to solid dispersions of poorly soluble compounds formed by coprecipitation, resulting in improved bioavailability, safety and tolerability. The invention also relates to Purified Eudragit L100-55 used to prepare such solid dispersions. | 05-08-2014 |
| 20100160374 | N-(2-Hydroxyethyl)-N-Methyl-4-(Quinolin-8-yl(1-(Thiazol-4-ylmethyl)Piperid- in-4-ylidene)Methyl)Benzamide - N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, pharmaceutically acceptable salts thereof, and/or mixtures thereof, as well as, pharmaceutical compositions thereof, methods of treatment therewith, and processes of making N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide and intermediates thereof. | 06-24-2010 |
| 20100120857 | USE OF TRIS-QUATERNARY AMMONIUM SALTS AS PAIN MODULATING AGENTS - Provided are tris-quaternary ammonium compounds which are modulators of nociception and pain. | 05-13-2010 |
| 20100204273 | Quinoline and Quinazoline Derivatives Having Affinity for 5HT1-Type Receptors - Disclosed are methods for use of compounds of formula (I) in the treatment of CNS disorders such as dysthymia, schizophrenia, panic disorder, obsessive compulsive disorder, post-traumatic stress disorder, pain, and memory disorders: | 08-12-2010 |
| 20100137364 | 6-Aminoisoquinoline Compounds - 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided. | 06-03-2010 |
| 20100137363 | Substituted Indoles And Methods Of Their Use - The present invention relates generally to substituted indoles and methods of using them. | 06-03-2010 |
| 20100137362 | HETEROCYCLIC HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME - A hydrazide compound represented by the formula (I), an N-oxide thereof or suitable salt thereof: has excellent pesticidal activity. | 06-03-2010 |
| 20100063089 | SUCCINATE SALT OF 2-((4-(1-METHYL-4-PYRIDIN-4-YL)-1H-PYRAZOL-3-YL)PHENOXY)METHYL)QUINOLINE - The present invention relates to a succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline, and to a method for treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal the succinate salt. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and the succinate salt. | 03-11-2010 |
| 20100120856 | Derivatives of the Aminated Hydroxyquinoline Class For Treating Cancers - The invention relates to compounds of the animated hydroxyquinoline type capable of preventing the migration of metastases or tumoral cells. Such compounds are useful for treating cancers. | 05-13-2010 |
| 20100234424 | DERIVATIVES OF N-PHENYL(PIPERIDINE-2-YL) METHYL BENZAMIDE PREPARATION METHOD THEREOF AND APPLICATIONS OF SAME IN THERAPEUTICS - Compounds of formula (I) as defined herein: | 09-16-2010 |
| 20100105729 | ARYL-SUBSTITUTED HETEROCYCLIC PDE4 INHIBITORS AS ANTI-INFLAMMATORY AGENTS - Disclosed herein are potent and selective aryl-substituted heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role. | 04-29-2010 |
| 20100152237 | BIS-PYRINDINO CONTAINING COMPOUNDS FOR THE USE IN THE TREATMENT OF CNS PATHOLOGIES - N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter. | 06-17-2010 |
| 20120149729 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 06-14-2012 |
| 20120149728 | NOVEL FUMARATE SALTS OF A HISTAMINE H3 RECEPTOR ANTAGONIST - The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof. | 06-14-2012 |
| 20100099706 | ARGATROBAN FORMULATION - An aqueous, stable, sterile pharmaceutical composition of the thrombin inhibitor argatroban in a solution containing an acid to solubilize the argatroban, substantially free from dehydrated alcohol is described, as well as a method for its preparation. | 04-22-2010 |
| 20100099705 | ARGATROBAN FORMULATION - An aqueous, stable, sterile pharmaceutical composition of the thrombin inhibitor argatroban in a solution containing an acid to solubilize the argatroban, substantially free from dehydrated alcohol is described, as well as a method for its preparation. | 04-22-2010 |
| 20100099704 | Lotion Preparation Containing Pyridonecarboxylic Acid Derivative - It is intended to provide a lotion preparation which exerts an excellent antibacterial effect, is excellent in the stability of active ingredient and does not contain an additive having a safety problem. The lotion preparation contains (a) 1-cyclo-propyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid and/or a pharmaceutically acceptable salt thereof, (b) a lower alcohol, (c) a water-soluble polymer and (d) a polyhydric alcohol and the pH of the preparation is in the range of 9 to 12. | 04-22-2010 |
| 20130023559 | ALCOHOL FREE FORMULATION OF ARGATROBAN - An aqueous formulation of argatroban and of related compounds is disclosed along with a reconstitutable formulation, each of which is substantially, if not totally alcohol free. The formulations are also substantially free, if not totally free, of mono-, di-, and oligo-saccharides. An especially preferred embodiment is a ready-to-use 1 mg/ml injectable dosage form having argatroban, lactobionic acid, and methionine. | 01-24-2013 |
| 20100093794 | Use of a Compound in Obtaining Cytoskeleton Blockage and Cell Elongation - A use of a compound in obtaining cytoskeleton and cell elongation is disclosed, the compound is 7-chloro-6-piperidin-1-yl-quinoline-5,8-dione with a chemical formula of C | 04-15-2010 |
| 20100093793 | METHODS FOR TREATING COGNITIVE DISORDERS USING 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS - Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas (1) and (2) wherein the variables have the meaning disclosed in the specification. | 04-15-2010 |
| 20140303207 | Novel 1-Heteroaryl-3-Azabicyclo[3.1.0]Hexanes Methods For Their Preparation And Their Use As Medicaments - The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety. | 10-09-2014 |
| 20100035926 | PYRAZOLE DERIVATIVES AS NON-STEROIDAL GLUCOCORTICOID RECEPTOR LIGANDS - The present invention provides compounds of formula (I): | 02-11-2010 |
| 20100179187 | INDOLONE COMPOUNDS USEFUL TO TREAT COGNITIVE IMPAIRMENT - This invention provides a method of treating a subject suffering from a cognitive impairment or a cognitive disorder which comprises administering to the subject an amount of an indolone compound effective to treat the subject's cognitive impairment or disorder. | 07-15-2010 |
| 20100076019 | ALCOHOL FREE FORMULATION OF ARGATROBAN - An aqueous formulation of argatroban and of related compounds is disclosed along with a reconstitutable formulation, each of which is substantially, if not totally alcohol free. The formulations are also substantially free, if not totally free, of mono-, di-, and oligo-saccharides. An especially preferred embodiment is a ready-to-use 1 mg/ml injectable dosage form having argatroban, lactobionic acid, and methionine. | 03-25-2010 |
| 20100076020 | QUINOLYNYLMETHYLIMIDIZOLES AS THERAPEUTIC AGENTS - Disclosed herein is a compound of the formula (I): (I). Therapeutic methods, compositions and medicaments related thereto are also disclosed. | 03-25-2010 |
| 20100056570 | FUNGICIDES - Compounds of the general formula wherein the substituents are as defined in claim ( | 03-04-2010 |
| 20120015979 | Compounds for Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 01-19-2012 |
| 20120202850 | METHOD FOR TREATING THROMBOSIS AND INHIBITING PLATELET AGGREGATION WITH 21-(S)-ARGATROBAN - A method for inhibiting coagulation including administering to a patient in need thereof a pharmaceutical composition containing 21-(S)-Argatroban and/or a pharmaceutically acceptable salt thereof. Compared with 21-(R)-Argatroban, 21-(S)-Argatroban significantly prolongs coagulation time of whole blood (CT), recalcification time (RT), kaolin partial thromboplastin time (APTT), pro-time prothrombin time (PT), thrombin time (TT), and reduces platelet adhesion rate and platelet aggregation rate in healthy dogs. Therefore, 21-(S)-Argatroban has a stronger effect for inhibiting coagulation and reducing therapeutically effective dose and is suitable for use in a method for treatment and/or prevention of thrombosis and inhibiting platelet aggregation. | 08-09-2012 |
| 20110301195 | TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE - The present invention relates to compound 1, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising Compound 1 and methods of using the compositions in the treatment of proliferative disorders. | 12-08-2011 |
| 20130102633 | TRANSGLUTAMINASE INHIBITORS AND METHODS OF USE THEREOF - Transglutaminase inhibitors and methods of use thereof are provided. | 04-25-2013 |
| 20090247579 | 2-[3H-THIAZOL-2-YLIDINEMETHYL]PYRIDINES AND RELATED COMPOUNDS AND THEIR USE - The present invention pertains to certain 2-[3H-thiazol-2-ylidinemethyl]pyridine compounds and analogs thereof, which, inter alia, inhibit cell proliferation, treat cancer, etc., and more specifically to compounds of the following formula, wherein R | 10-01-2009 |
| 20130005769 | INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: | 01-03-2013 |
| 20130005768 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example. | 01-03-2013 |
| 20130030018 | Tris-Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors - Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders. | 01-31-2013 |
| 20100240699 | METHOD OF TREATING SENSORIMOTOR DISORDERS WITH ALPHA-2 ADRENERGIC RECEPTOR AGONISTS - Disclosed herein is a method of treating sensorimotor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity. | 09-23-2010 |
| 20090318497 | SUBSTITUTED PYRIDYLMETHYL BICYCLICCARBOXYAMIDE COMPOUNDS - This invention provides a compound of the formula (I): wherein A | 12-24-2009 |
| 20130090355 | CHEMICAL AGENTS FOR THE PREVENTION OF INHIBITION OR TUMOR METASTASIS - The present invention provides methods of preventing or inhibiting tumor metastasis in a subject by administering a therapeutically effective amount of (1) a compound from a group of enumerated compounds, or a pharmaceutically acceptable salt thereof; (2) an agent that covalently modifies at least one cysteine residue of S100A4 protein; or (3) an agent that inhibits the interaction between S100A4 and myosin-IIA. | 04-11-2013 |
| 20140336221 | Antibiotic and Anti-Parasitic Agents that Modulate Class II Fructose 1, 6-Bisphosphate Aldolase - This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity. | 11-13-2014 |
| 20130197030 | Substituted 1,3-Dioxanes and There Uses - The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer. | 08-01-2013 |
| 20120149730 | METHODS AND COMPOSITIONS USING RACEMIC, (R)-, AND (S)-FEXOFENADINE IN COMBINATION WITH LEUKOTRIENE INHIBITORS - Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. | 06-14-2012 |
| 20130018072 | AMINOPYRAZOLE TRIAZOLOTHIADIAZOLE INHIBITORS OF C-MET PROTEIN KINASE - The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 01-17-2013 |
| 20150133495 | Substituted Acyloxyamidines as HCV NS3/4A Inhibitors - Disclosed herein is a compound of Formula I | 05-14-2015 |
| 20130123303 | PHARMACEUTICAL COMPOSITIONS COMPRISING 7-(1H-IMIDAZOL-4-YLMETHYL)-5,6,7,8-TETRAHYDRO-QUINOLINE FOR TREATING SKIN DISEASES AND CONDITIONS - The present invention relates to a method for treating skin diseases and skin conditions in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1H-Imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, or its individual enantiomers or the tautomers thereof, or a pharmaceutically acceptable salt thereof. | 05-16-2013 |
| 20130123302 | PROCESS FOR THE PREPARATION OF 2-(CYCLOHEXYLMETHYL)-N--1,2,3,4-TETRAHYDROISOQUINOLINE-7-SULFONAMIDE - Industrially applicable process for preparing 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, and salts thereof. | 05-16-2013 |
| 20130045990 | NOVEL 1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVE USEFUL FOR THE TREATMENT OF DIABETES - The present invention provides a compound of the formula below | 02-21-2013 |
| 20150018388 | Treatment of Amyotrophic Lateral Sclerosis - The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds. | 01-15-2015 |
| 20130116281 | Multiphoton Activable Quinoline Derivatives, Their Preparation and Their Uses - The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention. | 05-09-2013 |
| 20140094490 | ANTI-NEURODEGENERATIVE DISEASE AGENT - The present invention has an object to provide a novel agent for anti-neurodegenerative diseases and solves the object by providing an agent for anti-neurodegenerative diseases containing, as an effective ingredient, the compound(s) represented by the following General formula 1: | 04-03-2014 |
| 20130245066 | 2-Pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors - 2-pyridyl-substituted imidazoles which are used advantageously in the treatment of diseases mediated by ALK 5 or ALK 4 receptor or both. | 09-19-2013 |
| 20120035213 | Quinoline derivative - The present invention provides a compound having a melanin-concentrating hormone receptor antagonistic action and low toxicity, which is useful as an agent for the prophylaxis or treatment of obesity and the like. | 02-09-2012 |
| 20160051534 | PHARMACEUTICAL COMPOSITIONS COMPRISING 7-(1H-IMIDAZOL-4-YLMETHYL)-5,6,7,8- TETRAHYDRO-QUINOLINE FOR TREATING SKIN DISEASES AND CONDITIONS - The present invention relates to a method for treating skin diseases and skin conditions in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1H-Imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, or its individual enantiomers or the tautomers thereof, or a pharmaceutically acceptable salt thereof. | 02-25-2016 |
| 20120095046 | Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders - The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc. | 04-19-2012 |
| 20120101127 | NOVEL TETRAHYDROQUINOLINE DERIVATIVES - The present invention relates to compounds according to formula (I) | 04-26-2012 |
| 20140235673 | PYRIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 08-21-2014 |
| 20160101098 | SMALL MOLECULE ACTIVATORS OF NRF2 PATHWAY - This disclosure relates to compounds that act as activators of the NRF2/KEAP1/ARE pathway. Specifically, the compounds provided herein can act as high affinity reversible bindings for the NRF2 inhibitor, KEAP1. In some cases, NRF2/KEAP1/ARE pathway activation compounds are capable of repressing expression of inflammatory markers and/or reducing levels of TNFa to provide neuroprotective anti-inflammatory effects in the CNS. Such compounds are useful in the treatment of a variety of diseases including Huntington's disease, Parkinson's disease, Alzheimer's disease, inflammation, and cancer. | 04-14-2016 |
| 20130331414 | Inhibitors of Retroviral Replication - Methods for preventing or treating retroviral infection, such as human immunodeficiency virus, in vivo utilize transcriptional inhibitory compounds. These include cortistatin A and analogs of the cortistatin family. | 12-12-2013 |
| 20140163069 | COMPOSITIONS OF TARGETED DRUG DEVELOPMENT - Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR. | 06-12-2014 |
| 20120122924 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 05-17-2012 |
| 20110301194 | Method for Determining Treatment Efficacy - The present invention provides a method for determining the efficacy of a c-Met inhibitor in treating a cell proliferative disorder, comprising: a) administering to a subject in need thereof a therapeutically effective amount of the c-Met inhibitor, or a pharmaceutically acceptable salt, prodrug or metabolite thereof, either alone or in combination with a therapeutically effective amount of a second anti-proliferative agent; and b) measuring the concentration of hepatocyte growth factor (HGF) in the serum from the subject, wherein if the concentration of serum HGF does not decrease, or if the concentration of serum HGF increases, the c-Met inhibitor is efficacious in treating the cell proliferative disorder. | 12-08-2011 |
| 20110301193 | METHODS AND COMPOSITIONS OF TARGETED DRUG DEVELOPMENT - Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR. | 12-08-2011 |
| 20120083508 | ALPHA-2B RECEPTOR AGONIST AND ANTICONVULSANT COMPOSITIONS FOR TREATING CHRONIC PAIN - Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an alpha-2B receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed. | 04-05-2012 |
| 20110294849 | AMINOPYRAZOLE TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE - The present invention relates to anhydrous and hydrated forms of Compound 1, which qre useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 12-01-2011 |
| 20110294848 | SMALL MOLECULE INHIBITORS OF BOTULINUM NEUROTOXINS - The invention provides potent quinolinol-based BoNT/A small-molecule inhibitors of botulinum neurotoxins, in particular of | 12-01-2011 |
| 20150289795 | METHODS AND KITS FOR THE PROGNOSIS OF COLORECTAL CANCER - The invention relates to methods for predicting the risk of relapse of cancer patients as well as methods for providing personalized medicine to said patients based on the expression levels of different genes the expression of which is induced in response to TGF-beta stimulation. The invention also relates to kits for carrying out the diagnostic and predictive medicine methods. | 10-15-2015 |
| 20110294850 | INDOLINE DERIVATIVES - The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R | 12-01-2011 |
| 20110312996 | NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. | 12-22-2011 |
| 20140235672 | CHROMENE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MCP-1 or CCR-2 of formula | 08-21-2014 |
| 20110306635 | PYRIDINE COMPOUNDS AS SUBTYPE SELECTIVE MODULATORS OF ALPHA2B AND /OR ALPHA 2C ADRENERGIC RECEPTORS - The invention relates specifically to the use of certain 4-[1-(1H-Imidazol-4-yl)-ethyl]-2,3-substituted pyridine compounds and pharmaceutical compositions thereof to treat disorders associated with selective subtype alpha 2 adrenergic receptor modulation. | 12-15-2011 |
| 20110319447 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 12-29-2011 |
| 20100016355 | ALPHA-2B ADRENERGIC RECEPTOR AGONIST AND SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITOR COMPOSITIONS FOR TREATING CHRONIC PAIN - Disclosed herein is a pharmaceutical composition comprising a serotonin-norepinephrine reuptake inhibitor and an alpha-2B receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed. | 01-21-2010 |
| 20100016356 | METHOD FOR TREATING THROMBOSIS AND INHIBITING PLATELET AGGREGATION WITH 21-(S)-ARGATROBAN - A method for inhibiting coagulation including administering to a patient in need thereof a pharmaceutical composition having 21-(S)-Argatroban and/or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for inhibiting coagulation having 21-(S)-Argatroban and/or a pharmaceutically acceptable salt thereof. Compared with 21 (R) Argatroban, 21-(S)-Argatroban significantly prolongs coagulation time of whole blood (CT), recalcification time (RT), kaolin partial thromboplastin time (APTT), pro-time prothrombin time (PT), thrombin time (TT), and reduces platelet adhesion rate and platelet aggregation rate in healthy dogs. Therefore, 21-(S)-Argatroban has a stronger effect of inhibiting coagulation and reducing therapeutically effective dose and is suitable for treatment and/or prevention of thrombosis and inhibiting platelet aggregation. | 01-21-2010 |
| 20100016353 | BENZOIMIDAZOLE DERIVATIVES USEFUL AS ANTIPROLIFERATIVE AGENTS - The invention relates to substantially pure compounds of the formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R, R | 01-21-2010 |
| 20130310421 | TREATMENT OF AMYLOID BETA AMYLOIDOSIS - Provided is a method for the treatment and/or prevention of an amyloid beta amyloidosis in a subject comprising the step of administering to the subject an effective amount of a 5-lipoxygenase-activating protein (FLAP) antagonist. In preferred embodiments, the FLAP antagonist is MK-591, or a pharmaceutically acceptable salt thereof. Also provided is a method for decreasing or preventing the deposition of beta amyloid in the brain of a subject comprising the step of administering to a subject an effective amount of a FLAP antagonist. In preferred embodiments, the FLAP antagonist is MK-591, or a pharmaceutically acceptable salt thereof. | 11-21-2013 |
| 20130131109 | BICYCLIC DERIVATIVES AS MODULATORS OF VOLTAGE GATED ION CHANNELS - Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions. | 05-23-2013 |
| 20140148484 | PYRAZOLE COMPOUNDS FOR TREATING HAIRLOSS - The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof for use in the treatment or prevention of hairloss, | 05-29-2014 |
| 20140045890 | NOVEL COMPOUNDS - Compounds of the general formula (I) wherein the substituents are as defined in claim | 02-13-2014 |
| 20110065748 | COMPOSITIONS AND METHODS FOR TREATING DISORDERS OF GASTROINTESTINAL MOTILITY - Disclosed are methods of treating disorders of gastrointestinal motility by administering to a patient in need of such treatment a compound having the following formula: | 03-17-2011 |
| 20110065747 | COMPOSITIONS AND METHODS FOR TREATING SEIZURE DISORDERS - Disclosed are methods of treating a seizure disorder by administering to a patient in need of such treatment a compound having the following formula: | 03-17-2011 |
| 20110275669 | Novel pyrroles having hypolipidemic hypocholesteremic activities, process for their preparation and pharmaceutical compositions containing them and their use in medicine - The present invention relates to compounds of the general formula (I) | 11-10-2011 |
| 20120295936 | COMPOSITIONS AND METHODS FOR TREATING SEIZURE DISORDERS - Disclosed are methods of treating a seizure disorder by administering to a patient in need of such treatment a compound having the following formula: | 11-22-2012 |
| 20130217727 | 1-(HETEROCYCLIC CARBONYL)-2-SUBSTITUTED PYRROLIDINES - The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. | 08-22-2013 |
| 20130137725 | METHOD OF TREATING SENSORIMOTOR DISORDERS WITH ALPHA-2 ADRENERGIC RECEPTOR AGONISTS - Disclosed herein is a method of treating sensorimotor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity. | 05-30-2013 |
| 20130137724 | PHARMACEUTICAL COMPOSITIONS COMPRISING 7-(1H-IMIDAZOL-4-YLMETHYL)-5,6,7,8-TETRAHYDRO-QUINOLINE FOR RETINAL NEUROPROTECTION - The present invention relates to a method for retinal neuroprotection or for treating retinal diseases, in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1H-Imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, its enantiomers or pharmaceutically acceptable salts thereof. | 05-30-2013 |
| 20150307463 | SUBSTITUTED ISOXAZOLE AMIDE COMPOUNDS AS INHIBITORS OF STEAROYL-COA DESATURASE 1 (SCD1) - The invention is concerned with a compound of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compound of formula (I) as well as pharmaceutical compositions containing such compounds. The compound of formula (I) are SCD1 inhibitors and may be useful in treating cancer. | 10-29-2015 |
| 20110144156 | A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS - Provided are 2,4-disubstituted quinoline derivatives that are A3 adenosine receptor modulators (A | 06-16-2011 |
| 20120277265 | NOVEL POLYQUINOLINE DERIVATIVES AND THE THERAPEUTIC USE THEREOF - The invention relates to a method for chelating metal ion and/or dissolving amyloid aggregates, including chelating metal ions and/or dissolving amyloid aggregates with a compound of formula (I): | 11-01-2012 |
| 20160022634 | NOVEL 1-HETEROARYL-3-AZABICYCLO[3.1.0]HEXANES, METHODS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety. | 01-28-2016 |
| 20140113934 | HETEROCYCLIC COMPOUNDS FOR TREATING HELMINTH INFECTIONS - Disclosed are compounds of Formula 1, N-oxides, and salts thereof, | 04-24-2014 |
| 20140088144 | INHIBITING MICROBIAL INFECTIONS - A method of inhibiting a microbial infection can include: providing a compound of the invention or prodrugs or pharmaceutically acceptable salts thereof; and administering the compound to a subject in a therapeutically effective amount to inhibit the microbial infection. The therapeutically effective amount can be sufficient to inhibit a biological activity of a transcriptional activator of the microbe. The inhibited transcriptional activator is an AraC bacterial transcriptional activator. The AraC bacterial transcriptional activator can be RhaS, RhaR, Rns, or VirF. The microbe can be selected from | 03-27-2014 |
| 20120316200 | PYRIDONE DERIVATIVES - The present invention is directed to novel phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be useful in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases. | 12-13-2012 |
| 20110251238 | PPAR AGONIST COMPOSITIONS AND METHODS OF USE - Method for treating or preventing a PPAR-responsive condition in a subject, comprising administering to the subject a PPAR agonist that comprises a 8-hydroxyquinoline-methylene-N- group in an amount effective to activate a PPAR polypeptide. | 10-13-2011 |
| 20110251236 | GALACTOKINASE INHIBITORS - Therapeutic agents for treatment of Galactosemia and disorders thereof, and other enzyme related disorders thereof are identified. The compounds inhibit galactokinase (GALK) and other kinase activity and are identified by a high throughput screening assay. | 10-13-2011 |
| 20110263646 | 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. | 10-27-2011 |
| 20110281909 | SUBSTITUTED QUINOLINE DERIVATIVES AS H1 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula (I), | 11-17-2011 |
| 20110263647 | FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE - The invention relates to thiazole compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. | 10-27-2011 |
| 20110207774 | TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE - The present invention relates to compound 1, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising Compound 1 and methods of using the compositions in the treatment of proliferative disorders. | 08-25-2011 |
| 20110207772 | Glycine Chroman-6-Sulfonamides for Use as Inhibitors of Diacylglycerol Lipase - The present disclosure is generally directed to compounds that can inhibit DAGLα and/or β activity, compositions comprising such compounds, and methods for inhibiting DAGLα and/or β activity. | 08-25-2011 |
| 20110207771 | N-(L-ALKYL-2-PHENYLETHYL)-CARBOXAMIDE DERIVATIVES AND USE THEREOF AS FUNGICIDES - Compounds of the formula (I) in which the substituents are as defined in claim | 08-25-2011 |
| 20110178125 | USE OF GALR3 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF DEPRESSION AND/OR ANXIETY AND COMPOUNDS USEFUL IN SUCH METHODS - This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. | 07-21-2011 |
| 20110190344 | BENZIMIDAZOLE MODULATORS OF VR1 - The invention is directed to compounds of Formula (I): | 08-04-2011 |
| 20110190343 | HIV-1 FUSION INHIBITORS AND METHODS - A new series of HIV-1 fusion inhibitors and methods of use are disclosed. The compounds are based on a substituted indole, benzimidazole, indoline or isoindoline fragment. The compounds find use in inhibiting or preventing HIV fusion from occurring, thus inhibiting or preventing entry of viral RNA into host cells. The compounds may be useful towards other biological targets involving protein-protein interactions. | 08-04-2011 |
| 20080312278 | Hydroxyquinoline Derivatives - Compounds of the formula I in which X, Y, R | 12-18-2008 |
| 20090197914 | Piperidine Derivatives, Their Process for Preparation, Their Use as Therapeutic Agents and Pharmaceutical Compositions Containing Them - The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state. | 08-06-2009 |
| 20090018164 | 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. | 01-15-2009 |
| 20090076077 | Methods and Compositions for Selectin Inhibition - The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selecting. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compound of Formula I: | 03-19-2009 |
| 20090054484 | SUBSTITUTED HETEROARYL BENZOFURAN ACIDS - The present invention relates generally to substituted heteroaryl benzofuran acids and methods of using them. | 02-26-2009 |
| 20090176829 | BICYCLIC HETEROARYL COMPOUNDS AS PDE10 INHIBITORS - The invention pertains to tricyclic heteraaryi compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds which are selective inhibitors of PDE 10. The invention further relates to pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom. | 07-09-2009 |
| 20090054483 | Substituted Quinolines as Inhibitors of Leukotriene Biosynthesis - The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents. | 02-26-2009 |
| 20090143429 | Quinoline Derivatives as Neurokinin Receptor Antagonists - The present invention relates to substituted quinoline derivatives of Formula (I); wherein hal, n, A, formula (a), R | 06-04-2009 |
| 20080242701 | Novel Compounds And Methods Of Use Thereof - This invention relates to treating cancer or an angiogenesis-related disease using a compound of formula 1: | 10-02-2008 |
| 20090042936 | Compositions and Methods for Treating or Controlling Anterior-Segment Inflammation - A composition for treating or controlling an inflammatory anterior-segment disease or condition comprises a dissociated glucocorticoid receptor agonist (“DIGRA”). The composition can optionally include an anti-inflammatory agent, an anti-infective agent, or both. The composition can be formulated for topical application, injection, or implantation in the anterior portion of the eye or a tissue adjacent thereto. | 02-12-2009 |
| 20080275083 | 2,3,4,9-TETRAHYDRO-1H-CARBAZOLES - The present invention relates to 2,3,4,9-tetrahydro-1H-carbazoles of the general formula I, | 11-06-2008 |
| 20080287492 | Alkylpyridyl Quinolines as Nk3 Receptor Modulators - Compounds of Formula I | 11-20-2008 |
| 20080287491 | Tetrahydroquinoline Derivative for Treating Nicotine Craving - The present invention relates to a new medical use for a compound of formula (I): | 11-20-2008 |
| 20090163546 | DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - Provided herein are compounds of the formula (I): | 06-25-2009 |
| 20090186918 | Triazole Compounds as Lipoxygenase Inhibitors - There is provided compounds of formula (I) wherein W is an optionally substituted aryl or heteroaryl group, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation. | 07-23-2009 |
| 20090105301 | 9A-SUBSTITUTED AZALIDES FOR THE TREATMENT OF MALARIA - The present invention relates to novel 9a-substituted azalides having antimalarial activity. More particularly, the invention relates to 9a-substituted 9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A, 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-5-O-dedesosaminyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity, to the method of preparation, to the method of use, and to pharmaceutically acceptable derivatives thereof having antimalarial activity. | 04-23-2009 |
| 20090131475 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B—C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example. | 05-21-2009 |
| 20090221636 | ARGATROBAN FORMULATIONS AND METHODS FOR MAKING AND USING SAME - Formulations comprising argatroban and methods of making and using the formulations are provided. In an embodiment, the formulation comprises a solution having an argatroban concentration ranging from greater than about 10 to about 500 mg/mL. The solution can comprise an aqueous solution. The solution can be packaged in a sealed container that may either be aseptically-filled or subjected to sterilization to reduce the microbiological burden of the formulation. The solution can further be diluted and administered to persons needing same. | 09-03-2009 |
| 20090018163 | Substituted Heterocyclic Ethers and Their Use in CNS Disorders - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders. | 01-15-2009 |
| 20090221638 | 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. | 09-03-2009 |
| 20090221637 | SOLID-STATE SALT ARGATROBAN FORMULATIONS AND METHODS FOR PRODUCING AND USING THE SAME - Argatroban formulations and methods of making and using the formulations are provided. In an embodiment, the present disclosure provides a solid-state salt formulation of argatroban. Upon reconstitution, the solid-state argatroban forms a solution that can be essentially free of particles and suitable for administration. The solid-state argatroban can be in a crystalline and/or amorphous form. The solid-state argatroban can be packaged in a sealed container that may be aseptically-filled to reduce the microbiological burden of the formulation. The solid-state argatroban can be reconstituted with a solution and administered to persons needing same. | 09-03-2009 |
| 20090192191 | Substituted hydroxamic acid derivatives as tnf inhibitors - The present invention relates to novel compounds of formula (I) and their pharmaceutically useful compositions as MMP and TNF inhibitors. | 07-30-2009 |
| 20090176828 | 4-(CONDENSED CYCLICMETHYL)-IMIDAZOLE-2-THIONES ACTING AS ALPHA2 ADRENERGIC AGONISTS - Compounds of Formula 1 | 07-09-2009 |
| 20080312277 | Gpr41 and Modulators Thereof for the Treatment of Insulin-Related Disorders - The present invention relates to a method for identifying a glycemic stabilizing compound by: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is modulated, where a modulation in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound. In addition, the invention relates to a method for identifying a glycemic stabilizing compound, comprising: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is increased, wherein an increase in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound. Further, the invention relates to a method for identifying a glycemic stabilizing compound, comprising: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is decreased, wherein a decrease in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound. | 12-18-2008 |
| 20080262036 | Phenyl-[1,2,4]-oxadiazol-5-one Derivatives, Pharmaceutical Compositions and Therapeutic Use Thereof - The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: | 10-23-2008 |
| 20080287493 | ARYLMETHYLEN SUBSTITUTED N-ACYL-Y-AMINOALCOHOLS - The present invention relates to arylmethylen substituted N-acyl-Y-aminoalcohols of the general formula I | 11-20-2008 |
| 20080221161 | HETEROCYCLIC MODULATORS OF TGR5 FOR TREATMENT OF DISEASE - Disclosed herein are compounds useful as modulators of TGR5 and methods for the treatment or prevention of metabolic, cardiovascular, and inflammatory diseases. | 09-11-2008 |
| 20090088452 | Indole Orexin Receptor Antagonists - The present invention is directed to substituted indole compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 04-02-2009 |
| 20080300272 | Alcohol free formulation of argatroban - An aqueous formulation of argatroban and of related compounds is disclosed along with a reconstitutable formulation, each of which is substantially, if not totally alcohol free. The formulations are also substantially free, if not totally free, of mono-, di-, and oligo-saccharides. An especially preferred embodiment is a ready-to-administer 1 mg/ml injectable dosage form having argatroban, lactobionic acid, and methionine. | 12-04-2008 |
| 20080280949 | Oxopyridyl Quinoline Amides as Nk3 Receptor Modulators - Compounds of Formula I wherein R | 11-13-2008 |
| 20090170898 | Sulphonamide Derivatives as Modulators of the Glucocorticoid Receptor - Compounds of formula (I): | 07-02-2009 |
| 20080249131 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Various carbonyl amides are employed in vitro and in vivo as non-nucleoside inhibitors of a reverse transcriptase, and particularly of HIV reverse transcriptase. Therefore, contemplated compounds may be employed in the treatment of HIV infected patients. Further contemplated aspects include pharmaceutical compositions comprising therapeutically effective amounts of contemplated compounds. | 10-09-2008 |
| 20090048297 | 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION - The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I | 02-19-2009 |
| 20090239906 | ALKOXYALKYL-SUBSTITUTED CYCLIC KETOENOLS - The invention relates to new alkoxyalkyl-substituted cyclic ketoenols of the formula (I) | 09-24-2009 |
| 20090239905 | PIPERIDINES AND RELATED COMPOUNDS FOR THE TREATMENT OF DEMENTIA - Compounds of formula I: modulate the action of gamma secretase, and hence find use in treatment of Alzheimer's disease and related conditions. | 09-24-2009 |
| 20090099231 | 3-Sulfonylamino-Pyrrolidine-2-One Derivatives as Factor Xa Inhibitors - The present invention provides pyrrolidinone derivatives as Factor Xa inhibitors and pharmaceutical compositions comprising the same. The invention also relates to processes for the preparation of such compounds, and the use of such compounds in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated. | 04-16-2009 |
| 20090069374 | Novel 1-Heteroaryl-3-Azabicyclo[3.1.0]Hexanes, Methods For Their Preparation And Their Use As Medicaments - The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety. | 03-12-2009 |
| 20090048298 | Novel acetyl-CoA Carboxylase (ACC) Inhibitors and their use in Diabetes, Obesity and Metabolic Syndrome - The present invention relates to compounds of formula (I) | 02-19-2009 |
| 20090023776 | 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. | 01-22-2009 |
| 20080293766 | SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR - The present invention provides a method of inhibiting an androgen receptor by administering a compound of Formula I: | 11-27-2008 |
| 20080319013 | 4-(SUBSTITUTED CYCLOALKYLMETHYL) IMIDAZOLE-2-THIONES, 4-(SUBSTITUTED CYCLOALKENYLMETHYL) IMIDAZOLE-2-THIONES, 4-(SUBSTITUTED CYCLOALKYLMETHYL) IMIDAZOLE-2-ONES AND, 4-(SUBSTITUTED CYCLOALKYLMETHYL) IMIDAZOLE-2-ONES AND RELATED COMPOUNDS - Compounds of Formula 1 | 12-25-2008 |
| 20080319012 | 2-Pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors - 2-pyridyl-substituted imidazoles which are used advantageously in the treatment of diseases mediated by ALK 5 or ALK 4 receptor or both. | 12-25-2008 |
| 20080319011 | PROTEIN TYROSINE KINASE ENZYME INHIBITORS - This invention provides compounds of formula 1, having the structure | 12-25-2008 |
| 20080214607 | HETEROAROMATIC QUINOLINE COMPOUNDS - The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders. | 09-04-2008 |
| 20080200504 | Amide Alkyl Pyridiyl Quinolines as Nk3 Receptor Modulators - Compounds of Formula (I) wherein R | 08-21-2008 |
| 20080234319 | Novel Compounds 679 - The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R | 09-25-2008 |
| 20160143899 | METHOD FOR TREATING ABNORMAL B-AMYLOID MEDIATED DISEASES - A method for treating abnormal β-amyloid mediated diseases is disclosed, comprising administering a pharmaceutical composition to a subject in need, wherein the pharmaceutical composition comprises an indolylquinoline derivative represented by the following formula 1: | 05-26-2016 |
