| Entries |
| Document | Title | Date |
|---|
| 20080214606 | Methods for the Identification and Use of Compounds Suitable for the Treatment of Drug Resistant Cancer Cells - The present invention relates to novel methods for the identification of compounds useful for the treatment of drug resistance, and to novel treatment methods using the identified compounds. | 09-04-2008 |
| 20080227812 | 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 |
| 20080234318 | Chemical Compounds - The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell. | 09-25-2008 |
| 20080249130 | Gut microsomal triglyceride transport protein inhibitors - Compounds represented by formula (I): | 10-09-2008 |
| 20080262035 | Amide Derivatives as Inhibitors of Histone Deacetylase - The present invention relates to carboxylic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases. | 10-23-2008 |
| 20080269284 | Compounds and Methods for Treating Dyslipidemia -
Compounds of Formula I wherein n, q, Y, R | 10-30-2008 |
| 20080293765 | Alkylsulphonamide Quinolines - Compounds of Formula I | 11-27-2008 |
| 20080312274 | Quinoline Derivatives as Neurokinin Receptor Antagonists - The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-2 and/or neurokinin-3 (NK-3) receptors, such as schizophrenia. | 12-18-2008 |
| 20080312275 | Novel Cyanoguanidine Compounds -
Novel pyridyl cyanoguanidine compounds of general formula I (I) wherein R | 12-18-2008 |
| 20080312276 | 4,5 Dihydro-(1H)-Pyrazole Derivatives as Cannabinoid CB1 Receptor Modulators - The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB | 12-18-2008 |
| 20080319010 | Use of Chloroquine to Treat Metabolic Syndrome - The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and/or an inhibitor of cholesterol synthesis or absorption. | 12-25-2008 |
| 20090023775 | 1-[2-(4-BENZYL-4-HYDROXY-PIPERIDIN-1 -YL )-ETHYL]-3-(2-METHYL-QUINOLIN- 4-YL)- UREA AS CRYSTALLINE SULFATE SALT - The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt and a process for its preparation. Further, the present invention relates to the use of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt alone or in combination with other compounds. Further, the present invention relates to formulations of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt in the preparation of pharmaceutical compositions. The invention also relates to the use of such sulfate salts in formulations as neurohormonal antagonists. | 01-22-2009 |
| 20090069373 | Quinoline Acids - This invention relates generally to quinoline-based modulators of Liver X receptors (LXRs) and related methods. | 03-12-2009 |
| 20090076076 | INHIBITORS OF CYSTEINE PROTEASES AND METHODS OF USE THEREOF - The present invention relates to semicarbazone or thiosemicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L. | 03-19-2009 |
| 20090082395 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases. | 03-26-2009 |
| 20090082396 | 5-ARYL-4,5-DIHYDRO-(1H)-PYRAZOLINES AS CANNABINOID CB1 RECEPTOR AGONISTS - The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB | 03-26-2009 |
| 20090088451 | QUINOLINES - The present invention relates to 2-aminoquinolines of formula I | 04-02-2009 |
| 20090105300 | AMINE LINKED MODULATORS OF y-SECRETASE - The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, R | 04-23-2009 |
| 20090111852 | Carboxamide Compound and Use of the Same - A carboxamide compound represented by the formula (1): | 04-30-2009 |
| 20090118328 | Pharmaceutical Compositions Of Cholesteryl Ester Transfer Protein Inhibitors And Hmg-Coa Reductase - A solid amorphous dispersion comprises a cholesteryl ester transfer protein (CETP) inhibitor, an inhibitor of 3-hydroxy-3-methylglutaryl-conenzyme A reductase (HMG-CoA reductase inhibitor), and a concentration enhancing polymer. At least a major portion of the CETP inhibitor in the dispersion is amorphous. The solid amorphous dispersion provides concentration-enhancement of the CETP inhibitor when administered to an aqueous use environment. | 05-07-2009 |
| 20090118329 | Novel Substituted 2-Amino-4-Phenyldihydroquinolines, Processes for their Preparation, Pharmaceutical Compositions and Methods for Their Use - The invention relates to NHE-3 inhibitor compounds of formula I: | 05-07-2009 |
| 20090143428 | Quinoline Derivatives 057 - The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy. | 06-04-2009 |
| 20090170897 | Method of Treating Neuropathic Pain - The invention relates to the use of a CRTH2 receptor antagonist in the manufacture of a medicament for the treatment of neuropathic pain and to a method of treating neuropathic pain using an antagonist of CRTH2 receptor. | 07-02-2009 |
| 20090176827 | MALEATE SALTS OF (E)-N--4-(DIMETHYLAMINO)-2-BUTENAMIDE AND CRYSTALLINE FORMS THEREOF - The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family. | 07-09-2009 |
| 20090203735 | TREATMENTS FOR NEUROPATHY - Small fiber neuropathy is treated or prevented by topically administering to a subject in need thereof topically active quinoline compounds or pharmaceutically acceptable salts thereof under conditions effective to treat or prevent neuropathy in the subject. Glial cell-derived neurotrophic factor (GDNF) receptors are modulated with the subject active quinoline compounds, which may be formulated in topical lotions. | 08-13-2009 |
| 20090270450 | CHEMICAL COMPOUNDS - The invention relates to chemical compounds of formula (I): | 10-29-2009 |
| 20090275612 | Compound With Antimalarial Activity And Antimalarial Drug Containing The Same As Active Ingredient - Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R | 11-05-2009 |
| 20100022588 | PHARMACEUTICAL CARRIER COMPOSITION AND PHARMACEUTICAL COMPOSITION - The present invention relates to a pharmaceutical carrier composition and a pharmaceutical composition comprising said pharmaceutical carrier composition. The pharmaceutical composition comprises: (a) at least 20% (w/w) of the composition of a sugar or a sugar alcohol; (b) one or more pharmaceutically acceptable excipients; (c) one or more pharmaceutically active ingredients in their base form; and (d) water up to 100% (w/w). The present pharmaceutical composition is especially resistant against flocculation, clumping and/or precipitation at room temperature during prolonged time-periods such as one or more years. | 01-28-2010 |
| 20100029716 | NOVEL 1,2,3,4- TETRAHYDROQUINOLINE DERIVATIVES - The present invention relates to a novel derivative of Compound 1 selectively substituted with fluorine and/or deuterium and optionally further substituted with deuterium and | 02-04-2010 |
| 20100029717 | Alkylsulphonamide Quinolines - Compounds of Formula I | 02-04-2010 |
| 20100035924 | NOVEL 4-AMINO-PYRIDINE DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel 4-amino-pyridine derivative useful as modulators of small-conductance calcium-activated potassium channels (SK channels). 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. | 02-11-2010 |
| 20100035925 | COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AN DMETHODS FOR INHIBITING HIV INFECTIVITY - Compounds that possess anti-infective activity are described. Methods of using these compounds for the treatment or prevention of infectious diseases such as acquired immunodeficiency syndrome (AIDS) are also described. The compounds inhibit HIV infectivity and do not exhibit significant cytotoxicity in HIV producing cells. | 02-11-2010 |
| 20100041698 | HETEROCYCLIC COMPOUNDS AND THEIR USE AS BINDING PARTNERS FOR 5-HT5 RECEPTORS - The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions. | 02-18-2010 |
| 20100087482 | Method for Treating Gefitinib Resistant Cancer - The present invention is directed to methods for the treatment of gefitinib and/or erlotinib resistant cancer. An individual with cancer is monitored for cancer progression following treatment with gefitinib and/or erlotinib. Progression of the cancer is indicative that the cancer is resistant to gefitinib and/or erlotinib. Once progression of cancer is noted, the subject is administered a pharmaceutical composition comprising an irreversible epidermal growth factor receptor (EGFR) inhibitor. In preferred embodiments, the irreversible EGFR inhibitor is EKB-569, HKI-272 and HKI-357. | 04-08-2010 |
| 20100099703 | PHENYLAMINO-SUBSTITUTED PIPERIDINE COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to phenylamino-substituted piperidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals. | 04-22-2010 |
| 20100120853 | Derivatives of Hypoestoxide and Related Compounds - Novel diterpene compounds, in particular, hypoestoxide-related compounds, are provided in pure form or as contained in the native plant source, for treatment and prophylaxis of cancer, inflammatory diseases, hyperlipidemias, malaria, and diabetes mellitus. Embodiments also pertain to methods for using the hypoestoxide-related compounds to treat various diseases and symptoms associated with those diseases. | 05-13-2010 |
| 20100125091 | SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula (I): | 05-20-2010 |
| 20100168163 | CYCLIC-ALKYLAMINE DERIVATIVES AS 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 of formula (I) wherein n, m, p, t, R | 07-01-2010 |
| 20100249184 | INDUCTION AND/OR MAINTENANCE OF TUMOR DORMANCY BY DISRUPTION OF UROKINASE PLASMINOGEN ACTIVATOR RECEPTOR-INTEGRIN INTERACTION - The present invention relates to a method of inducing cancer cells into dormancy and treating cancer in a subject. This method involves administering to a subject an effective amount of a compound that disrupts interaction between urokinase plasminogen activator receptor and integrin, thereby including cancer cells into dormancy and treating cancer in the subject. Also disclosed is a method of disrupting interaction between integrin and urokinase plasminogen activator receptor on cancer cells. The present invention also relates to a method of screening for compounds effective in inducing tumor dormancy and treating cancer in a subject. | 09-30-2010 |
| 20110003851 | SMALL MOLECULE HEMATOPOIETIC GROWTH FACTOR MIMETIC COMPOUNDS THAT ACTIVATE HEMATOPOIETIC GROWTH FACTOR RECEPTORS - The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders. | 01-06-2011 |
| 20110009448 | Compound - A compound having Formula I | 01-13-2011 |
| 20110021562 | TREATMENT OF FRIEDREICH'S ATAXIA USING HISTONE DEACETYLASE INHIBITORS - The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors. | 01-27-2011 |
| 20110053976 | QUINOLINE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS - A compound of formula (I) | 03-03-2011 |
| 20110077270 | Compositions and Methods for Treating Ocular Inflammation with Lower Risk of Increased Intraocular Pressure - A composition for treating or controlling an ocular disease or condition comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), which disease or condition has an etiology, or results, in inflammation. 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 an affected eye to treat or control the ocular inflammatory disease or condition. | 03-31-2011 |
| 20110086877 | Small Molecule Inhibitors of Botulinum Neurotoxins - Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein. | 04-14-2011 |
| 20110086878 | Treatments for Neuropathy - Small fiber neuropathy is treated or prevented by topically administering to a subject in need thereof topically active quinoline compounds or pharmaceutically acceptable salts thereof under conditions effective to treat or prevent neuropathy in the subject. Glial cell-derived neurotrophic factor (GDNF) receptors are modulated with the subject active quinoline compounds, which may be formulated in topical lotions. | 04-14-2011 |
| 20110136864 | TETRAHYDROQUINOLINE INDOLE DERIVATIVES AND USES THEREOF - Compounds of the formula: | 06-09-2011 |
| 20110152317 | PREVENNTING THE OCCURRENCE OF OBESITY - Administration of autophagy inhibitor (e.g. 400 mg chloroquine daily) prevents occurrence of obesity and insulin resistance in human subject on prolonged high-fat diet. | 06-23-2011 |
| 20110166180 | METHOD FOR TREATMENT OF BONE DISEASES AND FRACTURES - Described herein are compounds, compositions, and methods useful for treating bone diseases or defects. Also described herein are compounds, compositions and methods for treating bone diseases or defects by inhibiting phosphatase complexes. | 07-07-2011 |
| 20110172270 | 2-'4(PHENYLAMINO)-PIPERIDIN-1-YL!-N-PHENYL-ACETAMINE DERIVATIVES AND RELATED COMPOUNDS AS NEUROPEPTIDE Y5 (NPY5) LIGANDS FOR THE TREATMENT OF OBESITY - 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim | 07-14-2011 |
| 20110178124 | PYRIDINIUM AND QUINOLINIUM DERIVATIVES - The invention provides compounds of formula I blocking phosphorylcholine biosynthesis by means of the selective blocking of the choline kinase enzyme in tumor cells or in cells affected by parasitic infection and therefore being applicable in the treatment of tumors and parasitic diseases or diseases produced by viruses and fungi in animals, including human beings; as well as to a method for preparing the compounds of the invention and certain intermediates of said method. | 07-21-2011 |
| 20110184018 | METHOD FOR TREATING PERIPHERAL NEUROPATHIC PAIN - A method for the treatment of peripheral neuropathic pain in a mammal is provided. The method comprises administering to a mammal (e.g., a human) suffering from peripheral neuropathic 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. The diphenylureido-dihalokynurenate compounds are shown to be agonists of cannabinoid receptor 1 (CB1) and stimulate CB1 activity. | 07-28-2011 |
| 20110263645 | Compositions and Methods of Treating Retinal Disease - Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed | 10-27-2011 |
| 20110275668 | Compound with antimalarial activity and antimalarial drug containing the same as active ingredient - Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R | 11-10-2011 |
| 20110281908 | Aminoquinoline Derived Heat Shock Protein 90 Inhibitors, Methods Of Preparing Same, And Methods For Their Use - Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors and methods for making these classes are provided herein. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases, such as inflammation and neurodegenerative disorders. Also provided herein are methods of treating and preventing cancer and other Hsp90 related disease. The methods include administering to a subject a therapeutically effective amount of an Hsp90 inhibitor. | 11-17-2011 |
| 20120010240 | CUT-POINT IN PTEN PROTEIN EXPRESSION THAT ACCURATELY IDENTIFIES TUMORS AND IS PREDICTIVE OF DRUG RESPONSE TO A PAN-ErbB INHIBITOR - A cut-point in the quantitative measurement of PTEN protein expression that accurately identifies tumors with two inactivated alleles of the PTEN gene. Patients with a normalized PTEN score of PTEN null will be treated with a pan-ErbB tyrosine kinase inhibitor. A normalized PTEN protein expression score is obtained by comparing the tumor PTEN OD expression value with the non-malignant PTEN OD expression value. | 01-12-2012 |
| 20120022103 | ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF - The present application is directed to compounds that are TRPV1 antagonists and have formula (I) | 01-26-2012 |
| 20120041024 | QUINOLYL AMINES AS KINASE INHIBITORS - Disclosed are compounds having the formula: | 02-16-2012 |
| 20120071507 | TREATMENT REGIMEN UTILIZING NERATINIB FOR BREAST CANCER - An extended regimen for treatment of HER-2/neu overexpressed/amplified cancer is described, with involves delivering a course of neratinib therapy to HER-2/neu overexpressed/amplified cancer patients following the completion of surgical and adjuvant therapy. The neratinib regimen may be continued for upwards of twelve months to five years. Also provided are pharmaceutical kits designed to facilitate compliance with the regimen. | 03-22-2012 |
| 20120071508 | CYCLIC-ALKYLAMINE DERIVATIVES AS 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 of formula (I) | 03-22-2012 |
| 20120077843 | MALIGNANT PRECURSOR CELLS FROM DUCTAL CARCINOMA IN SITU LESIONS - Described herein are progenitor cancer cells and cell lines isolated from human breast ductal carcinoma in situ (DCIS) lesions and the uses of these cells or cell lines in drug design, drug screening, and monitoring in vivo therapy. The DCIS malignant precursor cells or cell lines are epithelial in origin, are positive for markers of autophagy, show at least one genetic difference from normal cells of said fragment, form 3-D tube-like structures or ball aggregates, or are inhibited in formation of 3-D structures and migration by treatment with chloroquine. | 03-29-2012 |
| 20120095044 | TISSUE NON-SPECIFIC ALKALINE PHOSPHATASE INHIBITORS AND USES THEREOF FOR TREATING VASCULAR CALCIFICATION - Disclosed herein are compounds that are tissue-nonspecific alkaline phosphatase inhibitors. The disclosed compounds are used to treat, prevent, or abate vascular calcification, arterial calcification and other cardiovascular diseases. | 04-19-2012 |
| 20120095045 | INJECTABLE ANTICANCER COMPOSITION FOR LOCAL ADMINISTRATION CONTAINING HYDROXYCHLOROQUINE - The present invention relates to an injectable anticancer composition for local administration comprising hydroxychloroquine. The anticancer composition shows an IC | 04-19-2012 |
| 20120108633 | INJECTABLE COMPOSITION CONTAINING HYDROXYCHLOROQUINE FOR LOCAL ADMINISTRATION FOR TREATING HEMORRHOIDS - The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant. | 05-03-2012 |
| 20120122923 | DUAL MOLECULES CONTAINING A PEROXIDE DERIVATIVE, THEIR SYNTHESIS AND THERAPEUTIC USES - The invention concerns dual molecules corresponding to formula (I): in which: A represents a molecular residue with antimalarial activity of formula (IIa) or (IIIa) or a residue facilitating bioavailability; B represents a cycloalkyl group potentially substituted, or B represents a bi- or tricyclic group capable of being substituted, or B represents 2 cycloalkyl groups linked together through either a single bond or an alkylene chain; m and n represent independently of one another 0, 1 or 2; R | 05-17-2012 |
| 20120136026 | 5-MEMBERED HETEROCYCLIC COMPOUND CYCLOPENTA[C]PYRROLYLALKYLCARBAMATE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The invention relates to compounds of the general formula (I) where: R | 05-31-2012 |
| 20120142731 | METHODS OF INHIBITING VIRAL INFECTION - Compounds, pharmaceutical compositions and methods of inhibiting viral infection in a mammal in need of same, are provided, which employ compounds of the formula | 06-07-2012 |
| 20120157493 | Antifungal and Antiparasitic Indoloquinoline Derivatives - “An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N—R | 06-21-2012 |
| 20120202849 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT/PROPHYLAXIS OF NON-ALCOHOLIC FATTY LIVER DISEASE - Disclosed herein is a novel synergistic pharmaceutical composition comprising hydroxychloroquine with insulin sensitizing agents and lipid lowering agents such as statins along with pharmaceutical excipients/carriers useful in treating Non-Alcoholic Fatty Liver Disease. | 08-09-2012 |
| 20120220627 | Substituted 2-amino-quinoline-3-carboxamides as KCNQ2/3 modulators - The invention relates to substituted 2-amino-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. | 08-30-2012 |
| 20120232110 | Antimicrobial Compounds - This disclosure relates to compositions including certain compounds identified by a quantitative, high throughput assay to be effective in inhibiting the ability of a bacterium to kill a host organism, as well as methods for using these compounds for treating bacterial infections. | 09-13-2012 |
| 20120289545 | Maleate Salts of (E)-N--4-(Dimethylamino)-2-Butenamide and Crystalline Forms Thereof - The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family. | 11-15-2012 |
| 20120302601 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF MACULAR DEGENERATION - The present invention is directed to topical ophthalmic compositions of a lipophilic compound and an oligomeric or polymeric carrier wherein the compositions are useful in the treatment and prevention of macular degeneration. The invention also includes methods of treating macular degeneration by using a topical ophthalmic composition of a lipophilic compound and an oligomeric or polymeric carrier. | 11-29-2012 |
| 20120329830 | Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of Use - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein ring A, B | 12-27-2012 |
| 20130035357 | Compositions and Methods for Preventing Joint Destruction in Osteoarthritis - The present invention is methods for inhibiting collagen destruction in joints of osteoarthritis patients. The methods are based on use of rexinoid compounds, in particular bexarotene, and their activity to inhibit synthesis of matrix metalloproteinases (MMPs) in affected tissue. | 02-07-2013 |
| 20130085159 | COMPOUNDS DERIVED FROM ARTESUNATE, PREPARATION PROCESS, PHARMACEUTICAL COMPOSITION AND USE OF THE RESPECTIVE MEDICINE - The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R | 04-04-2013 |
| 20130102632 | SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula (I): | 04-25-2013 |
| 20130131108 | METHODS OF TREATING OBSTRUCTIVE LUNG DISEASES USING BITTER TASTANTS - Described herein are methods for enhancing airway dilation and/or relieving bronchoconstriction, e.g., to treat obstructive lung diseases such as asthma and COPD, by administering bitter tastants to subjects in need thereof. Also described herein are methods for identifying compounds that modulate function of bitter tastant receptors. | 05-23-2013 |
| 20130210861 | METHODS AND COMPOSITIONS FOR MANAGING CARDIOVASCULAR DISEASE ASSOCIATED WITH CHRONIC KIDNEY DISEASE - Methods of treating cardiovascular disease in patients predisposed to or afflicted with kidney disease, particularly chronic kidney disease, are described. In such methods, therapeutically effective amounts of chloroquine-based compounds, for example, hydroxychloroquine, are administered to prevent or otherwise ameliorate arthrosclerosis and other cardiovascular diseases. | 08-15-2013 |
| 20130281488 | MALEATE SALTS OF (E)-N--4-(DIMETHYLAMINO)-2-BUTENAMIDE AND CRYSTALLINE FORMS THEREOF - The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family. | 10-24-2013 |
| 20130338190 | PHARMACEUTICALLY ACCEPTABLE SALT OF (E)-N-[4-[[3-CHLORO-4-(2-PYRIDYLMETHOXY)PHENYL]AMINO]-3-CYANO-7-ETHOXY-6-- QUINOLYL]-3-[(2R)-1-METHYLPYRROLIDIN-2-YL]PROP-2-ENAMIDE, PREPARATION METHOD THEREOF, AND MEDICAL USE THEREOF - Provided as represented by formula (I) is a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, a preparation method thereof, and a use thereof as a therapeutic agent, and especially as a protein kinase inhibitor. | 12-19-2013 |
| 20130345258 | AMINO-QUINOLINES AS KINASE INHIBITORS - Disclosed are compounds having the formula: | 12-26-2013 |
| 20140005222 | DIMETHYL-BENZOIC ACID COMPOUNDS | 01-02-2014 |
| 20140011837 | COMPOSITIONS AND METHODS FOR TREATING WARTS ASSOCIATED WITH VIRAL INFECTIONS - The invention provides compositions and methods for the treatment, as well as the inhibition and prevention, of an infection of the human papillomavirus and the epithelial lesions, namely, the warts of the skin and mucosal surfaces, associated therewith. The compositions comprise a therapeutically effective amount of an active ingredient comprising a compound selected from the group consisting of chloroquine, hydroxychloroquine, chloroquine combined with amodiaquine, and hydroxychloroquine combined with amodiaquine, or in each case, a pharmaceutically acceptable salt thereof. The methods comprise topically administering a therapeutically and/or antivirally effective amount of such a compound to a human being in need of such treatment, although in certain of the compounds may alternatively be administered subcutaneously or transdermally. The compositions may optionally also comprise one or more pharmaceutically acceptable non-active ingredients. | 01-09-2014 |
| 20140011838 | COMPOSITIONS AND METHODS FOR TREATING WARTS ASSOCIATED WITH VIRAL INFECTIONS - The invention provides compositions and methods for the treatment, as well as the inhibition and prevention, of an infection of the human papillomavirus and the epithelial lesions, namely, the warts of the skin and mucosal surfaces, associated therewith. The compositions comprise a therapeutically effective amount of an active ingredient comprising at least one compound selected from the group consisting of chloroquine, hydroxychloroquine, amodiaquine, or in each case, a pharmaceutically acceptable salt thereof. The methods comprise topically administering a therapeutically and/or antivirally effective amount of such a compound to a human being in need of such treatment, although in certain of the compounds may alternatively be administered subcutaneously or transdermally. The compositions may optionally also comprise one or more pharmaceutically acceptable non-active ingredients. | 01-09-2014 |
| 20140011839 | COMPOSITIONS AND METHODS FOR TREATING AND INHIBITING VIRAL INFECTIONS - Compositions and methods for the treatment, as well as the inhibition and prevention, of an infection of the papillomavirus and the epithelial lesions, namely, the warts of the skin and mucosal surfaces, associated therewith, in a mammalian host, as well as methods of inhibiting the replication of a papillomavirus in an infected cell, are provided. The compositions comprise a therapeutically effective amount of an active ingredient comprising at least one compound selected from the group consisting of chloroquine, hydroxychloroquine, amodiaquine, or in each case, a pharmaceutically acceptable salt thereof. The methods comprise topically administering a therapeutically and/or antivirally effective amount of such a compound to a mammalian host, such as a human being, in need of such treatment, although alternatively other routes of administration may be used, including but not limited to transdermal, transmucosal, respiratory, and by injection. The compositions optionally also comprise one or more pharmaceutically acceptable non-active ingredients. | 01-09-2014 |
| 20140018388 | QUINOLINE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS - A compound of formula | 01-16-2014 |
| 20140039006 | Tetrahydroquinoline Derivatives Useful As Bromodomain Inhibitors - Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy. | 02-06-2014 |
| 20140088143 | Method of Inhibiting Constitutively Active Phosphorylated FLT3 Kinase - The present invention includes a method of inhibiting or reducing deregulated FLT3 tyrosine kinase activity or FLT3 tyrosine kinase expression in a subject with a proliferative disease by administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound of Formula I: | 03-27-2014 |
| 20140107155 | SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula (I): | 04-17-2014 |
| 20140107156 | Novel Amino Azaheterocyclic Carboxamides - The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 04-17-2014 |
| 20140155432 | ACTIVATORS AND THERAPEUTIC APPLICATIONS THEREOF - The invention presents methods of identifying small molecule compounds that are activators of tumor suppressor protein p53 pathway, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways and DNA damage response pathways with the small molecules. | 06-05-2014 |
| 20140194464 | Crenolanib for Treating FLT3 Mutated Proliferative Disorders - The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition: | 07-10-2014 |
| 20140235671 | SCRIPTAID ISOSTERES AND THEIR USE IN THERAPY - Compounds of the invention are of the formula | 08-21-2014 |
| 20140275164 | DESETHYLHYDROXYCHLOROQUINE FOR THE TREATMENT OF DISEASES ASSOCIATED WITH INFLAMMATION - Compositions and methods are provided for inhibiting or treating the early and established stages of inflammatory diseases by administration of an effective dose of the desethylhydroxychloroquine (DHCQ). A benefit of the methods is the ability to deliver a dose of agent that is effective in treating inflammation while sparing the individual from retinal toxicity. | 09-18-2014 |
| 20140288120 | COMPOUNDS USEFUL FOR TREATING AIDS - A compound having the following formula or a pharmaceutically acceptable salt thereof: | 09-25-2014 |
| 20140303206 | 3-Pyridyl Carboxamide-Containing Spleen Tyrosine Kinase (SYK) Inhibitors - The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. | 10-09-2014 |
| 20140309257 | TOPOISOMERASE INHIBITORS AND METHODS OF MAKING AND USE AS THERAPEUTIC AGENTS - The invention provides methods of inhibiting the growth or metastasis of cancer in a mammal by inhibiting TopoIIa in the mammal. The invention also provides small molecule inhibitors of TopoIIa useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds and methods of using the same. | 10-16-2014 |
| 20140329856 | METHOD OF TREATING PAIN - The instant application discloses methods of treating, reducing, or preventing pain in a mammal, which may include administering a compound capable of modulating a transient receptor potential channel. In one aspect, the TRP channel may be TRPC4. Types of pain contemplated by the present disclosure include acute, chronic, neuropathic, and nociceptive pain. | 11-06-2014 |
| 20140350048 | COMPOUNDS, COMPOSITIONS AND ASSOCIATED METHODS COMPRISING 3-ARYL QUINOLINES - Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed. | 11-27-2014 |
| 20150031723 | Quinoline Compounds Which Are Anti-Angiogenic Integrin Alpha5 Beta1 Inhibitors for Use in the Treatment of Fibrosis or Fibrosis-Related Diseases - A new medical therapy, and more particularly certain quinoline compounds which are anti-angiogenic integrin aplha5beta1 inhibitors, for use in the treatment of fibrosis, or a fibrosis-related disease, such as a fibrotic disease affecting the lung, liver, kidney, skin, epidermis, endodermis, muscle, tendon, cartilage, heart, stomach, large intestine, small intestine, colon, uterus, nervous system, testis, adrenal gland, artery, vein, biliary tract, or eye. | 01-29-2015 |
| 20150038531 | USE OF A NOVEL AMINOPYRIDINE DERIVATIVE TO PREVENT OR TREAT CANCER - An aminopyridine derivative of Formula 1 and a method of preventing or treating cancer using the same. Formula 1: | 02-05-2015 |
| 20150051245 | KINASE PROTEIN BINDING INHIBITORS - The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer. | 02-19-2015 |
| 20150057312 | SUBSTITUTED QUINOLINES AS BRUTON'S TYROSINE KINASES INHIBITORS - The present invention is directed to novel quinolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions. The disclosed substituted quinolines include Bruton's tyrosine kinase (Btk) inhibitors. | 02-26-2015 |
| 20150073017 | AZA-ARYL 1H-PYRAZOL-1-YL BENZENE SULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists. | 03-12-2015 |
| 20150094333 | AMINO-QUINOLINES AS KINASE INHIBITORS - Disclosed are compounds having the formula: | 04-02-2015 |
| 20150094334 | 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 | 04-02-2015 |
| 20150119421 | METHOD OF INHIBITING FLT3 KINASE - The present invention includes a method of inhibiting or reducing deregulated FLT3 tyrosine kinase activity or FLT3 tyrosine kinase expression in a subject with a proliferative disease by administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound (CP-673,451) of Formula I: | 04-30-2015 |
| 20150126550 | PHARMACEUTICAL USES OF 6-AMINO QUINAZOLINE OR 3-CYANO QUINOLINE DERIVATIVES - Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivatives are disclosed. Specifically, the 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, are protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification. | 05-07-2015 |
| 20150335632 | TOXIC ALDEHYDE RELATED DISEASES AND TREATMENT - The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE. | 11-26-2015 |
| 20150335633 | INHIBITION OF CHOROIDAL NEOVASCULARIZATION - Methods of treatment of diseases that include or are characterized by inappropriate or pathological neovascularization are disclosed. These diseases include diseases of the eye, such as diabetic retinopathy, retinopathy of prematurity, and choroidal neovascularization which can occur in age-related macular degeneration (AMD). Disclosed methods include administering agents that cause directly or indirectly upregulation of the ABCA1 transporter protein in macrophages. These agents include, without limitation, LXR agonists. In some embodiments, inhibitors of CETP expression or activity can also be effective. Administration routes can include, without limitation, intraocular, periocular, or systemic administration. | 11-26-2015 |
| 20150335635 | 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 | 11-26-2015 |
| 20160058749 | TREATMENTS FOR NEUROPATHY - Small fiber neuropathy is treated or prevented by topically administering to a subject in need thereof topically active quinoline compounds or pharmaceutically acceptable salts thereof under conditions effective to treat or prevent neuropathy in the subject. Glial cell-derived neurotrophic factor (GDNF) receptors are modulated with the subject active quinoline compounds, which may be formulated in topical lotions. | 03-03-2016 |
| 20160068511 | MALEATE SALTS OF (E)-N--4-(DIMETHYLAMINO)-2-BUTENAMIDE AND CRYSTALLINE FORMS THEREOF - The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family. | 03-10-2016 |
| 20160074379 | Antimicrobial Compounds - This disclosure relates to compositions including certain compounds identified by a quantitative, high throughput assay to be effective in inhibiting the ability of a bacterium to kill a host organism, as well as methods for using these compounds for treating bacterial infections. | 03-17-2016 |
| 20160083350 | A NK3 RECEPTOR ANTAGONIST COMPOUND (NK3RA) FOR USE IN A METHOD FOR THE TREATMENT OF POLYCYSTIC OVARY SYNDROME (PCOS) - A method for treating polycystic ovarian syndrome and related conditions with a compound (I): or a pharmaceutically acceptable salt thereof. | 03-24-2016 |
| 20160096806 | 2-Aminoquinoline-Based Compounds for Potent and Selective Neuronal Nitric Oxide Synthase Inhibition - Various 2-aminoquinoline compounds as can be used, in vivo or in vitro, for selective inhibition of neuronal nitric oxide synthase. | 04-07-2016 |
| 20160113920 | COMPOSITIONS AND METHODS FOR INHIBITING BACTERIAL AND VIRAL PATHOGENS - Compositions and methods including Amodiaquine (AQ) or N-Desethy Amodiaquine (DEAQ) are provided for treating, inhibiting, or preventing cathepsin B dependent pathogens and toxins in a host cell or infected subject. Compositions and methods also include AQ or DEAQ in combination with an antibiotic for more effective clearance of the pathogen and/or toxins. | 04-28-2016 |
| 20160151347 | PHARMACEUTICAL COMPOUNDS | 06-02-2016 |
| 20160168098 | COMPOSITIONS AND METHODS OF TREATING RETINAL DISEASE | 06-16-2016 |
| 20190144416 | INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE | 05-16-2019 |
