Class / Patent application number | Description | Number of patent applications / Date published |
514310000 | Nitrogen, other than as nitro or nitroso, attached directly to the isoquinoline ring system by nonionic bonding | 39 |
20090069371 | ISOQUINOLINE COMPOUNDS - Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline 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, osteoporosis and glaucoma are also provided. | 03-12-2009 |
20090118327 | SUBSTITUTED 1-AMINO-4-PHENYL-DIHYDROISOQUINOLINES, METHODS FOR THE PRODUCTION THEREOF, USE THEREOF AS A MEDICAMENT, AND MEDICAMENTS CONTAINING THEM - The present invention relates to compounds useful in the prevention or treatment of various disorders such as acute or chronic renal failure, for impairments of biliary function, for respiratory impairments such as snoring or sleep apneas or for stroke, and pharmaceutical compositions comprising them. More specifically, the compounds of the present invention comprises substituted 1-amino-4-phenyl-dihydroisoquinolines and their derivatives of formula I: | 05-07-2009 |
20090186917 | 6-And 7-amino isoquinoline compounds and methods for making and using the same - 6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-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. | 07-23-2009 |
20090192189 | TREATMENT OF CANCERS EXPRESSING P95 ERBB2 - The truncated ErbB2 receptor (p95 | 07-30-2009 |
20090281139 | MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS - The present invention relates generally to novel macrocycles of Formula (I): | 11-12-2009 |
20090306131 | CELL LINES WITH LATENT IMMUNODEFICIENCY VIRUS AND METHODS OF USE THEREOF - The present invention provides isolated cells that comprise, integrated into the genome of the cell, a transcription-competent immunodeficiency virus or a transcription-competent immunodeficiency virus-based retroviral vector. Under basal in vitro culture conditions, the immunodeficiency virus is latent, and the expression of the latent immunodeficiency virus can be reactivated. The invention farther provides methods of making a subject cell. The invention further provides screening methods for identifying agents that activate a latent immunodeficiency virus; and screening method for identifying agents that block reactivation of latent immunodeficiency virus expression in response to T cell activation signals. The invention further provides agents identified in the subject screening assays. The invention further provides methods of treating an immunodeficiency virus infection. | 12-10-2009 |
20100041696 | Compounds - The present invention relates to substituted 4-Aminopyrazole compounds of the formula (I): | 02-18-2010 |
20100048619 | Cold Menthol Receptor Antagonists - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 02-25-2010 |
20100093790 | ISOQUINOLINE COMPOUNDS - Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline 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, osteoporosis and glaucoma are also provided. | 04-15-2010 |
20100105726 | IMIDAZOLE DERIVATIVES THAT INDUCE APOPTOSIS AND THEIR THERAPEUTIC USES - The present invention relates to a pharmaceutical composition comprising compound for induction of apoptosis, a method for inducing cancer cell apoptosis, a method to suppress lymphocyte activation, a method to improve intracellular trafficking of misfolded mutants and a screening method to identify additional compounds useful for inducing apoptosis, and more specifically, it relates to pharmaceutical compositions comprising imidazole derivatives as active gradients for induction of apoptosis to treat various diseases including cancers and immune-related diseases, the method of inducing apoptosis by treating cancer cells with the said pharmaceutical composition, the method of inactivating human lymphocytes by treating lymphocytes with the said pharmaceutical composition, the method of improving intracellular trafficking of misfolded mutants by treating cells containing the mutants with the said pharmaceutical composition, and the screening method for identifying additional compound useful for inducing apoptosis, wherein cells are incubated with the said pharmaceutical composition and detected. | 04-29-2010 |
20100120846 | TRPV1 ANTAGONISTS - Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, | 05-13-2010 |
20100137360 | TRPV1 ANTAGONISTS - Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, | 06-03-2010 |
20100305153 | AMINOISOQUINOLINE THROMBIN INHIBITOR WITH IMPROVED BIOAVAILABILITY - The invention relates to the compound N-(2-oxo-2-propoxyethyl)-β-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases. | 12-02-2010 |
20100324086 | COMPOUNDS AND METHODS - A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder from pain, fever, inflammation and cancer. | 12-23-2010 |
20110009447 | Substituted Benzoic Acid Amides and Use thereof for the Inhibition of Angiogenesis - Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described. | 01-13-2011 |
20110092540 | SUBSTITUTED N-PHENYL-2,3-DIHYDROIMIDAZO[2,1-B]THIAZOLE-5-SULFONAMIDE DERIVATIVES AS 5-HT6 LIGANDS - The invention relates to compounds having pharmacological activity towards the 5-HT | 04-21-2011 |
20110124680 | NOVEL ANTHRANILAMIDE PYRIDINUREAS AS VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) RECEPTOR KINASE INHIBITORS - The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis. | 05-26-2011 |
20110136860 | Compounds - A compound of formula (I): | 06-09-2011 |
20120004261 | MIF MODULATORS - The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression. | 01-05-2012 |
20120029012 | 5, 6, or 7-SUBSTITUTED -3-(HETERO) ARYLISOQUINOLINAMINE DERIVATIVES AND THERAPEUTIC USE THEREOF - The present invention relates to 5, 6, or 7-substituted-3-(hetero)arylisoquinolinamine derivatives represented by general formula D, their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included. | 02-02-2012 |
20120065228 | COMPOSITIONS AND METHODS FOR TREATING, CONTROLLING, REDUCING, OR AMELIORATING OCULAR INFLAMMATORY WITH LOWER RISK OF INCREASED INTRAOCULAR PRESSURE - 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 ocular inflammation and/or pain such that it has lower risk of eliciting increased intraocular pressure seen with glucocorticoids. | 03-15-2012 |
20120202847 | Novel Tetrahydroisoquinoline Compounds - The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect and feeding suppressant effect. The present invention provides trans-6-[3-(2,4-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2-chloro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2,3-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2,5-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2,6-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, or the like, or a pharmacologically acceptable salt thereof. | 08-09-2012 |
20120252839 | GAIN-OF-FUNCTION BCL-2 INHIBITORS - Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-x | 10-04-2012 |
20130109716 | N-AMINOTETRAHYDROISOQUINOLINES AS ANTI-CANCER AGENTS | 05-02-2013 |
20130131106 | BIFUNCTIONAL RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE - This invention relates to synthetic bifunctional compounds comprising a first rho-associated kinase (ROCK) inhibiting compound and a second pharmaceutically active compound with complementary activity; the first and the second compounds are covalently linked by a biologically labile bond. This invention also relates to methods of making such compounds. The invention also relates to methods of using such bifunctional compounds in the prevention or treatment of diseases or conditions that are affected or can be assisted by altering the integrity or rearrangement of the cytoskeleton. Particularly, this invention relates to methods of treating ophthalmic diseases such as disorders in which intraocular pressure is elevated, for example primary open-angle glaucoma, using the bifunctional compounds. | 05-23-2013 |
20130274287 | PHENYL-TETRAHYDROISOQUINOLINE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 10-17-2013 |
20130296364 | MODULATORS OF ATP-BINDING CASSETTE-TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 11-07-2013 |
20140057942 | NOVEL ROCK INHIBITORS - The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, —NH—, or a direct bond; Y is —NH— or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of: Formula (II), Ar is selected from the group comprising: Formula (III), R | 02-27-2014 |
20140128428 | COLD MENTHOL RECEPTOR ANTAGONISTS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 05-08-2014 |
20140179735 | TYROSINE PHOSPHATASE INHIBITORS AND USES THEREOF TO MODULATE THE ACTIVITY OF ENZYMESp INVOLVED IN THE PATHOLOGY OF MYCOBACTERIUM TUBERCULOSIS - A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of | 06-26-2014 |
20140343095 | Methods of Diagnosing and Treating Multiple Sclerosis - Methods of using a 15-oxysterol, e.g., 15-ketocholestene (15-KE), 15-ketocholestane (15-KA), and/or 15-hydroxy-cholestene (15-HC), as a biomarker to monitor disease progression in multiple sclerosis (MS), and methods of treating secondary progressive MS (SPMS) using inhibitors of poly(ADP ribose) polymerase-1 (PARD-1). | 11-20-2014 |
20150119418 | BICYCLIC COMPOUND - Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: | 04-30-2015 |
20150119419 | 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. | 04-30-2015 |
20150299173 | NOVEL ROCK INHIBTORS - The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors. | 10-22-2015 |
20150344432 | PERI-CARBINOLS - The present invention is directed to compounds of formula(I): | 12-03-2015 |
20160039765 | INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND APO-B SECRETION - The present invention relates to compounds which are inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion. These compounds can be useful for the prevention and treatment of various diseases, particularly atherosclerosis and its clinical sequelae, for lowering serum lipids, and related ailments. The invention further relates to pharmaceutical compositions comprising the compounds and to methods of treating diseases, such as hypertriglyceridemia, hyperchylomicronemia, atherosclerosis, obesity, and related conditions using the compounds. A method for decreasing apolipoprotein B (apo B) secretion is also provided. | 02-11-2016 |
20160052870 | 3-AMIDOBENZAMIDES AND USES THEREOF FOR INCREASING CELLULAR LEVELS OF A3G AND OTHER A3 FAMILY MEMBERS - Disclosed are novel benzamide compounds and the uses thereof for treating diseases and disorders in a patient in need thereof by increasing cellular levels of A3G and/or other members of the A3 family of proteins in the patient. The disclosed compounds include | 02-25-2016 |
20160115159 | MACROCYCLIC FACTOR VIIA INHIBITORS - The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments. | 04-28-2016 |
20190142821 | COMPOSITIONS FOR TREATING OR PREVENTING VASOMOTOR SYMPTOMS | 05-16-2019 |