| Entries |
| Document | Title | Date |
|---|
| 20080214523 | Method for treating severe heart failure and medicament therefor - A method for treating severe heart failure, comprising administering to a patient an effective amount of a benzazepine compound (1): wherein R | 09-04-2008 |
| 20080221083 | Heterobicyclic metalloprotease inhibitors - The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors. | 09-11-2008 |
| 20080234251 | 8-Substituted Benzoazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency. | 09-25-2008 |
| 20080255091 | COMPOUNDS TO TREAT AMYLOIDOSIS AND PREVENT DEATH OF BETA-CELLS IN TYPE 2 DIABETES MELLITUS - The invention discloses aromatic amides and sulfonates to treat or prevent type 2 diabetes mellitus (T2DM), the pathological consequences of T2DM, to inhibit amyloidosis or to prevent death of β-cells of the pancreas. | 10-16-2008 |
| 20080280882 | Novel Substituted Diazabicyclo Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors - This invention relates to novel substituted diazabicyclo derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 11-13-2008 |
| 20080300235 | FXR Agonists for Reducing LOX-1 Expression - Provided are certain methods of treating at least one disease state characterized by elevated expression of the Lectin-like Oxidized Low-density Lipoprotein Receptor 1 (LOX-1) in a patient with farnesoid X receptor agonists. Also provided are certain methods of reducing expression of LOX-1 in a cell with farnesoid X receptor agonists. | 12-04-2008 |
| 20080306045 | 1-Benzazepine-3-Sulfonylamino-2-Pyrroridones as Factor Xa Inhibitors - The invention relates to chemical entities of formula (I): | 12-11-2008 |
| 20090036426 | CB1 antagonists and inverse agonists - The present invention relates to methods of treating obesity, anorexia nervosa, or bulimia nervosa comprising administering a compound of the invention conjointly with zonisamide, naltrexone, or a pharmaceutically acceptable salt thereof. The present invention further relates to the treatment of metabolic syndrome comprising administering a compound of the invention conjointly with zonisamide, naltrexone, or a pharmaceutically acceptable salt thereof. | 02-05-2009 |
| 20090042860 | Compounds for the Treatment of Hepatitis C - The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. | 02-12-2009 |
| 20090054402 | 7-SUBSTITUTED INDOLE MCL-1 INHIBITORS - Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed. | 02-26-2009 |
| 20090075978 | SUBSTITUTED PROPIOLIC ACID AMIDES AND THEIR USE FOR PRODUCING DRUGS - The present invention relates to substituted propiolic acid amides, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments. | 03-19-2009 |
| 20090088417 | VANILLOID RECEPTOR ANTAGONIST FOR PREVENTION AND TREATMENT OF DRUG DEPENDENCE AND ADDICTION - Disclosed is a composition for preventing and treating harmful actions caused by drugs of abuse. More particularly, disclosed is a pharmaceutical composition effective for preventing or treating dependence and spontaneous movements by using a drug acting against the vanilloid receptor Capsazepine, which is used as a drug acting against the vanilloid receptor, shows an excellent effect of alleviating conditions of cocaine dependence and addition during the development and recurrence thereof. Administration of the drug acting against the vanilloid receptor provides important information in developing an agent for preventing and treating drug dependence and addiction. | 04-02-2009 |
| 20090149444 | Benzylamine analogues - A compound of the formula (I): | 06-11-2009 |
| 20090163474 | FXR Agonists for the Treatment of Nonalcoholic Fatty Liver and Cholesterol Gallstone Diseases - Provided are certain methods of treating nonalcoholic fatty liver disease with farnesoid X receptor agonists. Also provided are certain methods of modulating levels of keratinocyte-derived chemokine (KC), alanine aminotransferase (ALT), aspartate aminotransferase (AST), cytokeratin 18 (CK-18), matrix metalloproteinase-9 (MMP-9), matrix metalloproteinase-14 (MMP-14), tissue inhibitor of metalloproteinase 1 (TIMP-1), and Cytochrome P450 2E1 (CYP2E1); certain methods of identifying FXR modulators; and certain methods of treating patients with existing cholesterol gallstone disease. | 06-25-2009 |
| 20090192141 | METHODS OF USE OF INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids. | 07-30-2009 |
| 20090325930 | SELECTIVE ESTROGEN RECEPTOR MODULATOR - The present invention provides a compound represented by the following formula (I); | 12-31-2009 |
| 20100022514 | Heterocycle Compounds and Methods of Use Thereof - The invention relates to the use of compounds in the treatment of deacetylase-associated diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases. | 01-28-2010 |
| 20100022515 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising compound of following formula (I), and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119 (G protein-coupled receptor 119) such as obesity, diabetes and hyperlipidemia. | 01-28-2010 |
| 20100048536 | Novel Substituted Diaryl Azepine Derivatives as Integrin Ligands - The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the α | 02-25-2010 |
| 20100099663 | 4-TRIFLUOROMETHOXYPHENOXYBENZOL-4'-SULFONIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF IN MEDICAMENTS - The present invention is directed to a compound of formula I, | 04-22-2010 |
| 20100184741 | GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R | 07-22-2010 |
| 20100210624 | ARYLOXY- AND HETEROARYLOXY-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN - The aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepine derivative compounds of the present invention are represented by formulae (I) (A-E) having the following structure where the carbon atom designated * is in the R or S configuration and the substituents X and R | 08-19-2010 |
| 20100249104 | METHODS FOR USING VASOPRESSIN ANTAGONISTS WITH ANTHRACYCLINE CHEMOTHERAPY AGENTS TO REDUCE CARDIOTOXICITY AND/OR IMPROVE SURVIVAL - The present invention relates to methods of reducing cardiotoxicity and/or improving survival from treatment with anthracycline agents comprising administering a therapeutically effective amount of a composition comprising a vasopressin antagonist compound or a pharmaceutically acceptable salt thereof as an active ingredient, administered simultaneously or prior to the anthracycline administration. | 09-30-2010 |
| 20100305100 | METHODS FOR TREATING HEPATITIS C - The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity. | 12-02-2010 |
| 20100311721 | COMPOUNDS - The present invention encompasses compounds of general formula (1) | 12-09-2010 |
| 20100331309 | Trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tet- razol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]met- hyl]-cyclohexanecarboxylic acid - Compounds of a formula | 12-30-2010 |
| 20110003795 | Substituted Aromatic Carboxamide and Urea Derivatives as Vanilloid Receptor Ligands - The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions. | 01-06-2011 |
| 20110021501 | SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES - The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, | 01-27-2011 |
| 20110046114 | ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN - The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): | 02-24-2011 |
| 20110092485 | SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 04-21-2011 |
| 20110112071 | NOVEL HETEROCYCLIDENE ACETAMIDE DERIVATIVE - A compound represented by formula (I′): | 05-12-2011 |
| 20110118235 | SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 05-19-2011 |
| 20110319385 | QUINOXALINE COMPOUND | 12-29-2011 |
| 20120058990 | Trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl] (2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-be- nzazepin-1-yl]methyl]-cyclohexanecarboxylic acid - Abstract Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof, hydrate, and hydrate in crystalline form; pharmaceutical formulations; and methods of use are disclosed. | 03-08-2012 |
| 20120165316 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 06-28-2012 |
| 20120165317 | 8-SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency. | 06-28-2012 |
| 20120232059 | 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. | 09-13-2012 |
| 20120238551 | Substituted Phenoxypropylcycloamine Derivatives as Histamine-3 (H3) Receptor Ligands - The present invention provides compounds of formula I: | 09-20-2012 |
| 20120309744 | DOSING REGIMENS AND METHODS FOR TREATING OR PREVENTING HEPATOCELLULAR CARCINOMA - The invention encompasses dosing regimens in which a subject is administered menatetrenone over a period of time to establish initial therapeutic baseline blood concentration of the menatetrenone followed by a maintenance therapy to maintain therapeutic blood concentrations. In other embodiments, the invention encompasses methods of treating hepatocellular adenocarcinoma in a subject in need thereof comprising administering to a subject a therapeutically effective dosing regimen of menatetrenone. | 12-06-2012 |
| 20130035327 | Modulators of ATP-Binding Cassette Transporters - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 02-07-2013 |
| 20130102588 | TOLVAPTAN SOLID DISPERSION AND ITS PREPARATION METHOD - A tolvaptan solid dispersion and its preparation method are disclosed. The solid dispersion comprises tolvaptan and cross-linked polyvinylprrolidone at a weight ratio of 1:0.05-20, preferably 1:0.1-10, and more preferably 2:1. The solid dispersion can further comprise one or more water-soluble polymers, such as polyvinylprrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose or methylcellulose, wherein the weight ratio of tolvaptan:the crosslinked polyvinylprrolidone:the water-soluble polymers is preferably 2:1:0.1. The solid dispersion exhibits good thermodynamic stability and solubility. The pharmaceutical composition thereof has improved release rate and bioavailability. | 04-25-2013 |
| 20130131045 | BENZAZEPINE COMPOUND - An object of the present invention is to provide a novel benzazepine compound or a salt thereof, which has excellent vasopressin antagonistic activity. | 05-23-2013 |
| 20130203736 | AGONIST/ANTAGONIST COMPOSITIONS AND METHODS OF USE - The present invention relates to novel compositions comprising an agonist and an antagonist, in certain ratios which allow for the onset of agonist action followed quickly by alleviation by antagonist action, and methods of use in personal defense and law enforcement. | 08-08-2013 |
| 20130274246 | Therapeutic Treatment for Metabolic Syndrome, Type 2 Diabetes, Obesity, or Prediabetes - The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic and/or serotonin neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient. | 10-17-2013 |
| 20140024640 | Benzazepine Derivatives Useful as Vasopressin Antagonists - The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) | 01-23-2014 |
| 20140031341 | MODULATORS AND METHODS FOR THE TREATMENT OF ROSACEA - An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology. | 01-30-2014 |
| 20140031342 | 6,7-DIHYDROIMIDAZO [2,1-b] [1,3]OXAZINE BACTERICIDES - The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): | 01-30-2014 |
| 20140051683 | 7-SUBSTITUTED INDOLE MCL-1 INHIBITORS - Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed. | 02-20-2014 |
| 20140142086 | Substituted Benzoazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 05-22-2014 |
| 20140163011 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 06-12-2014 |
| 20140364418 | COMPOSITIONS COMPRISING AN AROMATIC ALCOHOL AND A TRPV-1 ANTAGONIST, AND USES THEREOF - A topical composition providing reduced irritation that contains aromatic alcohols such as phenoxyethanol and a TRPV-1 antagonist is described. The composition is substantially free of parabens. The composition may be used for example for cleansing the skin. | 12-11-2014 |
| 20150065486 | METHODS FOR TREATING POLYCYSTIC KIDNEY DISEASE - Methods for treating autosomal dominant polycystic kidney disease (ADPKD) are described herein. More particularly, methods described herein relate generally to administering glutaminase1 inhibitors to subjects afflicted with ADPKD. Accordingly, the use and application of compounds or agents that inhibit glutaminase1 for treating ADPKD or for use in a medicament for treating ADPKD are encompassed herein. | 03-05-2015 |
| 20150065487 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 03-05-2015 |
| 20150299225 | COMPOUNDS FOR MODULATING TRPV3 FUNCTION - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 10-22-2015 |
| 20150315186 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 11-05-2015 |
| 20150352123 | USE OF CAPSAZEPINE AND ANALOGS THEREOF TO TREAT CANCER - Disclosed are methods and compositions for treating cancer, particularly for reducing cancerous cell growth, for example, in solid tumors. Disclosed methods and compositions include capsazepine (CPZ) or an analog of CPZ. Compositions comprising CPZ or an analog of CPZ may be useful for simultaneously treating cancer and alleviating pain by blocking TRPV1 channels. | 12-10-2015 |
| 20160000800 | MODULATORS AND METHODS FOR THE TREATMENT OF ROSACEA - An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology. | 01-07-2016 |
| 20160000801 | SUSPENSION FOR ORAL ADMINISTRATION COMPRISING AMORPHOUS TOLVAPTAN - This invention provides a suspension for oral administration comprising particles containing amorphous tolvaptan that can inhibit or delay crystallization of amorphous tolvaptan over time in the suspension, and stably maintain high solubility of tolvaptan and excellent absorbability of tolvaptan from the gastrointestinal tract; and a solid formulation for oral administration that can be suspended to prepare the suspension for oral administration at the time of use. | 01-07-2016 |
| 20160129010 | Substituted Benzoazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-versus-host disease. | 05-12-2016 |
| 20160130215 | CYCLOPROPANEAMINE COMPOUND - The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula | 05-12-2016 |
| 20160137608 | SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 05-19-2016 |
| 20160158207 | THERAPEUTIC COMPOUNDS AND USES THEREOF - The present invention relates to compounds of formula (I) or formula (II): | 06-09-2016 |
| 20160159774 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 06-09-2016 |
| 20190144450 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS | 05-16-2019 |
