Class / Patent application number | Description | Number of patent applications / Date published |
514212080 | Additional hetero ring attached directly or indirectly by nonionic bonding to the seven-membered hetero ring | 56 |
20080275025 | Substituted Lactams and Their Use as Anti-Cancer Agents - This invention relates to certain substituted lactam compounds, particularly caprolactam compounds, which are useful for the treatment of cancer. | 11-06-2008 |
20080293692 | SUCCINOYLAMINO LACTAMS AS INHIBITORS OF A-BETA PROTEIN PRODUCTION - This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome. | 11-27-2008 |
20080318928 | BENGAMIDES WITH A SUBSTITUTED CAPROLACTAM CYCLE, METHOD FOR THE PREPARATION THEREOF, COMPOSITIONS CONTAINING THEM AND USE THEREOF - The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as anticancer agents. | 12-25-2008 |
20090029968 | QUINAZOLINE DERIVATIVES USED AS INHIBITORS OF ERBB TYROSINE KINASE - A quinazoline derivative of the Formula I: | 01-29-2009 |
20090075977 | DEUTERIUM-ENRICHED MK0974 - The present application describes deuterium-enriched MK-0974, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090149443 | P38 INHIBITORS AND METHODS OF USE THEREOF - Compounds of formula (I): in which A, B, X, Ar | 06-11-2009 |
20090176758 | LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS - The present application describes lactam-containing compounds and derivatives thereof of Formula I: | 07-09-2009 |
20090215746 | SUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINES AS CALCIUM RECEPTOR MODULATING AGENTS - There is provided a calcium receptor modulator comprising a compound of the formula (I): | 08-27-2009 |
20090258857 | CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1) wherein R | 10-15-2009 |
20100009967 | SOLID DOSAGE FORMULATIONS OF TELCAGEPANT POTASSIUM - A solid dosage pharmaceutical formulation comprising as an active ingredient the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide (telcagepant), arginine, and a pharmaceutically acceptable surfactant. The invention is also directed to an amorphous form of the potassium salt of telcagepant. | 01-14-2010 |
20100029615 | BENZIMIDAZOLE DERIVATIVES - The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 02-04-2010 |
20100179127 | PYRIMIDINE DERIVATIVES - The invention relates to novel heterocyclic compounds of the formula | 07-15-2010 |
20100190774 | INHIBITORS OF C-MET AND USES THEREOF - The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders. | 07-29-2010 |
20100280006 | 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling - Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R. | 11-04-2010 |
20100286122 | CGRP Antagonist Salt - An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- | 11-11-2010 |
20100298295 | 2-BIPHENYLAMINO-4-AMINOPYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or anaplastic lymphoma kinase (ALK). | 11-25-2010 |
20110003794 | Naphthyridine Integrase Inhibitors - The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 01-06-2011 |
20110009387 | HISTONE H2AX (HH2AX) BIOMARKER FOR FTI SENSITIVITY - The present invention relates e.g., to methods for predicting cellular sensitivity to farnesyl protein transferase inhibitors, such as lonafarnib; manumycin A; FTI-276; L-744832; BMS-214662; tipifarnib; BMS-316810K. The methods involve determining if malignant cells exhibit increased expression. of phosphorylated histone H2Ax following contact of one or more of said cells with said inhibitor. | 01-13-2011 |
20110034439 | ACYLTHIOUREA COMPOUND OR SALT THEREOF, AND USE THEREOF - To provide an antitumor agent which exhibits excellent c-Met inhibitory effect and mitigates side effects by virtue of selectively affecting to tumor cells in which c-Met is specifically expressed. | 02-10-2011 |
20110053912 | PYRIMIDINE COMPOUND - A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like. | 03-03-2011 |
20110065682 | HETEROCYCLIC COMPOUNDS AS FACTOR IXA INHIBITORS - The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder. | 03-17-2011 |
20110218187 | INHIBITORS OF TYROSINE KINASES - The invention relates to compounds of formula | 09-08-2011 |
20110218188 | SUBSTITUTED (PYRIDYL)-AZINYLAMINE DERIVATIVES AS FUNGICIDES - The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q | 09-08-2011 |
20110230467 | 4,6-DIAMINONICOTINAMIDE COMPOUND - [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. | 09-22-2011 |
20110230468 | FUSED HETEROCYCLIC COMPOUNDS AND USES THEREOF - Fused heterocylic compounds of the following Formula | 09-22-2011 |
20110306599 | INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF - Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. | 12-15-2011 |
20120028959 | DIHYDROOROTATE DEHYDROGENASE INHIBITORS - The invention relates to compounds of formula (I) wherein R | 02-02-2012 |
20120040964 | N-SUBSTITUTED PIPERIDINES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 02-16-2012 |
20120142671 | BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma. | 06-07-2012 |
20120208794 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-16-2012 |
20120214795 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-23-2012 |
20120220569 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-30-2012 |
20120220570 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-30-2012 |
20120225861 | 6-O-Substituted Benzoxazole and Benzothiazole Compounds and Methods of Inhibiting CSF-1R Signaling - Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R. | 09-06-2012 |
20120238550 | COMPOUND - There is provided a compound of formula I | 09-20-2012 |
20120277213 | ETHYNYL COMPOUNDS - The present invention relates to ethynyl derivatives of formula I | 11-01-2012 |
20130085132 | PYRAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: | 04-04-2013 |
20130096106 | COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula: | 04-18-2013 |
20130116240 | INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF - Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. | 05-09-2013 |
20130158009 | PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS - Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X | 06-20-2013 |
20130158010 | METHODS FOR INCREASING THE STABILIZATION OF HYPOXIA INDUCIBLE FACTOR-1 ALPHA - Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1α) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1α prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1α. | 06-20-2013 |
20130184257 | PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS - Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X | 07-18-2013 |
20130203735 | CAPROLACTAM MGLUR5 RECEPTOR MODULATORS - The present invention is directed to caprolactams which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved. | 08-08-2013 |
20130237525 | LACTAM DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS - The present invention relates to lactam derivatives of formula (I) | 09-12-2013 |
20140113892 | LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS - The present application describes lactam-containing compounds and derivatives thereof of Formula I: | 04-24-2014 |
20140155383 | USE OF CATHEPSIN K INHIBITION FOR THE TREATMENT AND/OR PROPHYLAXIS OF PULMONARY HYPERTENSION AND/OR HEART FAILURE - The present invention relates to the use of cathepsin K and/or cathepsin S inhibitors in a method for the treatment and/or prophylaxis of pulmonary hypertension and/or heart failure. | 06-05-2014 |
20140256711 | Novel Compound Having Angiogenesis Inhibitory Activity, Method for Preparing Same, and Pharmaceutical Composition Comprising Same - Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formula I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent. | 09-11-2014 |
20150038492 | BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma. | 02-05-2015 |
20150119384 | ETHYNYL COMPOUNDS - The present invention relates to ethynyl derivatives of formula I | 04-30-2015 |
20150328219 | THIOETHER DERIVATIVES AS PROTEIN KINASE INHIBITORS - The present invention relates to thioether derivatives (1) as protein kinase inhibitors, which are useful for the treatment, relieve and/or prevention of diseases associated with abnormal and hyperproliferation of cells in a mammal, especially humans, and which are particularly useful for the treatment of all forms of cancer. | 11-19-2015 |
20150329493 | OMEGA-AMINO ACID DERIVATIVES OF BENZENE, PYRIDINE, AND PYRIDAZINE COMPOUNDS - Disclosed are compounds and pharmaceutically acceptable salts of Formula I | 11-19-2015 |
20160016907 | PYRIDINE DERIVATIVES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention provides, in part, compounds of Formula I: | 01-21-2016 |
20160075662 | INDAZOLYL- AND INDOLYL-BENZAMIDE DERIVATIVES - The invention relates to indazolylbenzamide, indolylbenzamide, benzo[d]imidazolyl-benzamide, and benzo[d]triazolylbenzamide derivatives of formula | 03-17-2016 |
20160130266 | ALPHA-OXOACYL AMINO-CAPROLACTAM BODY - The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an α-oxoacyl amino-caprolactam that is represented by formula (I) | 05-12-2016 |
20160130659 | COMPOSITIONS AND METHODS FOR TREATING CANCER - The instant invention relates to methods for the treatment of B-cell lymphomas and leukemia by administering a SYK inhibitor. In another embodiment, the invention relates to a method for treating a patient diagnosed with a B-cell lymphoma or leukemia, comprising administering a SYK inhibitor, wherein the B-cells of said patient to be treated are characterized by elevated expression levels of CD86. | 05-12-2016 |
20160375031 | ALPHA-OXOACYL AMINO-CAPROLACTAM DERIVATIVE - The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an α-oxoacyl amino-caprolactam derivative that is represented by formula (I) | 12-29-2016 |