Class / Patent application number | Description | Number of patent applications / Date published |
514253120 | Chalcogen bonded directly to ring carbon of the additional six-membered nitrogen containing hetero ring | 24 |
20090124633 | N-OXIDES OF HETEROCYCLIC SUBSTITUTED BISARYLUREAS FOR TREATING KINASE-MEDIATED DISEASES - The present invention relates to heterocyclic substituted N-Oxides of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. | 05-14-2009 |
20090203711 | Inhibitors of P38 Map Kinase - Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: | 08-13-2009 |
20090312344 | ARYLPIPERAZINE DERIVATIVES AS ADRENERGIC RECEPTOR ANTAGONISTS - The present invention relates to α | 12-17-2009 |
20100075982 | Pyridinone Derivative For The Treatment of Premature Ejaculation - The invention provides 3-(methyloxy)-1-{4-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]butyl}-2(1H)-pyridinone of formula (I), | 03-25-2010 |
20100125079 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 05-20-2010 |
20100168126 | Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine Carbomamides and Related Compounds - Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 07-01-2010 |
20100168127 | Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine Carbomamides and Related Compounds - Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 07-01-2010 |
20100292247 | HETEROCYCLYL PYRIDYL SULFONAMIDE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS - Objects of the present invention are the compounds of formula I, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer. | 11-18-2010 |
20110130408 | PIPERAZIN-1-YL-TRIFLUOROMETHYL-SUBSTITUTED-PYRIDINES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS - The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. | 06-02-2011 |
20110251213 | Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-Piperazine Carbomamides and Related Compounds - Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 10-13-2011 |
20110257195 | Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-Piperazine Carbomamides and Related Compounds - Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 10-20-2011 |
20110312970 | PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS RELATED TO INSULIN RESISTANCE OR HYPERGLYCEMIA - The present invention provides novel compounds represented by the general formula (I): | 12-22-2011 |
20130123274 | Antitumor Agent Using Compounds Having Kinase Inhibitory Effect in Combination - An antitumor agent for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound or pharmaceutically acceptable salt thereof represented by Formula (II) exhibits an excellent antitumor effect compared to cases where these are individually used, and exhibits antitumor effects against various cancer types: | 05-16-2013 |
20130158045 | PROLYL HYDROXYLASE INHIBITORS - Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1α), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response. | 06-20-2013 |
20130190325 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS - A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X., X2 and X3 is a N atom and the remaining two or one of X | 07-25-2013 |
20130289048 | CYCLOHEXANE DERIVATIVE COMPOUND - To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R | 10-31-2013 |
20140221391 | CYCLOHEXANE DERIVATIVE COMPOUND - To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R | 08-07-2014 |
20140221392 | CYCLOHEXANE DERIVATIVE COMPOUND - To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R | 08-07-2014 |
20140275111 | NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS - This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity. | 09-18-2014 |
20140296253 | DIPHENYLMETHYL PIPERAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION USING SAME - The present invention provides: a novel compound which has a useful pharmacological action for treating heart failure or shock without increasing heart rate; and a pharmaceutical composition using the same. The present invention relates to a diphenylmethyl piperazine derivative represented by general formula (I) | 10-02-2014 |
20140378471 | SUBSTITUTED OXINDOLE DERIVATIVES AND THEIR USE AS VASOPRESSIN RECEPTOR LIGANDS - The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent. | 12-25-2014 |
20150099762 | COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS - This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity. | 04-09-2015 |
20150126522 | ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS - This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. | 05-07-2015 |
20150335626 | FLUORINATED DERIVATIVES OF 3-HYDROXYPYRIDIN-4-ONES - Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Frederich's Ataxia. | 11-26-2015 |