专利号:ES-2975743-A1 优先权日:2022-11-22 标 题:METHOD OF PREPARATION OF MITAPIVAT, INTERMEDIATE SYNTHESIS OF MITAPIVAT AND METHODS OF PREPARATION THEREOF
专利号:US-6407103-B2 优先权日:1998-04-21 标 题:Indeno [1,2-c] pyrazol-4-ones and their uses 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-8003785-B2 优先权日:2008-06-18 标 题 :Halo-substituted pyrimidodiazepines 发明人:CAI JIANPING; CHEN SHAOQING; CHU XIN-JIE; LUK KIN-CHUN; MISCHKE STEVEN GREGORY; SUN HONGMAO; WOVKULICH PETER MICHAEL 权利人:TAKEDA PHARMACEUTICAL 摘要:The present invention provides PLK1 inhibitor compounds of formula I: n nuseful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
专利号:US-9951062-B2 优先权日:2012-12-14 标 题 :Substituted 1 H-pyrrolo [2, 3-b] pyridine and 1 H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors 发明人:VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANIPISETTY VENU BABU; TALLURI SURESHKUMAR; APPALANENI RAJENDRA P 权利人:ARRIEN PHARMACEUTICALS LLC 摘要:Compounds according to Formulas I, IA or IB: n nto pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.
专利号:US-9834551-B2 优先权日:2013-04-18 标 题 :Substituted pyrrolo[2,3-b]pyrazines and substituted pyrazolo[3,4-b]pyridines as ITK and JAK kinase inhibitors 发明人:VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANGIREDDY PARAMAREDDY; APPALANENI RAJENDRA P 权利人:ARRIEN PHARMACEUTICALS LLC 摘要:The present invention relates to compounds described by Formula I: n nsalts thereof, their synthesis, and their use as ITK and JAK3 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such disease associated with abnormal cell growth such as autoimmune, inflammation, rheumatoid arthritis, systemic lupus erythematosus, atherosclerosis, ulcerative colitis, psoriatic arthritis, psoriasis, Crohn's, metabolic and cancer diseases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions and processes for preparing the compounds of the invention.
专利号:US-9446047-B2 优先权日:2013-09-10 标 题 :Substituted 2,3-dihydro-1H-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis 发明人:VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY 权利人:ARRIEN PHARMACEUTICALS LLC 摘要:The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor γt (RORγt)/RORγ. The compounds of the present invention are useful for modulating RORγt)/RORγ activity and for treating diseases or conditions mediated by RORγt)/RORγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
参考文献:10.1007/s11696-024-03708-8 摘要:Wang K, Zhao D, Jin M, Li Y, Sun L, Zhu Y, Wang C, Li S, Wang Y, Miao Q, Chen X, Zhao Y, Hou Y. Multigram-scale synthesis of volasertib, an inhibitor of polo-like kinases in clinical evaluation. Chem. Pap. 2024 Oct 10;78(17):8965–77. doi: 10.1007/s11696-024-03708-8.