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公开(公告)号：US20160213676A1
公开(公告)日：2016-07-28
申请号：US15087807
申请日：2016-03-31
IPC分类号： A61K31/5375 , A61K31/4545 , A61K31/496 , A61K31/451 , A61K31/495 , A61K31/5377
CPC分类号： A61K31/5375 , A61K31/122 , A61K31/255 , A61K31/44 , A61K31/445 , A61K31/451 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/5377 , C07C323/22 , C07C2602/08 , C07D211/14 , C07D211/38 , C07D211/58 , C07D213/50 , C07D231/12 , C07D241/04 , C07D277/42 , C07D295/116 , C07D295/135 , C07D401/10 , C07D413/10 , C07D413/12
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.
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22.发明授权Substituted 2,3-dihydro-1H-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis 有权用于治疗多发性硬化的取代的2,3-二氢-1H-茚-1-酮维生素A相关的孤儿核受体拮抗剂公开(公告)号：US09359315B2
公开(公告)日：2016-06-07
申请号：US14469900
申请日：2014-08-27
IPC分类号： C07D295/116 , C07D241/04 , C07D413/10 , C07D401/10 , C07D413/12 , C07D295/135 , C07D213/50 , C07D211/14 , C07C323/22 , C07D231/12 , C07D277/42 , C07D211/38 , C07D211/58
CPC分类号： A61K31/5375 , A61K31/122 , A61K31/255 , A61K31/44 , A61K31/445 , A61K31/451 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/5377 , C07C323/22 , C07C2602/08 , C07D211/14 , C07D211/38 , C07D211/58 , C07D213/50 , C07D231/12 , C07D241/04 , C07D277/42 , C07D295/116 , C07D295/135 , C07D401/10 , C07D413/10 , C07D413/12
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.
摘要翻译： 本发明涉及化合物及其合成及其作为视黄酸相关孤儿核受体γt（RORγt）/RORγ的拮抗剂，反向激动剂，调节剂和/或抑制剂的用途。 本发明的化合物可用于调节RORγt/RORγ活性和用于治疗由RORγt）/RORγ介导的疾病或病症，例如与人自身免疫性疾病如多发性硬化（MS），类风湿关节炎 关节炎（RA），炎症性结肠炎，牛皮癣，COPD，疼痛，肥胖，糖尿病，血脂异常，骨质疏松症，哮喘，神经退行性疾病和癌症。
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![Substituted 1 H-Pyrrolo [2, 3-b] pyridine and 1 H-Pyrazolo [3, 4-b] pyridine Derivatives as Salt Inducible Kinase 2 (SIK2) Inhibitors](/abs-image/US/2016/03/31/US20160090382A1/abs.jpg.150x150.jpg)
23.发明申请Substituted 1 H-Pyrrolo [2, 3-b] pyridine and 1 H-Pyrazolo [3, 4-b] pyridine Derivatives as Salt Inducible Kinase 2 (SIK2) Inhibitors 有权取代的1 H-吡咯并[2,3-b]吡啶和1 H-吡唑并[3,4-b]吡啶衍生物作为盐诱导型激酶2（SIK2）抑制剂公开(公告)号：US20160090382A1
公开(公告)日：2016-03-31
申请号：US14958625
申请日：2015-12-03
发明人： Hariprasad Vankayalapati , Venkatakrishnareddy Yerramreddy , Venu Babu Ganipisetty , Sureshkumar Talluri , Rajendra P Appalaneni
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/635
摘要： Compounds according to Formulas I, IA or IB: to 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.
摘要翻译： 根据式I，IA或IB的化合物：其药学上可接受的组合物，其盐，它们的合成及其作为包括这些化合物的SIK2抑制剂的用途和使用所述化合物治疗各种疾病和/或病症如癌症，中风的方法 ，心血管，肥胖和II型糖尿病。
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![Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors](/abs-image/US/2015/12/08/US09206188B2/abs.jpg.150x150.jpg)
24.发明授权公开(公告)号：US09206188B2
公开(公告)日：2015-12-08
申请号：US14254398
申请日：2014-04-16
发明人： Hariprasad Vankayalapati , Venkatakrishnareddy Yerramreddy , Paramareddy Gangireddy , Rajendra P. Appalaneni
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to compounds described by Formula I: salts 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.
摘要翻译： 本发明涉及式I所述的化合物：其盐，它们的合成及其作为包括这些化合物的ITK和JAK3抑制剂的用途以及使用所述化合物治疗各种疾病和/或障碍的方法，所述疾病与异常细胞生长相关 例如自身免疫，炎症，类风湿性关节炎，系统性红斑狼疮，动脉粥样硬化，溃疡性结肠炎，银屑病关节炎，牛皮癣，克罗恩病，代谢和癌症疾病。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用组合物和制备本发明化合物的方法的方法。
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