4-(cyclopropylamino)-2-(4-(3,3-difluoropyrrolidin-1-yl)phenylamino)pyrimidine-5-carboxamide | 1198301-50-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 4-(cyclopropylamino)-2-(4-(3,3-difluoropyrrolidin-1-yl)phenylamino)pyrimidine-5-carboxamide
• 英文别名: US9868729, Example 179；4-(cyclopropylamino)-2-[4-(3,3-difluoropyrrolidin-1-yl)anilino]pyrimidine-5-carboxamide
• CAS: 1198301-50-6
• 化学式: C₁₈H₂₀F₂N₆O
• 分子量: 374.393
• InChiKey: RGOZWVYEQRUTTA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  96.2
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• [EN] 2, 6-DIAMINO-PYRIMIDIN- 5-YL-CARBOXAMIDES AS SYK OR JAK KINASES INHIBITORS<br/>[FR] 2, 6-DIAMINO-PYRIMIDIN- B-YL-CARBOXAMIDES SERVANT D'INHIBITEURS DE Syk KINASES ET DE JANUS KINASES
  申请人：PORTOLA PHARM INC

  公开号：WO2009145856A1

  公开（公告）日：2009-12-03

  The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK 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 and/or JAK 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 and/or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder, thrombosis, allergy, asthma, rheumatoid arthritis, leukemia, or non-Hodgkin's lymphoma.

  本发明涉及式I-II的化合物及其药学上可接受的互变异构体、盐或立体异构体，这些化合物是syk和/或JAK激酶的抑制剂。本发明还涉及用于制备这类化合物的中间体，制备这种化合物，含有这种化合物的药物组合物，抑制syk和/或JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗由syk和/或JAK激酶活性至少部分介导的多种疾病的方法，如心血管疾病、炎症性疾病、自身免疫疾病和细胞增殖障碍、血栓形成、过敏、哮喘、类风湿关节炎、白血病或非霍奇金淋巴瘤。
• Inhibitors of protein kinases
  申请人：Bauer Shawn M.

  公开号：US20090318407A1

  公开（公告）日：2009-12-24

  The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK 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 and/or JAK 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 and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及式I-II化合物及其药学上可接受的互变异构体、盐或立体异构体，其是SYK和/或JAK激酶的抑制剂。本发明还涉及用于制备这种化合物的中间体，该化合物的制备，含有该化合物的制药组合物，抑制SYK和/或JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗由SYK和/或JAK激酶活性至少部分介导的多种疾病，如不良血栓和非霍奇金淋巴瘤的方法。
• INHIBITORS OF PROTEIN KINASES
  申请人：Bauer Shawn M.

  公开号：US20120129867A1

  公开（公告）日：2012-05-24

  The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK 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 and/or JAK 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 and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及式I-II化合物及其药学上可接受的互变异构体、盐或立体异构体，其为syk和/或JAK激酶的抑制剂。本发明还涉及用于制备这种化合物的中间体，制备这种化合物的方法，包含这种化合物的制药组合物，抑制syk和/或JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由syk和/或JAK激酶活性介导的多种情况的方法，例如不良血栓形成和非何杰金淋巴瘤。
• 2, 6-DIAMINO-PYRIMIDIN- 5-YL-CARBOXAMIDES AS SYK OR JAK KINASES INHIBITORS
  申请人：Portola Pharmaceuticals, Inc.

  公开号：EP2321283A1

  公开（公告）日：2011-05-18
• US8138339B2
  申请人：——

  公开号：US8138339B2

  公开（公告）日：2012-03-20