N-(3-(5H-pyrrolo[2,3-b]pyrazin-2-yl)phenyl)acrylamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡嗪类
• 英文名称: N-(3-(5H-pyrrolo[2,3-b]pyrazin-2-yl)phenyl)acrylamide
• 英文别名: N-[3-(5H-pyrrolo[2,3-b]pyrazin-2-yl)phenyl]prop-2-enamide
• 化学式: C₁₅H₁₂N₄O
• 分子量: 264.286
• InChiKey: MCMJWJFHHMBXSO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  70.7
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  5-溴-4,7-二氮杂吲哚 、 3-丙烯酰胺基苯硼酸 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 sodium carbonate 作用下， 以 乙醇 、 甲苯 为溶剂， 生成 N-(3-(5H-pyrrolo[2,3-b]pyrazin-2-yl)phenyl)acrylamide
  参考文献：
  名称：

  3,5-(Un)substituted-1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H- pyrrolo[2,3-b]pyrazine dual ITK and JAK3 Kinase Inhibitors

  摘要：

  本发明涉及由式I描述的化合物： 其盐，它们的合成，以及它们作为ITK和JAK3抑制剂的用途，包括这些化合物以及使用这些化合物治疗各种疾病和/或疾病的方法，这些疾病与异常细胞生长有关，如自身免疫、炎症、类风湿关节炎、系统性红斑狼疮、动脉粥样硬化、溃疡性结肠炎、银屑病性关节炎、银屑病、克罗恩病、代谢和癌症疾病。本发明还提供包括本发明化合物的药学上可接受的组合物以及使用这些组合物的方法和制备本发明化合物的方法。

  公开号：

  US20140315909A1

文献信息

• Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
  申请人：Arrien Pharmaceuticals LLC

  公开号：US09206188B2

  公开（公告）日：2015-12-08

  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.

  本发明涉及公式I所描述的化合物及其盐、它们的合成以及它们作为ITK和JAK3抑制剂的用途，包括这些化合物和使用这些化合物治疗各种疾病和/或障碍的方法，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、银屑病性关节炎、牛皮癣、克罗恩病、代谢和癌症疾病等与异常细胞生长有关的疾病。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以及使用这些组合物的方法和制备本发明化合物的过程。
• ITK and JAK Kinase Inhibitors
  申请人：Arrien Pharmaceuticals LLC

  公开号：US20160046627A1

  公开（公告）日：2016-02-18

  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.

  本发明涉及公式I所描述的化合物及其盐，它们的合成以及它们作为ITK和JAK3抑制剂的用途，包括这些化合物和使用这些化合物治疗各种疾病和/或紊乱的方法，例如与异常细胞生长相关的疾病，如自身免疫、炎症、类风湿性关节炎、系统性红斑狼疮、动脉硬化、溃疡性结肠炎、银屑病性关节炎、牛皮癣、克罗恩病、代谢和癌症等。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以及使用这些组合物的方法和制备本发明化合物的过程。
• 3,5-(UN)SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE, 1H-PYRAZOLO[3,4-B]PYRIDINE AND 5H- PYRROLO[2,3-B]PYRAZINE DUAL ITK AND JAK3 KINASE INHIBITORS
  申请人：Arrien Pharmaceuticals LLC

  公开号：EP3545956A1

  公开（公告）日：2019-10-02

  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.

  本发明涉及式 I 所述的化合物： 其盐类、它们的合成和它们作为 ITK 和 JAK3 抑制剂的用途，包括这种化合物和使用所述化合物治疗各种疾病和或紊乱的方法，这种疾病与异常细胞生长有关，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。本发明还提供了包含本发明化合物的药学上可接受的组合物以及使用组合物的方法和制备本发明化合物的工艺。
• 3,5-(UN)SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE, 1H-PYRAZOLO[3,4-B]PYRIDINE AND 5H-PYRROLO [2-,3-B]PYRAZINE DUAL ITK AND JAK3 KINASE INHIBITORS
  申请人：Arrien Pharmaeuticals LLC

  公开号：EP2986300A2

  公开（公告）日：2016-02-24
• Phosphatase Binding Compounds and Methods of Using Same
  申请人：Yale University

  公开号：US20200268897A1

  公开（公告）日：2020-08-27

  The present invention provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Such target proteins can be any protein involved in the pathway of a disease or disorder, such as but not limited to cancer, neurodegeneration, metabolic disease, diabetes, insulin resistance, and so forth.