2-(3-(4-((1H-indazol-5-yl)amino)-6-(1,4-diazepan-1-yl)pyrimidin-2-yl)phenoxy)-N-isopropylacetamide | 1595290-02-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-(3-(4-((1H-indazol-5-yl)amino)-6-(1,4-diazepan-1-yl)pyrimidin-2-yl)phenoxy)-N-isopropylacetamide
• 英文别名: 2-[3-[4-(1,4-diazepan-1-yl)-6-(1H-indazol-5-ylamino)pyrimidin-2-yl]phenoxy]-N-propan-2-ylacetamide
• CAS: 1595290-02-0
• 化学式: C₂₇H₃₂N₈O₂
• 分子量: 500.603
• InChiKey: YAZONQLRTKPOSI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  37
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  120
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• TREATMENT OF OCULAR DISORDERS
  申请人：KADMON CORPORATION, LLC

  公开号：US20150238601A1

  公开（公告）日：2015-08-27

  The invention provides methods of treatment of ocular disorders, including ocular disease with an angiogenic component. In certain embodiments, the treatment comprises administration of a ROCK2 inhibitor and an angiogenesis inhibitor. In certain embodiments, the ROCK2 inhibitor is ROCK2 selective. In certain embodiments, the angiogenesis inhibitor is a VEGF antagonist, for example, and VEGFR2 antibody.

  本发明提供了治疗眼部疾病的方法，包括具有血管生成成分的眼部疾病。在某些实施例中，治疗包括给予ROCK2抑制剂和血管生成抑制剂。在某些实施例中，ROCK2抑制剂是ROCK2选择性的。在某些实施例中，血管生成抑制剂是VEGF拮抗剂，例如VEGFR2抗体。
• RHO KINASE INHIBITORS
  申请人：KADMON CORPORATION

  公开号：US20150252025A1

  公开（公告）日：2015-09-10

  The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2.

  本发明涉及ROCK1和/或ROCK2的抑制剂。还提供了通过抑制ROCK1和/或ROCK2治疗涉及疾病和障碍的方法。
• Rho kinase inhibitors
  申请人：KADMON CORPORATION, LLC

  公开号：US10183931B2

  公开（公告）日：2019-01-22

  The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2.

  本发明涉及 ROCK1 和/或 ROCK2 的抑制剂。还提供了涉及抑制 ROCK1 和/或 ROCK2 的治疗疾病和失调的方法。
• Treatment of GVHD
  申请人：KADMON CORPORATION, LLC

  公开号：US11311541B2

  公开（公告）日：2022-04-26

  The invention relates to treatment of graft versus host disease (GVHD) using compounds that inhibit ROCK2. In preferred aspects, the present invention provides methods for the treatment of GVHD, including chronic GVHD (cGVHD) using compounds having the formulae 1-XXV, as set forth herein.

  本发明涉及使用抑制 ROCK2 的化合物治疗移植物抗宿主疾病（GVHD）。在优选方面，本发明提供了使用具有本文所述式 1-XXV 的化合物治疗 GVHD（包括慢性 GVHD（cGVHD））的方法。
• TREATMENT OF GVHD
  申请人：KADMON CORPORATION, LLC

  公开号：US20170112832A1

  公开（公告）日：2017-04-27

  The invention relates to treatment of graft versus host disease (GVHD) using compounds that inhibit ROCK2. In preferred aspects, the present invention provides methods for the treatment of GVHD, including chronic GVHD (cGVHD) using compounds having the formulae 1-XXV, as set forth herein.