5-methyl-N-[3-[(1S)-1-[[6-[6-(2-morpholin-4-ylethylamino)pyridin-3-yl]pyrazin-2-yl]amino]ethyl]phenyl]pyridine-3-carboxamide | 1027254-14-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-methyl-N-[3-[(1S)-1-[[6-[6-(2-morpholin-4-ylethylamino)pyridin-3-yl]pyrazin-2-yl]amino]ethyl]phenyl]pyridine-3-carboxamide
• CAS: 1027254-14-3
• 化学式: C₃₀H₃₄N₈O₂
• 分子量: 538.652
• InChiKey: XJYMSBNQQGMZKM-QFIPXVFZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  40
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  117
• 氢给体数：
  3
• 氢受体数：
  9

文献信息

• INHIBITORS OF KINASE ACTIVITY
  申请人：Burns Christopher John

  公开号：US20100130447A1

  公开（公告）日：2010-05-27

  The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFRβ, PDGFRα or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.

  本发明涉及抑制激酶的吡啶或吡嗪类化合物。特别地，本发明的化合物抑制III类PTK受体家族的成员，如FMS（CSF-IR）、c-KIT、PDGFRβ、PDGFRα或FLT3和KDR、SRC、EphA2、EphA3、EphA8、FLT1、FLT4、HCK、LCK、PTK5（FRK）、SYK、DDR1和DDR2以及RET。本发明的化合物在治疗激酶相关疾病方面具有用途，包括免疫和炎症性疾病；增生性疾病，包括癌症和涉及新生血管形成的疾病；肾脏疾病；骨重塑性疾病；代谢性疾病；以及血管疾病。
• Inhibitors of kinase activity
  申请人：YM BioSciences Australia Pty Ltd

  公开号：EP2848610A1

  公开（公告）日：2015-03-18

  The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-1R), c-KIT, PDGFRβ, PDGFRα or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.

  本发明涉及可抑制激酶的吡啶或吡嗪类化合物。特别是本发明的化合物可抑制 III 类 PTK 受体家族的成员，如 FMS（CSF-1R）、c-KIT、PDGFRβ、PDGFRα 或 FLT3 和 KDR、SRC、EphA2、EphA3、EphA8、FLT1、FLT4、HCK、LCK、PTK5 (FRK)、SYK、DDR1 和 DDR2 以及 RET。本发明的化合物可用于治疗激酶相关疾病，如免疫和炎症性疾病；过度增殖性疾病，包括癌症和涉及新血管生成的疾病；肾脏和肾脏疾病；骨重塑疾病；代谢性疾病和血管疾病。
• US8461161B2
  申请人：——

  公开号：US8461161B2

  公开（公告）日：2013-06-11
• US9029386B2
  申请人：——

  公开号：US9029386B2

  公开（公告）日：2015-05-12