(13S)-4-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-13-phenyl-1,3,5,11-tetrazatricyclo[7.4.0.02,7]trideca-2,4,6,8-tetraen-10-one | 1374742-95-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (13S)-4-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-13-phenyl-1,3,5,11-tetrazatricyclo[7.4.0.02,7]trideca-2,4,6,8-tetraen-10-one
• CAS: 1374742-95-6
• 化学式: C₂₅H₂₆N₈O
• 分子量: 454.534
• InChiKey: PBMNQMWMHILVLQ-OAQYLSRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  34
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  91.2
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• CDK INHIBITORS
  申请人：G1 THERAPEUTICS, INC.

  公开号：US20130237534A1

  公开（公告）日：2013-09-12

  Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

  式I、II或III的化合物及其药用盐可用作CDK抑制剂。
• [EN] TRANSIENT PROTECTION OF NORMAL CELLS DURING CHEMOTHERAPY<br/>[FR] PROTECTION TRANSITOIRE DE CELLULES NORMALES PENDANT UNE CHIMIOTHÉRAPIE
  申请人：G1 THERAPEUTICS INC

  公开号：WO2014144326A1

  公开（公告）日：2014-09-18

  This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.

  该发明涉及改进化合物、组合物和方法的领域，用于短暂保护健康细胞，特别是造血干细胞和祖细胞（HSPC）以及肾细胞，免受与损伤有关的DNA损伤化疗药物。在一个方面，通过使用所述的化合物揭示了对健康细胞的改进保护，这些化合物在接受DNA损伤化疗方案治疗增殖性疾病的受试者时作为高度选择性和短暂作用的细胞周期依赖性激酶4/6（CDK 4/6）抑制剂。
• CDK Inhibitors
  申请人：G1 Therapeutics, Inc.

  公开号：US20140142299A1

  公开（公告）日：2014-05-22

  Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

  式子I、II或III的化合物及其药学上可接受的盐，可用作CDK抑制剂。
• CDK inhibitors
  申请人：G1 Therapeutics, Inc.

  公开号：US10189849B2

  公开（公告）日：2019-01-29

  Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

  式 I、II 或 III 的化合物及其药学上可接受的盐类可用作 CDK 抑制剂。
• Anti-neoplastic combinations and dosing regimens using CDK4/6 inhibitor compounds to treat RB-positive tumors
  申请人：G1 Therapeutics, Inc.

  公开号：US10231969B2

  公开（公告）日：2019-03-19

  This invention directed to methods for treating select RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders using CDK4/6 inhibitors in specific dosing and combination or alternation regimes. In one aspect, treatments of select RB-positive cancers are disclosed using specific CDK4/6 inhibitors in combination or alternation with another chemotherapeutic, for example, an additional kinase inhibitor, PD-1 inhibitor, or BCL-2 inhibitor, or combination thereof.

  本发明涉及使用 CDK4/6 抑制剂以特定剂量和联合或交替方案治疗选择性 RB 阳性癌症和其他 Rb 阳性异常细胞增殖紊乱的方法。在一个方面，本发明公开了使用特定CDK4/6抑制剂与另一种化疗药物（例如，另一种激酶抑制剂、PD-1抑制剂或BCL-2抑制剂或其组合）联合或交替使用治疗选择性RB阳性癌症的方法。