[2-[(5-Bromo-2-chloropyrimidin-4-yl)amino]-3-methylbutyl]carbamic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: [2-[(5-Bromo-2-chloropyrimidin-4-yl)amino]-3-methylbutyl]carbamic acid
• 英文别名: [2-[(5-bromo-2-chloropyrimidin-4-yl)amino]-3-methylbutyl]carbamic acid
• 化学式: C₁₀H₁₄BrClN₄O₂
• 分子量: 337.6
• InChiKey: PDUYATICFBMIMB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  87.1
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] COMBINATIONS AND DOSING REGIMES TO TREAT RB-POSITIVE TUMORS<br/>[FR] COMBINAISONS ET RÉGIMES POSOLOGIQUES POUR TRAITER DES TUMEURS RB-POSITIVES
  申请人：G1 THERAPEUTICS INC

  公开号：WO2016040858A1

  公开（公告）日：2016-03-17

  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.

  这项发明涉及使用特定剂量和组合或交替方案中的CDK4/6抑制剂治疗选择性RB阳性癌症和其他RB阳性异常细胞增殖紊乱疾病的方法。在一个方面，揭示了使用特定CDK4/6抑制剂与另一种化疗药物（例如，额外的激酶抑制剂、PD-1抑制剂或BCL-2抑制剂，或其组合）组合或交替治疗选择性RB阳性癌症。
• [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。
• Transient protection of normal cells during chemotherapy
  申请人：G1 Therapeutics, Inc.

  公开号：US10660896B2

  公开（公告）日：2020-05-26

  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.

  本发明涉及瞬时保护健康细胞，特别是造血干细胞和祖细胞（HSPC）以及肾脏细胞免受DNA损伤性化疗药物损害的改良化合物、组合物和方法。 在一个方面，所公开的化合物可作为高选择性、短效、瞬时起作用的细胞周期蛋白依赖性激酶4/6（CDK 4/6）抑制剂，用于接受DNA损伤性化疗方案治疗增殖性疾病的受试者，从而改善对健康细胞的保护。
• TRANSIENT PROTECTION OF NORMAL CELLS DURING CHEMOTHERAPY
  申请人：G1 Therapeutics, Inc.

  公开号：EP2968290A1

  公开（公告）日：2016-01-20
• COMBINATIONS AND DOSING REGIMES TO TREAT RB-POSITIVE TUMORS
  申请人：G1 Therapeutics, Inc.

  公开号：EP3191098A1

  公开（公告）日：2017-07-19