10,10-dimethyl-2-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-6,6a,9,10-tetrahydro-5H-pyrazino[1',2':1,6]pyrido[2,3-d]pyrimidine-5,7(8H)-dione

• 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: 10,10-dimethyl-2-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-6,6a,9,10-tetrahydro-5H-pyrazino[1',2':1,6]pyrido[2,3-d]pyrimidine-5,7(8H)-dione
• 英文别名: 10,10-dimethyl-2-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-6,6a,9,10-tetrahydro-5H-pyrazino[1’,2’:1,6]pyrido[2,3-d]pyrimidine-5,7(8H)-dione；US10829490, Cmpd # 1；14,14-dimethyl-4-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-1,3,5,12-tetrazatricyclo[8.4.0.02,7]tetradeca-2,4,6-triene-8,11-dione
• 化学式: C₂₂H₂₈N₈O₂
• 分子量: 436.517
• InChiKey: UNHLUCCQTMZQPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  32
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  107
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• [EN] TRICYCLIC LACTAMS FOR USE IN THE PROTECTION OF NORMAL CELLS DURING CHEMOTHERAPY<br/>[FR] LACTAMES TRICYCLIQUES POUR UNE UTILISATION DANS LA PROTECTION DE CELLULES NORMALES LORS D'UNE CHIMIOTHÉRAPIE
  申请人：G1 THERAPEUTICS INC

  公开号：WO2015161287A1

  公开（公告）日：2015-10-22

  This invention is in the area of tricyclic lactam compounds, compositions and methods of 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, protection of healthy cells is disclosed using compounds that act as cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.

  这项发明涉及三环内酰胺化合物领域，以及保护健康细胞的方法和组合物，特别是造血干细胞和祖细胞（HSPC）以及肾脏细胞，免受与DNA损伤化疗药物相关的损害。在一个方面，揭示了使用作为细胞周期依赖性激酶4/6（CDK 4/6）抑制剂的化合物来保护健康细胞，当这些化合物被用于接受DNA损伤化疗方案治疗增殖性疾病的患者时。
• Tricyclic Lactams for Use in the Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation
  申请人：G1 THERAPEUTICS, INC.

  公开号：US20150297606A1

  公开（公告）日：2015-10-22

  This invention is in the area of tricyclic lactam compounds and methods for protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC), from the damage associated with ionizing radiation (IR) exposure using selective radioprotectants.

  这项发明涉及三环内酰胺化合物和保护健康细胞的方法，特别是造血干细胞和祖细胞（HSPC），使用选择性辐射保护剂保护它们免受电离辐射（IR）暴露所带来的损伤。
• Tricyclic Lactams for Use in the Protection of Normal Cells During Chemotherapy
  申请人：G1 Therapeutics, Inc.

  公开号：US20150297607A1

  公开（公告）日：2015-10-22

  This invention is in the area of tricyclic lactam compounds, compositions and methods of 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, protection of healthy cells is disclosed using compounds that act as cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.

  本发明涉及三环内酰胺化合物、组成物和保护健康细胞的方法，特别是造血干细胞和神经细胞，以及肾细胞，免受与DNA损伤化疗药物相关的损伤。在一个方面，使用作为细胞周期依赖性激酶4/6（CDK 4/6）抑制剂的化合物披露了健康细胞的保护，当这些化合物被给予正在接受DNA损伤化疗方案治疗增殖性疾病的受试者时。
• Tricyclic Lactams for Use as Anti-Neoplastic and Anti-Proliferative Agents
  申请人：G1 Therapeutics, Inc.

  公开号：US20150297608A1

  公开（公告）日：2015-10-22

  This invention is in the area of tricyclic lactam compounds and methods for treating selected cancers and hyperproliferative disorders.

  这项发明涉及三环内酰胺化合物及其治疗特定癌症和增生性疾病的方法。
• Tricyclic Lactams for Use in HSPC-Sparing Treatments for RB-Positive Abnormal Cellular Proliferation
  申请人：G1 THERAPEUTICS, INC.

  公开号：US20150299212A1

  公开（公告）日：2015-10-22

  This invention is in the area of tricyclic lactam compounds for and methods of treating selected Rb-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, treatment of select Rb-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as selective cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.

  这项发明涉及三环内酰胺化合物及其治疗选定的Rb阳性癌症和其他Rb阳性异常细胞增殖性疾病的方法，同时最大程度地减少与当前治疗方法相关的对健康细胞（例如健康造血干细胞和前体细胞）的有害影响。在某些方面，利用此处披露的特定化合物治疗选择的Rb阳性癌症。在某些实施例中，所述化合物在给予受试者时作为选择性细胞周期蛋白依赖性激酶4/6（CDK 4/6）抑制剂。