2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-(methyl(tetrahydro-2H-pyran-4-yl)amino)-3-nitrophenyl)sulfonyl)benzamide

• 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: 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-(methyl(tetrahydro-2H-pyran-4-yl)amino)-3-nitrophenyl)sulfonyl)benzamide
• 英文别名: 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[methyl(oxan-4-yl)amino]-3-nitrophenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
• 化学式: C45H50ClN7O7S
• 分子量: 868.4
• InChiKey: JQFGDJSDMASTCH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.6
• 重原子数：
  61
• 可旋转键数：
  11
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  174
• 氢给体数：
  2
• 氢受体数：
  11

文献信息

• COMBINATION THERAPY OF A TYPE II ANTI-CD20 ANTIBODY WITH A SELECTIVE BCL-2 INHIBITOR
  申请人：GENENTECH, INC.

  公开号：EP3919079A1

  公开（公告）日：2021-12-08

  The invention provides a method for the treatment of a cancer in a human in need thereof comprising administering to said human an effective amount of a GA101 antibody or 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(3-nitro-4-((tetrahydro-2H-pyran-4-yl)methylamino)phenylsulfonyl)benzamide or a pharmaceutically acceptable salt thereof, for one or more dosing periods, followed by co-administering an effective amount of said GA101 antibody and 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(3-nitro-4-((tetrahydro-2H-pyran-4-yl)methylamino)phenylsulfonyl)benzamide or a pharmaceutically acceptable salt thereof, for one or more dosing periods.

  本发明提供了一种用于治疗有需要的人类癌症的方法，该方法包括向所述人类施用有效量的 GA101 抗体或 2-(1H-吡咯并[2、3-b]吡啶-5-氧基)-4-(4-((2-(4-氯苯基)-4,4-二甲基环己-1-烯基)甲基)哌嗪-1-基)-N-(3-硝基-4-((四氢-2H-吡喃-4-基)甲基氨基)苯磺酰基)苯甲酰胺或其药学上可接受的盐、在一次或多次给药期间，然后联合给药有效量的所述 GA101 抗体和 2-(1H-吡咯并[2,3-b]吡啶-5-氧基)-4-(4-((2-(4-氯苯基)-4、4-(4-((2-(4-氯苯基)-4, 4-二甲基环己-1-烯基)甲基)哌嗪-1-基)-N-(3-硝基-4-((四氢-2H-吡喃-4-基)甲氨基)苯磺酰基)苯甲酰胺或其药学上可接受的盐，用药一次或多次。
• Combination therapy with an anti-HER2 antibody-drug conjugate and a Bcl-2 inhibitor
  申请人：Genentech, Inc.

  公开号：US10898570B2

  公开（公告）日：2021-01-26

  The present invention is directed to a combination therapy involving an anti-HER2 antibody-drug conjugate and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a HER2-expressing cancer.

  本发明涉及一种联合疗法，包括一种抗 HER2 抗体-药物共轭物和一种选择性 Bcl-2 抑制剂，用于治疗癌症患者，特别是 HER2 表达癌症患者。
• Combination therapy of a type II anti-CD20 antibody with a selective BCL-2 inhibitor
  申请人：GENENTECH, INC.

  公开号：US10993942B2

  公开（公告）日：2021-05-04

  The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.

  本发明涉及一种包括 II 型抗 CD20 抗体和选择性 Bcl-2 抑制剂的联合疗法，用于治疗癌症患者，尤其是表达 CD20 的癌症患者。
• Combination therapy of a type II anti-CD20 antibody with a selective Bcl-2 inhibitor
  申请人：GENENTECH, INC.

  公开号：US11110087B2

  公开（公告）日：2021-09-07

  The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.

  本发明涉及一种包括 II 型抗 CD20 抗体和选择性 Bcl-2 抑制剂的联合疗法，用于治疗癌症患者，尤其是表达 CD20 的癌症患者。
• COMBINATION THERAPY WITH AN ANTI-HER2 ANTIBODY-DRUG CONJUGATE AND A BCL-2 INHIBITOR
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3319995B1

  公开（公告）日：2019-04-17