tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5-dimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate | 1349068-00-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻烯杂卓类
• 英文名称: tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5-dimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate
• CAS: 1349068-00-3
• 化学式: C₂₂H₂₃ClN₄O₂S
• 分子量: 442.969
• InChiKey: LPBHVXYAYSYZPV-INIZCTEOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  97.6
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• [EN] MALE CONTRACEPTIVE COMPOSITIONS AND METHODS OF USE<br/>[FR] COMPOSITIONS CONTRACEPTIVES POUR LES HOMMES ET PROCÉDÉS D'UTILISATION ASSOCIÉS
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2011143657A1

  公开（公告）日：2011-11-17

  The invention relates to compositions and methods for effecting male contraception.

  这项发明涉及用于实现男性避孕的组合物和方法。
• Thienotriazolodiazepine compounds for treating neoplasia
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：EP2902030A1

  公开（公告）日：2015-08-05

  The invention features compositions for treating or preventing a neoplasia. More specifically, the invention provides thienotriazolodiazepine compounds for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

  本发明的特征是用于治疗或预防肿瘤的组合物。更具体地说，本发明提供了噻吩三唑二氮杂卓化合物，用于破坏包含溴多聚酶链的 BET 家族多肽与染色质的相互作用（例如，破坏溴多聚酶链与存在于组蛋白 N 端尾巴上的乙酰-赖氨酸修饰的相互作用）。
• Compositions and methods for treating neoplasia, inflammatory disease and other disorders
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10407441B2

  公开（公告）日：2019-09-10

  The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

  本发明的特点是治疗或预防肿瘤的组合物和方法。 更具体地说，本发明提供了破坏包含溴多聚酶链的 BET 家族多肽与染色质相互作用的组合物和方法（例如，破坏溴多聚酶链与存在于组蛋白 N 端尾上的乙酰-赖氨酸修饰的相互作用）。
• Combination therapy of transcription inhibitors and kinase inhibitors
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10702527B2

  公开（公告）日：2020-07-07

  The present disclosure provides combination therapy of a transcription inhibitor and a kinase inhibitor. The combination of the transcription inhibitor and the kinase inhibitor may be useful in treating and/or preventing in a subject a proliferative disease, such as proliferative a disease that is resistant to the transcription inhibitor alone or the kinase inhibitor alone. In certain embodiments, the proliferative disease is a cancer. The combination of the transcription inhibitor and the kinase inhibitor is expected to be synergistic.

  本公开提供了转录抑制剂和激酶抑制剂的组合疗法。转录抑制剂和激酶抑制剂的组合可用于治疗和/或预防受试者的增殖性疾病，如对单独转录抑制剂或单独激酶抑制剂耐药的增殖性疾病。在某些实施方案中，增殖性疾病是癌症。转录抑制剂和激酶抑制剂的组合可望产生协同作用。
• Compositions and methods for treating leukemia
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10676484B2

  公开（公告）日：2020-06-09

  The invention provides compositions, methods, and kits for the treatment of acute myeloid leukemia in a subject.

  本发明提供了用于治疗受试者急性髓性白血病的组合物、方法和试剂盒。