2-[(9R)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetohydrazide | 1349713-55-8

• 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: 2-[(9R)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetohydrazide
• CAS: 1349713-55-8
• 化学式: C₁₉H₁₉ClN₆OS
• 分子量: 414.918
• InChiKey: LVAFENBQDUAWFC-CQSZACIVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  126
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  异硫氰酸荧光素酯 、 2-[(9R)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetohydrazide 以 乙醇 为溶剂， 以85%的产率得到5-[[[2-[(9R)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetyl]amino]carbamothioylamino]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acid
  参考文献：
  名称：

  [EN] MALE CONTRACEPTIVE COMPOSITIONS AND METHODS OF USE
  [FR] COMPOSITIONS CONTRACEPTIVES POUR LES HOMMES ET PROCÉDÉS D'UTILISATION ASSOCIÉS

  摘要：

  这项发明涉及用于实现男性避孕的组合物和方法。

  公开号：

  WO2011143657A1
• 作为产物：
  描述：

  2-((6R)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F]的[1,2,4 在 氯甲酸甲酯 、 肼 作用下， 以85%的产率得到2-[(9R)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetohydrazide
  参考文献：
  名称：

  [EN] MALE CONTRACEPTIVE COMPOSITIONS AND METHODS OF USE
  [FR] COMPOSITIONS CONTRACEPTIVES POUR LES HOMMES ET PROCÉDÉS D'UTILISATION ASSOCIÉS

  摘要：

  这项发明涉及用于实现男性避孕的组合物和方法。

  公开号：

  WO2011143657A1

文献信息

• Polymer, method for producing polymer, and drug conjugate
  申请人：Kawasaki Institute of Industrial Promotion

  公开号：US10441662B2

  公开（公告）日：2019-10-15

  Provided is a polymer including a repeating unit (I) represented by Formula (I) and a repeating unit (II) represented by Formula (II) (in the formulae, m represents 1 or 2, L represents a divalent aromatic hydrocarbon group or a divalent aliphatic hydrocarbon group, R1 represents a hydrogen atom, an aliphatic hydrocarbon group, or an aromatic hydrocarbon group, X represents ORx, SRx, or NRx1Rx2, Rx represents a hydrogen atom, an aliphatic hydrocarbon group, or an aromatic hydrocarbon group, Rx1 and Rx2 each independently represent a hydrogen atom, an aliphatic hydrocarbon group, or an aromatic hydrocarbon group).

  提供了一种聚合物，包括由式（I）表示的重复单元（I）和由式（II）表示的重复单元（II）（式中，m代表1或2，L代表二价芳香烃基团或二价脂肪烃基团，R1代表氢原子、脂肪烃基团或芳香烃基团，X代表ORx、SRx或NRx1Rx2，Rx代表氢原子、脂肪烃基团或芳香烃基团）、X代表ORx、SRx或NRx1Rx2，Rx代表氢原子、脂肪族烃基或芳香族烃基，Rx1和Rx2各自独立地代表氢原子、脂肪族烃基或芳香族烃基）。
• 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 Neoplasia, Inflammatory Disease And Other Disorders
  申请人：Bradner James Elliott

  公开号：US20130184264A1

  公开（公告）日：2013-07-18

  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).
• Male Contraceptive Compositions and Methods of Use
  申请人：Bradner James Elliott

  公开号：US20130210813A1

  公开（公告）日：2013-08-15

  The invention relates to compositions and methods for effecting male contraception.
• COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20180169097A1

  公开（公告）日：2018-06-21

  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.