5-(4-Chloro-phenyl)-6-methyl-1,3-dihydro-thieno[2,3-e][1,4]diazepin-2-one | 54359-55-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 5-(4-Chloro-phenyl)-6-methyl-1,3-dihydro-thieno[2,3-e][1,4]diazepin-2-one
• 英文别名: 5-(4-Chlorophenyl)-6-methyl-1,3-dihydrothieno[2,3-e][1,4]diazepin-2-one
• CAS: 54359-55-6
• 化学式: C₁₄H₁₁ClN₂OS
• 分子量: 290.773
• InChiKey: SJGNFBBWYWJVLK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  69.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] FUSED 1,4-DIAZEPINES AS BET PROTEIN DEGRADERS<br/>[FR] 1,4-DIAZÉPINES FUSIONNÉES EN TANT QU'AGENTS DE DÉGRADATION DE PROTÉINES BET
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2018052949A1

  公开（公告）日：2018-03-22

  The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

  本公开提供由式I表示的化合物：I，及其药用可接受的盐、水合物和溶剂合物，其中R1、R2a、R2b、R3、R4、Ar、L、X、Y和B的定义如规范中所述。本公开还提供用于治疗对BET溴结构域降解敏感的疾病或疾病的式I化合物，如癌症。
• [EN] FUSED 1,4-DIAZEPINES AS BET BROMODOMAIN INHIBITORS<br/>[FR] 1,4-DIAZÉPINES FUSIONNÉES UTILISÉES EN TANT QU'INHIBITEURS DE BROMODOMAINES BET
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2018144789A1

  公开（公告）日：2018-08-09

  The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.

  本公开提供了由式（I）表示的融合1,4-二氮杂环烷，并其药用盐和溶剂合物，其中A、E、R1、R2、R3、R4、R5和Ar如规范中所定义。本公开还涉及使用具有式（I）的化合物来治疗对BET溴结构域蛋白抑制敏感的疾病、症状或紊乱，如癌症。
• Fused 1,4-diazepines as BET protein degraders
  申请人：THE REGENTS OF THE UNIVERSITY OF MICHIGAN

  公开号：US10975093B2

  公开（公告）日：2021-04-13

  The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

  本公开提供了式 I 所代表的化合物：I及其药学上可接受的盐、水合物和溶液，其中R1、R2a、R2b、R3、R4、Ar、L、X、Y和B如说明书中所定义。本公开还提供了式 I 的化合物，用于治疗对 BET 溴链降解有反应的病症或紊乱，如癌症。
• Fused 1,4-diazepines as BET bromodomain inhibitors
  申请人：THE REGENTS OF THE UNIVERSITY OF MICHIGAN

  公开号：US11046709B2

  公开（公告）日：2021-06-29

  The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.

  本公开提供了由式（I）代表的融合 1，4-二氮杂卓：及其药学上可接受的盐和溶剂，其中 A、E、R1、R2、R3、R4、R5 和 Ar 如说明书中所定义。本公开还涉及具有式（I）的化合物用于治疗对抑制 BET 溴链蛋白有反应的疾病、病症或失调，如癌症。
• FUSED 1,4-DIAZEPINES AS BET PROTEIN DEGRADERS
  申请人：The Regents of The University of Michigan

  公开号：EP3512853B1

  公开（公告）日：2020-12-23