(9ci)-1H-1,2,4-噻唑并[4,3-a][1,4]二氮杂卓 | 108775-12-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并二氮卓类
• 中文名称: (9ci)-1H-1,2,4-噻唑并[4,3-a][1,4]二氮杂卓
• 英文名称: 1H-[1,2,4]Triazolo[4,3-a][1,4]diazepine
• CAS: 108775-12-8
• 化学式: C₆H₆N₄
• mdl: MFCD18807125
• 分子量: 134.14
• InChiKey: MIBXSOAJXOSVRS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  40
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] FUSED 1,4-OXAZEPINES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS<br/>[FR] 1,4-OXAZEPINES CONDENSÉES ET LEURS ANALOGUES ASSOCIÉS EN TANT QU'INHIBITEURS DE BROMODOMAINE BET
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2017142881A1

  公开（公告）日：2017-08-24

  The present disclosure provides fused 1,4-oxazepines and related analogs represented by Formula (I) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, A, and Y are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer.

  本发明公开了式(I)表示的融合1,4-噁嗪和相关类似物及其药学上可接受的盐、水合物和溶剂化物，其中R1、R2a、R2b、R3a、R3b、R4、R5、A和Y的定义如说明书中所述。本发明还涉及式(I)化合物用于治疗对BET溴结构域抑制有反应的病症或疾病，如癌症的用途。
• [EN] BROMODOMAIN-INHIBITING COMPOUNDS AND METHODS TO PREVENT OR TREAT A CANCER<br/>[FR] COMPOSÉS INHIBITEURS DE BROMODOMAINE ET MÉTHODES POUR PRÉVENIR OU TRAITER UN CANCER
  申请人：KAINOS MEDICINE INC

  公开号：WO2016171470A1

  公开（公告）日：2016-10-27

  Provided is a novel compound inhibiting the bromodomain and extra terminal domain (BET) proteins, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of a precancerous transformation or a cancer.

  提供了一种新型化合物，可以抑制溴结构域和额外末端结构域（BET）蛋白，并且包括该化合物的药物组合物，可用于预防或治疗癌前病变或癌症。
• Fused quadracyclic compounds, compositions and uses thereof
  申请人：Tabomedex Biosciences, LLC

  公开号：US10562909B2

  公开（公告）日：2020-02-18

  Provided herein are substituted fused quadracyclic compounds useful as inhibitors of MK2. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted fused quadracyclic compounds.

  本发明提供了可用作 MK2 抑制剂的取代融合四环化合物。本发明进一步提供了本发明化合物的药物组合物。本发明还提供了取代的融合四环化合物的医疗用途。
• 6H-THIENO[3,2-f][1,2,4]TRIAZOLO[4,3-a][1,4]DIAZEPINE
  申请人：Bayer Intellectual Property GmbH

  公开号：EP2751114A1

  公开（公告）日：2014-07-09
• FUSED 1,4-OXAZEPINES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS
  申请人：The Regents of The University of Michigan

  公开号：EP3416969A1

  公开（公告）日：2018-12-26