2,6-Dimethoxy-1-methylcyclohexa-2,4-diene-1-sulfonamide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磺酸及其衍生物
• 英文名称: 2,6-Dimethoxy-1-methylcyclohexa-2,4-diene-1-sulfonamide
• 英文别名: 2,6-dimethoxy-1-methylcyclohexa-2,4-diene-1-sulfonamide
• 化学式: C₉H₁₅NO₄S
• 分子量: 233.29
• InChiKey: WZIMBSOQLNGARD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  87
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Cortistatin analogues and syntheses and uses thereof
  申请人：President and Fellows of Harvard College

  公开号：US10273241B2

  公开（公告）日：2019-04-30

  Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the -catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGFβ/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.

  本文提供的是式(A)、(B)、(C)、(D)和(E)化合物、其药学上可接受的盐、季胺盐和 N-氧化物及其药物组合物。 式(A)、(B)、(C)、(D)和(E)化合物可考虑用作治疗多种疾病的药物，例如，包括但不限于与血管生成和CDK8和/或CDK19激酶活性相关的疾病。进一步提供的是使用式（A）、（B）、（C）、（D）或（E）化合物抑制 CDK8 和/或 CDK19 激酶活性的方法、调节 -catenin 通路的方法、调节 STAT1 活性的方法、调节 TGFβ/BMP 通路的方法、调节细胞中 HIF-1-α 活性的方法以及增加 BIM 表达以诱导细胞凋亡的方法。进一步提供 CDK8 和 CDK19 点突变体及其使用方法。
• EP2956138A1
  申请人：——

  公开号：EP2956138A1

  公开（公告）日：2015-12-23
• CORTISTATIN ANALOGUES AND SYNTHESES AND USES THEREOF
  申请人：President and Fellows of Harvard College

  公开号：US20180319814A1

  公开（公告）日：2018-11-08

  Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the -catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGFβ/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.
• [EN] THERAPEUTIC COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS THÉRAPEUTIQUES ET UTILISATIONS DE CEUX-CI
  申请人：KALA PHARMACEUTICALS INC

  公开号：WO2014127214A1

  公开（公告）日：2014-08-21

  Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions hereof for treating diseases are also provided.