N-(3-(9H-carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)-1-phenylmethanesulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: N-(3-(9H-carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)-1-phenylmethanesulfonamide
• 英文别名: N-(3-carbazol-9-yl-2-hydroxypropyl)-N-(furan-2-ylmethyl)-1-phenylmethanesulfonamide
• 化学式: C₂₇H₂₆N₂O₄S
• 分子量: 474.58
• InChiKey: ATBAEWYTYWFVIA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  34
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  84.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  咔唑 在 potassium hydroxide 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 48.0h， 生成 N-(3-(9H-carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)-1-phenylmethanesulfonamide
  参考文献：
  名称：

  Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents

  摘要：

  A series of novel carbazole-containing sulfonamides and sulfamides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the results of efficacy studies in diet-induced obese (DIO) mice, and the desired pharmacokinetic parameters, compound 41 was selected for further profiling. (C) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2015.12.102

文献信息

• Carbazole-Containing Sulfonamides as Cryptochrome Modulators
  申请人：Reset Therapeutics, Inc.

  公开号：US20130303524A1

  公开（公告）日：2013-11-14

  The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.

  本文涉及含有咔唑基磺胺衍生物及其药用可接受盐或水合物的结构式I，其中变量R1、R2、R3、R4、R5、R6、R7、A、B、C、D、E、F、G、H、a和b分别描述。还提供了包含式I化合物的药物组合物，用于治疗Cry介导的疾病或紊乱，如糖尿病、肥胖症、代谢综合征、库欣综合征和青光眼。
• CARBAZOLE-CONTAINING SULFONAMIDES AS CRYPTOCHROME MODULATORS
  申请人：RESET THERAPEUTICS, INC.

  公开号：US20160200732A1

  公开（公告）日：2016-07-14

  The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , A, B, C′, D, E, F, G, H′, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.

  本文的主题是针对含有咔唑基的磺酰胺衍生物及其结构式I中的药学上可接受的盐或水合物，其中变量R1、R2、R3、R4、R5、R6、R7、A、B、C'、D、E、F、G、H'、a和b分别进行描述。同时提供了包含式I化合物的药物组合物，用于治疗Cry介导的疾病或紊乱，如糖尿病、肥胖症、代谢综合征、库欣综合征和青光眼。
• Carbazole-containing sulfonamides as cryptochrome modulators
  申请人：Reset Therapeutics, Inc.

  公开号：US10383880B2

  公开（公告）日：2019-08-20

  The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C′, D, E, F, G, H′, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.

  本发明的主题涉及结构式I的含咔唑磺酰胺衍生物及其药学上可接受的盐或水合物，其中相应地描述了变量R1、R2、R3、R4、R5、R6、R7、A、B、C′、D、E、F、G、H′、a和b。还提供了包含式 I 化合物的药物组合物，用于治疗 Cry 介导的疾病或紊乱，如糖尿病、肥胖症、代谢综合征、库欣综合征和青光眼。
• US9265772B2
  申请人：——

  公开号：US9265772B2

  公开（公告）日：2016-02-23
• US9775845B2
  申请人：——

  公开号：US9775845B2

  公开（公告）日：2017-10-03