6-Chloro-1-methyl-1H-indole-3-carboxylic acid | 1257122-37-4

• 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: 6-Chloro-1-methyl-1H-indole-3-carboxylic acid
• 英文别名: 6-chloro-1-methylindole-3-carboxylic acid
• CAS: 1257122-37-4
• 化学式: C₁₀H₈ClNO₂
• 分子量: 209.63
• InChiKey: UMVCXQBKCZPXCR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] NOVEL INDOLE AND PYRROLOPYRIDINE AMIDES<br/>[FR] NOUVEAUX AMIDES D'INDOLE ET DE PYRROLOPYRIDINE
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：WO2012114252A1

  公开（公告）日：2012-08-30

  The present invention relates to indole and pyrrolopyridine amide derivatives of formula (I) wherein R1, R 2, R 3, U, V, W, X, Y, Z and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

  本发明涉及式(I)的吲哚和吡咯吡啶酰胺衍生物，其中R1、R2、R3、U、V、W、X、Y、Z和环A如描述中所述，以及它们的制备方法，其药学上可接受的盐，以及它们作为药物的用途，含有式(I)的一个或多个化合物的药物组合物，特别是它们作为促进睡眠激素受体拮抗剂的用途。
• ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS CALCIUM OR SODIUM CHANNEL BLOCKERS
  申请人：Inoue Tadashi

  公开号：US20120101105A1

  公开（公告）日：2012-04-26

  The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Na v1.3 and Na v1.7 , and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

  本发明涉及公式(I)或其药学上可接受的盐的芳基取代羧酰胺衍生物，其具有T型钙通道或电压门控钠通道的阻滞活性，如Nav1.3和Nav1.7等Tetrodotoxin敏感(TTX-S)阻滞剂，并且在涉及T型钙通道或电压门控钠通道的疾病或疾病的治疗或预防中有用。本发明还涉及包含这些化合物的制药组合物以及在涉及T型钙通道或电压门控钠通道的疾病或疾病的预防或治疗中使用这些化合物和组合物的用途。
• ARYL CARBOXAMIDE DERIVATIVES AS TTX-S BLOCKERS
  申请人：Yamagishi Tatsuya

  公开号：US20120232052A1

  公开（公告）日：2012-09-13

  The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar 1 is phenyl; Ar 2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO 2 —, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.

  本发明涉及公式（I）的芳基羧酰胺衍生物，其中Ar1是苯基；Ar2是芳基；n为1-4；X为—O—、—S—、—SO—或—SO2—，其前体药物或其药学上可接受的盐，具有阻断电压门控钠通道如TTX-S通道的活性，并在治疗或预防涉及电压门控钠通道的疾病和疾病，如疼痛方面中有用。本发明还涉及包含这些化合物的制药组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病和疾病，如疼痛方面的使用。
• US9051296B2
  申请人：——

  公开号：US9051296B2

  公开（公告）日：2015-06-09
• US9101616B2
  申请人：——

  公开号：US9101616B2

  公开（公告）日：2015-08-11