N-(endo-8-Methyl-8-azabicyclo[3.2.1]octa-3-yl)-1-methyl-2-(4-nitrophenyl)indole-3-carboxamide hydrochloride | 287113-35-3

• 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-(endo-8-Methyl-8-azabicyclo[3.2.1]octa-3-yl)-1-methyl-2-(4-nitrophenyl)indole-3-carboxamide hydrochloride
• CAS: 287113-35-3
• 化学式: C₂₄H₂₆N₄O₃*ClH
• 分子量: 454.956
• InChiKey: QJRGTAMWBFJRSM-QIKSELNLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.53
• 重原子数：
  32.0
• 可旋转键数：
  4.0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  80.41
• 氢给体数：
  1.0
• 氢受体数：
  5.0

文献信息

• AMIDE DERIVATIVES AND DRUG COMPOSITIONS
  申请人：Nippon Shinyaku Co., Ltd.

  公开号：EP1156045A1

  公开（公告）日：2001-11-21

  The present invention is composed of an amide derivative represented by the following formula [1] or pharmaceutically acceptable salt thereof:    wherein R1 and R2 may be the same or different and each is hydrogen, alkyl which may be substituted, acyl, aryl which may be substituted, or an aromatic heterocyclic group which may be substituted; R3, R4, R5, and R6 may be the same or different and each is hydrogen, halogen, hydroxy, amino which may be substituted, alkyl which may be substituted, alkoxy, or nitro and the like; and R7 represents cyclic amino which may be substituted or azabicycloalkylamino which may be substituted, and a pharmaceutical composition which comprises it as an active ingredient. The compound of the invention is useful as an inhibitor of TGF-β production or an antagonist of TGF-β.

  本发明由下式[1]代表的酰胺衍生物或其药学上可接受的盐组成： 其中R1和R2可以相同或不同，各自为氢、可被取代的烷基、酰基、可被取代的芳基或可被取代的芳杂环基团；R3、R4、R5和R6可以相同或不同，各自为氢、卤素、羟基、可被取代的氨基、可被取代的烷基、烷氧基或硝基等；R7代表可被取代的环氨基或可被取代的氮杂环烷基氨基，以及将其作为活性成分的药物组合物。 本发明的化合物可用作 TGF-β 生成的抑制剂或 TGF-β 的拮抗剂。
• MEDICINAL COMPOSITION
  申请人：Nippon Shinyaku Co., Ltd.

  公开号：EP1243268A1

  公开（公告）日：2002-09-25

  The present invention is composed of a pharmaceutical composition for the therapy of nephritis which comprises an amide derivative represented by the following formula [1] or pharmaceutically acceptable salt thereof, as an active ingredient:    wherein R1 and R2 may be the same or different and each is hydrogen, alkyl which may be substituted, acyl, aryl which may be substituted, or an aromatic heterocyclic group which may be substituted; R3, R4, R5 and R6 may be the same or different and each is hydrogen, halogen, hydroxy, amino which may be substituted, alkyl which may be substituted, alkoxy or nitro and the like; and R7 represents cyclic amino which may be substituted or azabicycloalkylamino which may be substituted. The pharmaceutical composition of the invention is useful for the therapy of nephritis.

  本发明由一种治疗肾炎的药物组合物组成，该药物组合物包括下式[1]代表的酰胺衍生物或其药学上可接受的盐作为活性成分： 其中 R1 和 R2 可以相同或不同，各自为氢、可被取代的烷基、酰基、可被取代的芳基或可被取代的芳香杂环基团；R3、R4、R5 和 R6 可以相同或不同，各自为氢、卤素、羟基、可被取代的氨基、可被取代的烷基、烷氧基或硝基等；R7 代表可被取代的环氨基或可被取代的氮杂环烷基氨基。 本发明的药物组合物可用于治疗肾炎。