KR960007588A - Indole Derivatives Having Angiotensin II Blocking Effect - Google Patents

Abstract

The present invention relates to a novel indole derivative or pharmaceutically acceptable non-toxic salt thereof having an angiotensin II inhibition effect represented by the following general formula (I) and a method for preparing the same.

Wherein X is N or C-CO ₂ H, R ¹ is C ₁ -C ₃ lower alkyl or C ₁ -C ₃ lower alkoxy, R ² , R ³ are each hydrogen or methyl and R ⁴ is hydrogen or C _1- C ₃ lower alkyl and R ⁵ is hydrogen, acetoxymethyl or ethoxycarbonyloxyethyl-1-yl.

Description

Indole Derivatives Having Angiotensin II Blocking Effect

Since this is an open matter, no full text was included.

Claims (4)

A novel indole derivative or pharmaceutically acceptable non-toxic salt thereof having the Angiotensin II inhibition effect of the general formula (I). Wherein R ₁ is C ₁ -C ₃ loweralkyl or C ₁ -C ₃ loweralkoxy, R ² , R ³ are each hydrogen or methyl, R ₄ is hydrogen or C ₁ -C ₃ loweralkyl, and R ₅ is Hydrogen, acetoxymethyl or ethoxycarbonyloxyethyl-1-yl, X is N or C-CO ₂ R ₆ , and R ₆ is hydrogen or C ₁ -C ₃ loweralkyl. The compound according to claim 1, wherein 2- [4- (5,7-dimethyl-2-ethylimidazo [4,5-b] pyridin-3-ylmethyl) phenyl] -1-ethyl-3- (5- Tetrazolyl) indole, 3- [2- (acetoxymethyl) tetrazol-5-yl] -2- [4- (5,7-dimethyl-2-ethylimidazo [4,5-b] pyridine- 3-ylmethyl) phenyl] -1-ethylindole, 2- [4- (5,7-dimethyl-2-ethylimidazo [4,5-b] pyridin-3-yl) methylphenyl] -3- [ 2- (ethoxycarbonyloxyethyl-1-yl) tetrazol-5-yl] -1-ethylindol, ethyl 2-ethoxy-1- [4- [1-ethyl-3- (5-tetrazolyl ) Indol-2-yl] phenylmethyl] benzimidazole-7-carboxylate, and 2-ethoxy-1- [4- [1-ethyl-3- (5-tetrazolyl) indol-2-yl) phenyl A novel indole derivative or pharmaceutically acceptable non-toxic salt thereof having an angiotensin II inhibition effect, characterized in that it is selected from the group consisting of methyl] benzimidazole-7-carboxylic acid. By reacting a compound of formula (II) with a metal azide or tri (lower) alkyl tin azide to prepare a compound of formula (I '), or reacting a compound of formula (I') with an alkyl halide A process for producing a compound of formula (I ′) or a compound of formula (I ″), which comprises producing a compound of formula (I ″). Wherein R ₁ is C ₁ -C ₃ loweralkyl or C ₁ -C ₃ loweralkoxy, R ² , R ³ are each hydrogen or methyl, R ₄ is hydrogen or C ₁ -C ₃ loweralkyl, and R ₅ is Hydrogen, acetoxymethyl or ethoxycarbonyloxyethyl-1-yl, X is N or C-CO ₂ R ₆ , and R ₆ is hydrogen or C ₁ -C ₃ loweralkyl. Angiotensin II inhibition composition comprising a novel indole derivative represented by the following general formula (I) or a pharmaceutically acceptable non-toxic salt thereof as an active ingredient and a pharmaceutically acceptable carrier. Wherein R ₁ is C ₁ -C ₃ loweralkyl or C ₁ -C ₃ loweralkoxy, R ² , R ³ are each hydrogen or methyl, R ₄ is hydrogen or C ₁ -C ₃ loweralkyl, and R ₅ is Hydrogen, acetoxymethyl or ethoxycarbonyloxyethyl-1-yl, X is N or C-CO ₂ R ₆ , and R ₆ is hydrogen or C ₁ -C ₃ loweralkyl. ※ Note: The disclosure is based on the initial application.