Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process for their preparation, and their use

US5859025A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Adalbert Wagner · Gersthofen, DE
• Holger Heitsch · Hofheim, DE
• Gerhard Nolken · Pocking, DE
• Klaus Wirth · Frankfurt am Main, DE
• Bernward Scholkens · Kelkheim, DE

Key dates

• Filing date: Mar 18, 1997
• Grant date: Jan 12, 1999
• Expiry date: Mar 18, 2017

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process or their preparation, and their use Heterocyclic fluoroalkyl derivatives and fluoroalkoxy derivatives of the formula (I) having bradykinin-antagonistic action ##STR1## in which X.sub.1 -X.sub.3 are N or CR.sup.5, R.sup.1 and R.sup.2 are H or halogen, R.sup.3 and R.sup.4 are H, halogen, alkyl or alkenyl, R.sup.5 is H, halogen, (substituted) alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (substituted) aryl, (substituted)aryl-alkyl, --C(O)--OR.sup.6 or --C(O)--H, R.sup.6 and R.sup.8 H, alkyl, alkenyl or aryl-alkyl, R.sup.7 is (substituted) alkyl or (substituted) alkoxy, B is an aminocarboxylic acid, D is alkenediyl, alkanediyl or --(CH.sub.2).sub.n --Y.sub.p --(CH.sub.2).sub.m --, E is oxygen or sulfur, Y is oxygen, sulfur or NR.sup.8, n and m are a number 0-3, o is a number 1-3 and p is 0 or 1, and their physiologically tolerable salts and a process for their preparation are described.