Excitatory amino acid receptor antagonists in methods for the use thereof

US5196421A · kind A · utility

Assignee

• ELI LILLY AND COMPANY · US

Inventors

• Loretta A. McQuaid · Indianapolis, US
• Charles H. Mitch · Columbus, US
• Paul Leslie Ornstein · Carmel, US
• Darryle D. Schoepp · Indianapolis, US
• Edward C. R. Smith · Fishers, US

Key dates

• Filing date: Jun 25, 1992
• Grant date: Mar 23, 1993
• Expiry date: Jun 25, 2012

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/505
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Excitatory amino acid receptor antagonists and methods for the use thereof are disclosed. The antagonists include compounds having the preferred formula: ##STR1## in which: each of A.sub.1, A.sub.2 and A.sub.3 is independently either C or N, except that at least one of A.sub.1, A.sub.2 and A.sub.3 is N; one of A.sub.4 and A.sub.5 is C and the other is N; each R.sub.1 and R.sub.2 is independently hydrogen, halogen, CN, NO.sub.2, alkyl, aromatic, azido or CF.sub.3 ; and R.sub.3 is hydrogen, alkyl, aromatic or CF.sub.3. Also included are the tautomers thereof, and the pharmaceutically acceptable salts of (III) and (IV) and the tautomers thereof. These compounds are useful as EAA antagonists for blocking one or more EAA receptors, as neuroprotective agents, and in the treatment of various neurological disorders associated with EAA receptors.