Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1992-06-25
1993-03-23
Friedman, S. J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
A61K 31495
Patent
active
051964210
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.
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McQuaid Loretta A.
Mitch Charles H.
Ornstein Paul L.
Schoepp Darryle D.
Smith Edward C. R.
Eli Lilly and Company
Friedman S. J.
Leeds James P.
Whitaker Leroy
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