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US 5,717,109 AGranted
Excitatory amino acid receptor antagonists
AssigneeEli Lilly and Company
InventorsM. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano
Life of this patent
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Abstract
The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.
Claims14
A compound of formula ##STR11## in which R represents a group of formula --L--Q in which
- L represents a bond or a diradical of formula --(CH.sub.2).sub.m (Z.sup.1).sub.p (CH.sub.2).sub.n --
- in which
- m is 1 to 10;
- p is 0 or 1;
- n is 0 to 6;
- and
- Z.sup.1 is oxygen, sulphur or a group of formula NR.sup.a in which R.sup.a represents hydrogen, (1-6C)alkyl or phenyl(1-3C)alkyl;
- and
- Q is hydrogen, an unsubstituted or substituted heteroaromatic group, an unsubstituted or substituted aromatic group, a non-aromatic carbocyclic group, a non-aromatic heterocyclic group, or a non-aromatic monocyclic carbocyclic group fused with one or two monocyclic aromatic or heteroaromatic groups, a non-aromatic monocyclic heterocyclic group fused with one or two monocyclic aromatic or heteroaromatic groups;
- or a group of formula --C(R.sup.1 R.sup.2 R.sup.3)
- in which R.sup.1 represents (1-6C)alkyl, an unsubstituted or substituted heteroaromatic group, an unsubstituted or substituted aromatic group, a non-aromatic carbocyclic group, a non-aromatic heterocyclic group, a non-aromatic monocyclic carbocyclic group fused with one or two monocyclic aromatic or heteroaromatic groups, or a non-aromatic monocyclic heterocyclic group fused with one or two monocyclic aromatic or heteroaromatic groups;
- one or both of R.sup.2 and R.sup.3 is as defined for R.sup.1 or represents a group of formula --Z.sup.2 --R.sup.4 in which Z.sup.2 represents a bond, O, S, CH.sub.2 or --NR.sup.b -- in which R.sup.b represents hydrogen, (1-6C) alkyl or phenyl(1-3C)alkyl, and R.sup.4 represents an unsubstituted or substituted heteroaromatic group or an unsubstituted or substituted aromatic group;
- and the other of R.sup.2 and R.sup.3, if any, represents hydrogen;
- provided that when Q represents hydrogen, L does not represent a bond or methylene;
- or a pharmaceutically acceptable metabolically labile ester or amide thereof;
- or a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.