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US 5,912,248 AGranted
Excitatory amino acid receptor antagonists
AssigneeEli Lilly and Company
InventorsCarmen Dominguez Fernandez, James Allen Monn, Matthew John Valli
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## in which X represents a bond, S, SO or SO.sub.2 ; and R is as defined in the specification are useful as modulators of metabotropic glutamate receptor function.
Claims10
A compound of the formula ##STR10## in which X represents a bond, S, SO or SO.sub.2 ;
- and R represents a (1-6C) alkyl group;
- a (2-6C)alkenyl group;
- a (2-6C)alkynyl group;
- an optionally substituted aromatic group;
- an optionally substituted heteroaromatic 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;
- a non-aromatic monocyclic heterocyclic group fused with one or two monocyclic aromatic or heteroaromatic groups;
- or a (1-6C) alkyl, (2-6C)alkenyl or (2-6C)alkynyl group which is substituted by one, two or three groups selected independently from an optionally substituted aromatic group, an optionally substituted heteroaromatic 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 and a non-aromatic monocyclic heterocyclic group fused with one or two monocyclic aromatic or heteroaromatic groups;
- or a non-toxic metabolically labile ester or amide thereof;
- or a pharmaceutically acceptable salt thereof.
9 more elements
A process for the preparation of a compound of formula I which comprises (a) hydrolyzing a compound of formula ##STR12## in which R.sup.1 represents a hydrogen atom or an acyl group and R.sup.2 represents a carboxyl group or an esterified carboxyl group, or a salt thereof;
- (b) hydrolyzing a compound of formula ##STR13## in which R.sup.3 represents a carboxyl group or an esterified carboxyl group, and R.sup.4 and R.sup.5 each independently represent a hydrogen atom, a (2-6C) alkanoyl group, a (1-4C) alkyl group, a (3-4C) alkenyl group or a phenyl (1-4C) alkyl group in which the phenyl is unsubstituted or substituted by halogen, (1-4C) alkyl or (1-4C) alkoxy, or a salt thereof;
- or
- (c) deprotecting a compound of formula ##STR14## in which R.sup.6 represents a hydrogen atom or a nitrogen protecting group and each of R.sup.7 and R.sup.8 independently represents a hydrogen atom or a carboxyl protecting group, or a salt thereof;
- whereafter, if necessary and/or desired
- (i) resolving the compound of formula I;
- (ii) converting the compound of formula I into a non-toxic metabolically labile ester thereof;
- and/or;
- (iii) converting the compound of formula I or a non-toxic metabolically labile ester thereof into a pharmaceutically acceptable salt thereof.
5 more elements
Dependencies are inferred from the claim text.