Eli Lilly and Company

Université Louis Pasteur

Lilly, Sa

Darryle D Schoepp

James Allen Monn

Joseph P Tizzano

Paul Leslie Ornstein

David R Helton

William H Lunn

Mary Jeanne Kallman

Charles Howard Mitch

Camille-Georges Wermuth

Concepcion Pedregal Tercero

Jesus Ezquerra Carrera

Loretta A McQuaid

Almudena Rubio Esteban

Lawrence J Heinz

M Brian Arnold

Edward C Smith

Thomas Charles Britton

Kirk Willis Johnson

Steven Scott Henry

Thomas John Bleisch

Matthew John Valli

Michael Parvin Johnson

Nancy K Augenstein

Gunnar Erik Jagdmann, Jr

Andr E Mann

Ang Ele Schoenfelder

Thomas Hallett Large

Darrell Stephen Coleman

The present invention relates to potentiators of metabotropic glutamate receptor function and specifically provides compounds of formula I, compositions thereof and methods of using the same.

Potentiators of glutamate receptors

The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.

Synthetic excitatory amino acids

The present invention provides a method of treating anxiety and related disorders using an agonist which acts at negatively coupled cAMP-linked metabotropic glutamate receptors.

Anxiolytic agents

The present invention provides novel compounds that affect excitatory amino acid receptors and are useful in the treatment of neurological disorders. This invention also provides synthetic methods for the preparation of the novel compounds.

Excitatory amino acid receptor antagonists

Disclosed herein is a method of treating a disease of the central nervous system with a compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,

Pharmaceutical compounds for the treatment of CNS diseases

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.

This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof.

The present invention provides a method of treating substance dependence disorders using an agonist which acts at negatively coupled cAMP-linked metabotropic glutamate receptors.

Psychiatric agents

A pharmaceutical compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,

Pharmaceutical compounds

Pyrrolidinyl di-carboxylic acid derivatives as metabotropic glutamate

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.

Excitatory amino acid receptor antagonists in methods for the use thereof

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 neurological disorders associated with EAA receptors.

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Indianapolis, IN, United States of America

Darryle D Schoepp