Merrell Pharmaceuticals, Inc.

Aventis Pharmaceuticals Inc.

Hoechst Marion Roussel

Merrell Dow Pharmaceuticals

Other

Shujaath Mehdi

Gary A Flynn

Douglas Wade Beight

Alan M Warshawsky

John F French

Norton P Peet

John H Kehne

Philippe Bey

Joseph P Burkhart

Edward D Daugs

Timothy Paul Burkholder

Michael R Angelastro

Philip M Weintraub

Eugene L Giroux

Paul Robert Eastwood

Kwon Yon Musick

John Ziqi Jiang

Neil Moorcroft

Jack Roger Koehl

Stefan Peukert

Hwa-Ok Kim

Michael John Janusz

Niall S Doherty

Uwe Schwahn

Sungtaek Lim

David Stefany

Matthew D Linnik

Paul R Eastwood

Phillipe Bey

David W Stefany

The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R, R, Rand Rare as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5'-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Substituted pyridones as inhibitors of poly(ADP-ribose) polymerase (PARP)

The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R, R, R, R, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5'-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Substituted AZA-indoles as inhibitors of poly(ADP-ribose) polymerase (PARP)

The present invention relates to a series of substituted indole derivatives of the formula I: 

Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP)

This invention relates to acylated enol derivatives of &agr;-ketoesters and &agr;-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema.

Acylated enol derivative of &agr;-ketoesters and &agr;-ketoamides

This invention relates to acylated enol derivatives of known elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema or as prodrugs of compounds which are useful in the treatment of said diseases.

Acylated enol derivatives as prodrugs of elastase inhibitors

This invention relates to acylated enol derivatives of .alpha.-ketoesters and .alpha.-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema.

Acylated enol derivatives of .alpha.-ketoesters and .alpha.-ketoamides

The present invention relates to certain novel mercaptoacetylamido 1,3,4,5-tetrahydro-benzo�c!azepin-3-one disulfide derivatives useful as inhibitors of enkephalinase and of ACE.

Mercaptoacetylamino 1,3,4,5-tetrahydro-benzo(C)azepin-2-one disulfide

Mercaptoacetylamide disulfide derivatives useful as inhibitors of

This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide group of the substrate peptide has been replaced by H, an aldehyde, a substituted carbonyl or a substituted malonyl moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Peptidase inhibitors

The present invention relates to certain novel mercaptoacetylamido 1,3,4,5-tetrahydro-benzo�c!azepin-3-one disulfide derivatives of the formula ##STR1## useful as inhibitors of enkephalinase and of ACE.

Mercaptoacetylamido 1,3,4,5-tetrahydro-benzo�c!azepin-3-one disulfide

This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

Substituted oxazolidine calpain and/or cathepsin B inhibitors

The present invention relates to compounds of formula 1, ##STR1## including all of its stereoisomers, compositions, and processes for preparation of the same. The compounds of the present invention are also useful in their pharmacological activities as they directly act as inhibitors of prolyl endopeptidase and thereby provide a methods for memory enhancement, preventing or slowing the affects of amnesia or memory deficits.

Prolyl endopeptidase inhibitors

The present invention relates to certain novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and of ACE.

2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful

The present invention relates to certain novel indane-2-mercaptoacetylamide disulfide derivatives of the formula ##STR1## useful as inhibitors of enkephalinase.

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Cincinnati, OH, United States of America

Shujaath Mehdi