Aventis Pharmaceuticals Inc.

Axys Pharmaceuticals, Inc.

Aventis Pharma Limited

Aventis Pharma S.a.

Rhone Poulenc Rorer

David John Aldous

Sukanthini Thurairatnam

Paul Joseph Cox

Michael Graupe

Stevan Wakefield Djuric

John R Regan

Daniel Gerard McGarry

Gregory Bernard Poli

Kevin Joseph Moriarty

Christopher Hulme

Rose Mappilakunnel Mathew

Andreas Paul Timm

Fu-Chih Huang

John O Link

John W Patterson

Frank Halley

Jiayao Li

James T Palmer

Tahir Nadeem Majid

Peter Charles Astles

Shelley Amendola

Shelley Bower

Jiayo Li

Michael L Edwards

Conception Nemecek

Stephanie Deprets

Andrew James Ratcliffe

Iain M McLay

Bernard Baudoin

Brian L Pedgrift

Sylvie Wentzler

Christopher D Edlin

Corinne Venot

Stephen Dennis Pickett

Roger John Aitchison Walsh

John Edward Souness

Justine Lai Yeun Quai

Vincent Leroy

Novel inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Compounds and compositions as cathepsin inhibitors

This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and pharmaceutically acceptable salts of the compounds of formula (I) and N-oxides thereof, Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmnaceutical compositions comprising compoundS of formula (I), their phatmaceUtical use and methods for their preparation.

Substituted azabicyclic compounds

Compounds of the formula and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.

Pyrrolopyrimidines

The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. 

Compounds and compositions as cathepsin S inhibitors

The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

The present invention concerns compounds of general formula (I): in which the substituents are as described herein.

Chemical compounds

The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

This invention is directed to certain physiologically active compounds of formula (I)

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Gillette, NJ, United States of America

David John Aldous