Aventis Pharmaceuticals Inc.

Aventis Pharma Limited

Aventis Pharma S.a.

Rhone Poulenc Rorer

Tahir Nadeem Majid

Shelley Amendola

Paul Joseph Cox

Andrew David Morley

Stephanie Deprets

Brian L Pedgrift

Christopher D Edlin

Michael L Edwards

Herve Bouchard

Garry Fenton

Malcolm Norman Palfreyman

Charles J Gardner

Timothy A Gillespy

Frank Halley

Conception Nemecek

Justine Yeun Quai Lai

Didier Babin

John Charles Reader

Dominique Damour

Francois Clerc

David John Aldous

Michael Cherry

Dorothea Kominos

Chantal Carrez

Laurence Gauzy

Nawaz Mohammed Khan

Olivier Houille

Alain Le-Brun

Lloyd J Payne

Daniel N A Bezard

Andrew James Ratcliffe

Sukanthini Thurairatnam

Iain M McLay

Bernard Baudoin

Sylvie Wentzler

Nicola Collar

Jean Merrill

Corinne Venot

Christoper David Edlin

Roger John Aitchison Walsh

John Edward Souness

Corey Hopkins

Friederike Wirtz-Brugger

Stephanie D Deprets

Justine Y Q Lai

The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Benzimidazoles

This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

Compounds as PDE IV and TNF inhibitors

The invention is directed to physiologically active compounds of general formula (I):&#x2014; and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Azaindoles for inhibiting aurora2 and other kinases

A compound of formula XIX wherein R, R, Z, Z, Q, Qand Qas defined in the specification.

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

Chemical compositions containing physiologically active compounds of general formula (I): wherein Ris aryl or heteroaryl; Rrepresents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -ZR, &#x2014;C(&#x2550;O)&#x2014;NYY, &#x2014;COR, &#x2014;NYY, &#x2014;N(R)&#x2014;C(&#x2550;O)&#x2014;R, &#x2014;N(R)&#x2014;C(&#x2550;O)&#x2014;NYY, &#x2014;N(R)&#x2014;C(&#x2550;O)&#x2014;OR, &#x2014;N(R)&#x2014;SO&#x2014;R, &#x2014;N(R)&#x2014;SO&#x2014;NYYand one or more halogen atoms; Rrepresents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, &#x2014;C(&#x2550;O)&#x2014;ORor &#x2014;C(&#x2550;O)&#x2014;NYY; and Xrepresents N, CH, C-halo, C&#x2014;CN, C&#x2014;R, C&#x2014;NYY, C&#x2014;OH, C-ZR, C&#x2014;C(&#x2550;O)&#x2014;OR, C&#x2014;C(&#x2550;O)&#x2014;NYY, C&#x2014;N(R)&#x2014;C(&#x2550;O)&#x2014;R, C&#x2014;SO&#x2014;NYY, C&#x2014;N(R)&#x2014;SO&#x2014;R, C-alkenyl, C-alkynyl or C&#x2014;NO; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

Azaindoles

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

Chemical compounds

Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.

Pyrazoloisoquinoline derivative as kinase inhibitors for the treatment of various disorders

Compounds as PDE IV and TNF-inhibitors

The invention is directed to physiologically active compounds of general formula (I):and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

The invention is directed to physiologically active compounds of the general formula (Ix)and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

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Hoboken, NJ, United States of America

Tahir Nadeem Majid