Aventis Pharma S.a.

Sanofi

Sanofi-aventis

The Salk Institute for Biological Studies

Jacques Mauger

Anil Nair

Fahad A Al-Obeidi

Kirsten Bjergarde

Michel Tabart

Serge Mignani

Volkmar Wehner

Karl Schoenafinger

Marcel Patek

Jean-Francois Gourvest

Neerja Bhatnagar

Mark Dodson

Hartmut Strobel

Kurt Ritter

Jean-Luc Malleron

Francois Nique

Herve Bouchard

Dominique Lesuisse

Sven Ruf

Youssef El-Ahmad

Patrick Van De Velde

Augustin Hittinger

Conception Nemecek

Tony Hunter

Mark Gabriel Palermo

Thomas Faitg

Magda Stankova

Jean-Christophe Carry

Uwe Heinelt

Laurent Schio

Henning Steinhagen

Bruno Filoche-Romme

Hervé Bouchard

Yasmina Bouali

Daniel Bond

Stephen Rush Fuhs

Didier Bénard

Greg Harlow

Jill Meisenhelder

Matthias Herrmann

Pavel Safar

Francois Clerc

Chantal Alcouffe

Bodo Scheiper

Cecile Combeau

Odile Angouillant-Boniface

Didier Benard

Robert Alan Binnie

Pierre Broto

Robert A Binne

Nina Ma

Karl Schoenafinager

Kirsten Bjegarde

Fahad Al-Obeidi

Mark Palermo

The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.

Pyrazolopyridine derivatives, preparation process therefor and therapeutic use thereof

A peptide is disclosed of the general structure: Z&#x2014;W&#x2014;Y, wherein Z and Y are independently a one to eight amino acid sequence wherein the amino acids are selected from glycine and alanine and W is a non-hydrolyzable pHis analogue. Such peptides can be used to produce sequence-independent anti-phosphohistidine antibodies. Also provided are antibodies that specifically bind to a peptide comprising a phosphohistidine (or a non-hydrolyzable pHis analogue) but fail to specifically bind to an identical peptide containing histidine instead of phosphohistidine.

Compositions and methods for analyzing histidine phosphorylation

Isolated monoclonal antibodies and or antigen binding fragments thereof are disclosed herein that specifically bind polypeptides comprising a histidine phosphorylated at N3 (3-pHis). Nucleic acids encoding these antibodies, vectors including these nucleic acids, and host cells transformed with these vectors and nucleic acids are also disclosed. Methods are also disclosed for using these antibodies, such as for detection of polypeptides comprising a histidine phosphorylated at N3 (3-pHis). In some embodiments, the methods can be used to investigate signal transduction pathways.

Generation and use of polyclonal and monoclonal antibodies specific for 3-phosphohistidine

The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.

Pyridylvinylpyrazoloquinolines as PAR1 inhibitors

The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R, R, R, Ra, Rb, and Rare as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.

Substituted pyrazoles, compositions containing these, method of production and use

This invention relates to compounds of formula (I) to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.

1,4-dihydropyridine-fused heterocycles, process for preparing the same, use and compositions containing them

The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

Cyclic urea compounds, preparation thereof and pharmaceutical use thereof as kinase inhibitors

The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors

The present invention discloses and claims hexahydropyridazine-3-carboxylic acid hydrazides and hydrazones of formula (I) as inhibitors of proteases and kinases, and methods of using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of the compounds of formula (I), pharmaceutical compositions, and methods for the preparation of combinatorial libraries and the compounds of formula (I) are also disclosed and claimed.

Hexahydropyridazine-3-carboxylic acid hydrazide and hydrazone derivatives, combinatorial libraries containing same, pharmaceutical compositions containing same and methods of preparation

The invention relates to a pyridazine derivative of formula (I), wherein the variables are as defined herein, pharmaceutical composition thereof, process for its preparation, and its pharmaceutical use.

Pyridazine derivative, pharmaceutical composition thereof, its pharmaceutical use, and process for its preparation

The present invention discloses and claims compounds of formula (I)as inhibitors of proteases and kinases, method using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of compounds of formula (I), pharmaceutical compositions and methods for preparation of combinatorial libraries and compounds of formula (I) are also disclosed and claimed.

Hexahydropyridazine-3-carboxylic acid derivatives, pharmaceutical compositions containing same and methods of preparation

17-Halogenated 19-nor steroids, preparation process and intermediates, use as medicaments and the pharmaceutical compositions containing them

17-halogenated 19-nor steroids, method and intermediates for preparing same, use as medicines and pharmaceutical compositions containing same

Growing community of inventors

Tucson, AZ, United States of America

Jacques Mauger