Centre National De La Recherche Scientifique

Institut National De La Sante Et De La Recherche Medicale

Université´ D'aix-marseille

Institut Jean Paoli & Irène Calmettes

L'institut Paoli-calmettes

Inserm (institut National De La Sante Et De La Recherche Medicale)

Sébastien Combes

Yves Collette

Philippe Roche

Xavier Morelli

Iuliia Voitovich

Jean-Michel Brunel

Marc Lopez

Jean-Claude Guillemot

Stéphane Betzi

Laurent Hoffer

Adrien Lugari

Brigit Raux

Sabine Milhas

Stéphanie Betzi

Brigitt Raux

Lynda Mezil

This invention relates to xanthine derivative compounds that are inhibitors of BET bromodomains proteins, the method of preparation thereof and applications thereof. 

Xanthine derivative inhibitors of BET proteins

The present invention relates to a compound having the following formula (I): (I) wherein: &#x2014;R is a (C-C)alkyl group; &#x2014;R&#x2033; is preferably H; &#x2014;Ar is a (C-C)arylene radical; &#x2014;Xis &#x2014;C(&#x2550;O)&#x2014;or &#x2014;SO&#x2014;; and &#x2014;R' is chosen from the group consisting of possibly substituted (C-C)alkyl, heteroaryl, (C-C)aryl, and (hetero)cycloalkyl groups, or a pharmaceutically acceptable salt and/or tautomeric form thereof, or its racemates, diastereomers or enantiomers. 

Xanthine derivatives and uses thereof as inhibitors of bromodomains of BET proteins

Provided are compounds of formula (I): wherein R, R, R, Rand Rare independently selected from the group comprising, inter aliae, H, optionally substituted, branched or linear C-Calkyl, halogen atom and C-Chaloalkyl, and wherein A represents a single bond or an optionally substituted C-Calkylene radical, notably useful for the treatment of human cancers.

Apoptosis inducing compounds

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Marseilles, France

Sébastien Combes