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

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

Xavier Morelli

Philippe Roche

Yves Collette

Sébastien Combes

Iuliia Voitovich

Stéphane Betzi

Adrien Lugari

Brigit Raux

Laurent Hoffer

Jean-Claude Guillemot

Sabine Milhas

Stéphanie Betzi

Brigitt Raux

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

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Marseilles, France

Xavier Morelli