New histone deacetylases inhibitors

Details New histone deacetylases inhibitors New histone deacetylases inhibitors

C - Chemistry, Metallurgy

07

C

C07C 259/06 (2006.01) A61K 31/165 (2006.01) C07D 207/337 (2006.01) C07D 213/56 (2006.01) C07D 295/155 (2006.01) C07D 307/54 (2006.01) C07D 307/80 (2006.01) C07D 333/24 (2006.01) C07D 333/60 (2006.01) C07D 409/06 (2006.01)

Patent

CA 2581730

New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.

L'invention concerne de nouveaux inhibiteurs des histone-déacétylases à activité antitumorale, ainsi que le procédé de préparation de ceux-ci. Ces composés correspondent à la formule (I), dans laquelle R1 représente une chaîne linéaire ou ramifiée qui contient au moins deux liaisons double conjuguées, A représente un cycle phényle ou pyridyle éventuellement substitué, Ar représente un groupe aryle ou hétéroaryle éventuellement substitué, et R3 représente hydrogène ou alcoxyalkyle. Par ailleurs, l'invention concerne l'utilisation de ces composés dans le traitement des maladies associées à la dérégulation de l'activité des histone-déacétylases, telles que les tumeurs, ainsi que des compositions pharmaceutiques associées devant être administrées aux patients concernés.

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