5-phenyl-thiaz0l-2-yl-urea derivatives and use as pi3 kinase...

Details 5-phenyl-thiaz0l-2-yl-urea derivatives and use as pi3 kinase... 5-phenyl-thiaz0l-2-yl-urea derivatives and use as pi3 kinase...

C - Chemistry, Metallurgy

07

D

C07D 277/48 (2006.01) A61K 31/427 (2006.01) A61P 11/00 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2650655

The present invention concerns a compound of formula Ia wherein: Ra * is hydrogen or C1-C4-alkyl; Rb* is -(C1-C4-alkylene)-Y-C1-C4-haloalkyl or -(C1-C4-alkylene)-Y-C1-C4-hydroxyalkyl; Y represents -CONH- or a five membered heteroaryl group. R2* is C1-C4-alkyl or halogen; R3* is halo, -SO2-CH3, -SO2-CF3, carboxy, -CO-NH2, -CO-di(C1-C8-alkyl)amino, or a 5- or 6- membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, that ring being optionally substituted by halo, cyano, oxo, hydroxy, carboxy, nitro, C3-C8-cycloalkyl, C1-C8-alkylcarbonyl, C1-C8-alkoxy optionally substituted by aminocarbonyl, or C1-C8-alkyl optionally substituted by hydroxy, C1- C8-alkoxy, C1- C8-alkylamino or di(C1- C8-alkyl)amino; R4* is hydrogen, halo, -SO2-CH3, nitrile, C1- C8-haloalkyl, imidazolyl, C1- C8-alkyl, -NR8*R9*, or -SO2-NR8*R9*; and R5* is hydrogen, halogen or C1- C8-alkyl; R8* and R9* are independently hydrogen, amino, C1- C8-alkylamino, di(C1- C8-alkyl)amino, or CC1- C8-alkyl optionally substituted by hydroxyl; or a pharmaceutically acceptable salt, or solvate thereof, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

La présente invention concerne une composition de formule Ia dans laquelle : Ra * est de l'hydrogène ou de l'alkyle C1-C4; Rb* représente -(C1-C4-alkylène)-Y-C1-C4-haloalkyle ou -(C1-C4-alkylène)-Y-C1-C4-hydroxyalkyle; Y représente -CONH- ou un groupe d'hétéroaryle à cinq chaînons. R2* représente alkyle C1-C4-ou halogène, R3* représente halo, -SO2-CH3, -SO2-CF3, carboxy, -CO-NH2, -CO-di(C1-C8-alkyl)amino, ou un anneau hétérocyclique à 5 ou 6 chaînons possédant un ou plusieurs hétéroatomes cycliques sélectionnés dans un groupe comprenant oxygène, azote et soufre, cet anneau étant éventuellement substitué par halo, cyano, oxo, hydroxy, carboxy, nitro, C3-C8-cycloalkyle, C1-C8-alkylcarbonyle, C1-C8-alkoxy substitué facultativement par aminocarbonyle, ou C1-C8-alkyle facultativement substitué par hydroxy, C1- C8-alkoxy, C1- C8-alkylamino ou di(C1- C8-alkyl)amino; R4* représente hydrogène, halo, -SO2-CH3, nitrile, C1- C8-haloalkyle, imidazolyle, C1- C8-alkyle, -NR8*R9*, ou -SO2-NR8*R9*; et R5*représente hydrogène, halogène ou C1- C8-alkyle; R8* et R9* représentent indépendamment hydrogène, amino, C1- C8-alkylamino, di(C1- C8-alkyl)amino, ou CC1- C8-alkyle éventuellement substitués par hydroxyle, ou un sel pharmaceutiquement acceptable, ou un solvate dérivé, pour des compositions et l'utilisation de compositions dans le traitement de maladies amélioré par l'inhibition de la 3-kinase inositol phosphatidyle.

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