| abstract |
5-PHENYL-THIAZOL-2-IL-UREA DERIVATIVES AND USE AS P13 KINASE INHIBITORS. The present invention relates to a compound of the formula Ia: in which: R a a * ^ ^ is hydrogen or C ~ 1 ~ -C ~ 4 ~ -alkyl; R ^ b * ^ is - (C ~ 1 ~ -C ~ 4 ~ -alkylene) -YC ~ 1 ~ -C ~ 4 ~ -haloalkyl or - (C ~ 1 ~ -C ~ 4 ~ -alkylene) -YC ~ 1 ~ -C ~ 4 ~ -hidoxyalkyl; Y represents -CONH- or a five-membered heteroaryl group. R ^ 2 * ^ is C ~ 1 ~ -C ~ 4 ~ -alkyl or halogen; R ^ 3 * ^ is halo, -S0 ~ 2 ~ -CH ~ 3 ~, -S0 ~ 2 ~ -CF ~ 3 ~, carboxy, -CO-NH ~ 2 ~, -CO-di (C ~ 1 ~ - C ~ 8 ~ - alkyl) amino, or a 5- or 6-membered heterocyclic ring with one or more heteroatoms in the ring, selected from the group consisting of oxygen, nitrogen and sulfur, this ring being optionally substituted by halo, cyan, oxo , hydroxy, carboxy, nitro, C ~ 3 ~ -C ~ 8 ~ -cycloalkyl, C ~ 1 ~ -C ~ 8 ~ -alkylcarbonyl, C ~ 1 ~ -C ~ 8 ~ - alkoxy optionally substituted by aminocarbonyl, or C ~ 1 ~ -C ~ 8 ~ -alkyl optionally substituted by hydroxy, C ~ 1 ~ -C ~ 8 ~ -alkoxy, C ~ 1 ~ -C ~ 8 ~ -alkylamino or di (C ~ 1 ~ -C ~ 8-alkyl) amino; R ^ 4 * ^ is hydrogen, halo, -S0 ~ 2 ~ -CH ~ 3 ~, nitrile, C ~ 1 ~ -C ~ 8 ~ -haloalkyl, imidazolyl, C ~ 1 ~ -C ~ 8 ~ - alkyl, ~ NR ^ 8 * ^ R ^ 9 * ^ or SO ~ 2 ~ NR ^ 8 * ^ R ^ 9 * ^; and R ^ 5 * ^ is hydrogen, halogen or C ~ 1 ~ -C ~ 8 ~ -alkyl; and R ^ 9 * ^ are independently hydrogen, amino, C ~ 1 ~ -C ~ 8 ~ -alkylamino, di (C ~ 1 ~ -C ~ 8 ~ -alkyl) amino or C ~ 1 ~ -C ~ 8 ~ - 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 that improve by inhibiting phosphatidylinositol 3 kinase. |