| 摘要 |
<p>The present invention concerns a compound of formula Ia wherein: Ra * is hydrogen or C<sub>1</sub>-C<sub>4</sub>-alkyl; Rb* is -(C<sub>1</sub>-C<sub>4</sub>-alkylene)-Y-C<sub>1</sub>-C<sub>4 </sub>-haloalkyl or -(C<sub>1</sub>-C<sub>4</sub>-alkylene)-Y-C<sub>1</sub>-C<sub>4 </sub>-hydroxyalkyl; Y represents -CONH- or a five membered heteroaryl group. R2* is C<sub>1</sub>-C<sub>4</sub>-alkyl or halogen; R3* is halo, -SO<sub>2</sub>-CH<sub>3</sub>, -SO<sub>2</sub>-CF<sub>3</sub>, carboxy, -CO-NH<sub>2</sub>, -CO-di(C<sub>1</sub>-C<sub>8</sub>-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, C<sub>3</sub>-C<sub>8</sub>-cycloalkyl, C<sub>1</sub>-C<sub>8</sub>-alkylcarbonyl, C<sub>1</sub>-C<sub>8</sub>-alkoxy optionally substituted by aminocarbonyl, or C<sub>1</sub>-C<sub>8</sub>-alkyl optionally substituted by hydroxy, C<sub>1</sub>- C<sub>8</sub>-alkoxy, C<sub>1</sub>- C<sub>8</sub>-alkylamino or di(C<sub>1</sub>- C<sub>8</sub>-alkyl)amino; R4* is hydrogen, halo, -SO<sub>2</sub>-CH<sub>3</sub>, nitrile, C<sub>1</sub>- C<sub>8</sub>-haloalkyl, imidazolyl, C<sub>1</sub>- C<sub>8</sub>-alkyl, -NR8*R9*, or -SO<sub>2</sub>-NR8*R9*; and R5* is hydrogen, halogen or C<sub>1</sub>- C<sub>8</sub>-alkyl; R8* and R9* are independently hydrogen, amino, C<sub>1</sub>- C<sub>8</sub>-alkylamino, di(C<sub>1</sub>- C<sub>8</sub>-alkyl)amino, or CC<sub>1</sub>- C<sub>8</sub>-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.</p> |
