申请人:VERTEX PHARMACEUTICALS INCORPORATED
公开号:EP1698627A1
公开(公告)日:2006-09-06
This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2 are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.
本发明描述了式 II 的新型吡唑化合物:其中环 C 选自苯基、吡啶基、嘧啶基、哒嗪基、吡嗪基或 1,2,4-三嗪基环,R2、R2、Rx 和 Ry 如说明书所述。环 C 具有一个正交取代基,并可选择在非正交位置被取代。R2 和 R2 与它们之间的原子任选结合在一起形成一个融合环系统,如吲唑环;Rx 和 Ry 与它们之间的原子任选结合在一起形成一个融合环系统,如喹唑啉环。这些化合物可作为蛋白激酶抑制剂,尤其是 GSK-3 的抑制剂,用于治疗糖尿病和阿尔茨海默病等疾病。