公开(公告)号：US06696452B2

公开(公告)日：2004-02-24

申请号：US09955601

申请日：2001-09-14

申请人： Robert Davies ,  David Bebbington ,  Ronald Knegtel ,  Marion Wannamaker ,  Pan Li ,  Cornelia Forster ,  Albert Pierce

发明人： Robert Davies ,  David Bebbington ,  Ronald Knegtel ,  Marion Wannamaker ,  Pan Li ,  Cornelia Forster ,  Albert Pierce

IPC分类号： C07D40314

CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

摘要： 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.

摘要翻译： 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，R 2，R 2'，R 和R y如说明书中所述。 环C具有邻位取代基，并且在非邻位任选被取代。 R 2和R 2'任选地与它们的插入原子一起形成稠环体系，例如吲唑环; 并且R x和R y任选地与它们的插入原子一起形成稠环体系，例如喹唑啉环。 这些化合物可用作蛋白激酶抑制剂，特别是GSK-3的抑制剂，用于治疗诸如糖尿病和阿尔茨海默病的疾病。