公开(公告)号：US07115739B2

公开(公告)日：2006-10-03

申请号：US09953471

申请日：2001-09-14

申请人： David Bebbington ,  Ronald Knegtel ,  Hayley Binch ,  Julian M. C. Golec ,  Pan Li ,  Jean-Damien Charier

发明人： David Bebbington ,  Ronald Knegtel ,  Hayley Binch ,  Julian M. C. Golec ,  Pan Li ,  Jean-Damien Charier

IPC分类号： C07D403/12 ,  C07D403/14 ,  A61K31/517 ,  A61P5/48

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 triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

摘要翻译： 本发明描述了式IX的新型三唑化合物：其中Z 1是氮或CR 9和Z 2是氮或CH，条件是在 Z 1和Z 2中的至少一个是氮; G是环C或环D; 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，其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; R＆lt; x＆gt;和＆lt; y＆gt; y＆lt; / sup＆gt;是独立地选自TR 3，或R x x和R y， / SUP>与它们的插入原子一起形成稠环; R 1，R 3和R 3如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为GSK-3和Aurora的抑制剂，用于治疗诸如糖尿病，癌症和阿尔茨海默病的疾病。