公开(公告)号：US20090131470A1

公开(公告)日：2009-05-21

申请号：US11916485

申请日：2006-06-06

申请人： David Lee Walmsley ,  Martin James Drysdale ,  Christopher John Northfield ,  Christophe Fromont

发明人： David Lee Walmsley ,  Martin James Drysdale ,  Christopher John Northfield ,  Christophe Fromont

IPC分类号： A61K31/439 ,  C07D453/02 ,  A61K31/454 ,  C07D401/14 ,  A61P37/02

CPC分类号： C07D451/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D453/02 ,  C07D487/04

摘要： Compounds of formula (I) are inhibitors of PDK1 and CHK1 activity, and of use in the treatment of cancer and autoimmune disorders (I): wherein R2 is a radical of formula R7—(CH2)n−, or a radical of formula -Alk-N(—R5)—R9 wherein n is 0, 1, 2 or 3 and Alk is C1-C6 alkylene; R7 is (i) a heterocyclic ring of 5 or 6 ring atoms coupled via a ring carbon wherein the sole heteroatom is nitrogen, optionally substituted by C1-C6 alkyl or aryl C1-C6 alkyl, (ii) 1-aza-bicyclo[2.2.2]oct-3-yl, or (iii) 8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl; R8 and R9 are independently selected from hydrogen or C1-C3 alkyl; and the remaining substituents are as defined in the claims.

摘要翻译： 式（I）化合物是PDK1和CHK1活性的抑制剂，并且用于治疗癌症和自身免疫性疾病（I）：其中R2是式R7-（CH2）n-的基团，或式 - Alk-N（-R5）-R9，其中n为0,1,2或3，Alk为C1-C6亚烷基; R 7是（i）通过环碳连接的5或6个环原子的杂环，其中唯一杂原子是氮，任选被C 1 -C 6烷基或芳基C 1 -C 6烷基取代，（ii）1-氮杂 - 双环[2.2 .2]辛-3-基，或（iii）8-甲基-8-氮杂 - 双环[3.2.1]辛-3-基; R 8和R 9独立地选自氢或C 1 -C 3烷基; 而其余取代基如权利要求中所定义。