公开(公告)号：US20100056524A1

公开(公告)日：2010-03-04

申请号：US12384477

申请日：2009-04-02

申请人： Edward Giles Mciver ,  Justin Stephen Bryans ,  Ela Smiljanic ,  Stephen John Lewis ,  Joanne Hough ,  Thomas Drake

发明人： Edward Giles Mciver ,  Justin Stephen Bryans ,  Ela Smiljanic ,  Stephen John Lewis ,  Joanne Hough ,  Thomas Drake

IPC分类号： A61K31/5377 ,  C07D239/02 ,  C07D403/12 ,  C07D413/12 ,  A61K31/505 ,  A61K31/506

CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D471/04

摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, —NR4R5, —OR6, —NR7(CO)R6, —NR7(CO)NR4R5, —NR7SO2R6, —NR7COOR7, —CONR4R5, C3-6-heterocycloalkyl and wherein R4-7 and A are as defined in the claims.Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.

摘要翻译： 本发明的第一方面涉及式（I）化合物或其药学上可接受的盐或酯，其中：R 1为C 3-8 - 环烷基; X是O，NR 7或C 3-6 - 杂环烷基; R 2是芳基，杂芳基，稠合或未稠合的芳基-C 3-6 - 杂环烷基或稠合或未稠合的杂芳基-C 3-6 - 杂环烷基，其各自任选被一个或多个选自芳基，杂芳基，C 1-6 - 烷基 C 3-7 - 环烷基和基团A，其中所述C 1-6 - 烷基任选被一个或多个选自芳基，杂芳基，R 10和A基团的取代基取代，所述杂芳基任选地被一个或多个R 10 团体 并且其中所述C 3-6杂环烷基任选地含有一个或多个选自氧，硫，氮和CO的基团; R 3是任选被一个或多个选自芳基，杂芳基，-NR 4 R 5，-OR 6，-NR 7（CO）R 6，-NR 7（CO）NR 4 R 5，-NR 7 SO 2 R 6，-NR 7 COOR 7，-CONR 4 R 5，C 3 -6-杂环烷基，其中R 4-7和A如权利要求中所定义。 其它方面涉及所述化合物在治疗各种治疗性疾病中的用途，更具体地涉及一种或多种激酶的抑制剂。

公开(公告)号：US20100317646A1

公开(公告)日：2010-12-16

申请号：US12727754

申请日：2010-03-19

申请人： Edward Giles Mciver ,  Ela Smiljanic ,  Denise Jamilla Harding ,  Joanne Hough

发明人： Edward Giles Mciver ,  Ela Smiljanic ,  Denise Jamilla Harding ,  Joanne Hough

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/538 ,  A61K31/498 ,  A61K31/506 ,  A61P25/28 ,  A61P35/00 ,  A61P25/16

CPC分类号： C07D471/04

摘要： A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-heterocycloalkyl ring; each R6 is independently selected from C1-6-alkyl, C3-7 cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted each R7 is selected from hydrogen, optionally substituted C1-6-alkyl and C3-7-cycloalkyl; each of R8 and R9 is independently hydrogen or optionally substituted C1-6-alkyl; or R8 and R9 together with the N to which they are attached form a C4-6-heterocycloalkyl; each R10 is selected from C3-7-cycloalkyl and optionally substituted C1-6-alkyl; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6 alkyl-C3-7-cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; A is selected from halogen, —NR4SO2R5, —CN, —OR6, —NR4R5, —NR7R11, hydroxyl, —CF3, —CONR4R5, —NR4COR5, —NR7(CO)NR4R5, —NO2, —CO2H, —CO2R6, —SO2R6, —SO2NR4R5, —NR4COR5, —NR4COOR5, C1-6-alkyl and —COR6. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula I.