BOYLE, Robert George,WALKER, David Winter,BOYCE, Richard Justin
申请号：
GBGB2011/000739
公开号：
WO2011/141716A3
申请日:
2011.05.12
申请国别(地区):
WO
年份:
2012
代理人:
摘要：
The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof wherein R1 is cyano or C1-4 alkyl R2 is hydrogen or C1-4 alkyl R3 is hydrogen or C1-4 alkyl R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms R8 is hydrogen or C1-4 alkyl Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group -CH2CH2- which together with the said one carbon atom forms a cyclopropyl group m is 1, 2, 3 or 4 n is 0 or 1 and Ar is a monocyclic or bicyclic aryl or heteroaryl group of 5 to 10 ring members containing 0, 1, 2, 3 or 4 heteroatom ring members selected from O, N and S, the aryl or heteroaryl group being optionally substituted with one to four substituents R13 as defined in the claims. The compounds are inhibitors of Chk-1 kinase and are active against cancers.La présente invention concerne un composé de formule (1) : ou un sel, N-oxyde ou tautomère de celui-ci où R1 est un groupe cyano ou alkyle en C1-4 R2 est un hydrogène ou un groupe alkyle en C1-4 R3 est un hydrogène ou un groupe alkyle en C1-4 R4 et R5 sont identiques ou différents et chacun est choisi parmi un hydrogène, un groupe hydrocarbyle en C1-4 saturé et hydrocarbyloxy en C1-4 saturé R6 et R7 sont identiques ou différents et chacun est choisi parmi un hydrogène, un halogène, CN, un groupe alkyle en C1-4 et alcoxy en C1-4, lesdits groupes alkyle en C1-4 et alcoxy en C1-4 é
