摘要 |
The invention relates to compounds of formula (I) or a salt, solvate, or physiologically functional derivative thereof, in which: X is CH2-CH2, CH=CH, or CC; Y is hydrogen, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, aryl, hetaryl, arylC1-4alkyl, or hetarylC1-4alkyl, wherein the aryl and hetaryl groups are optionally substituted by halo, nitro, C1-6 alkyl, C1-6haloalkyl, hydroxy, C1-6 alkoxy, cyano, -C(O)nR<1>, -NR<1>S(O)nR<2>, -C(O)NR<1>R<2>, or -NR<1>R<2>, wherein R<1> and R<2> are independently selected from hydrogen, C1-4 alkyl and C1-4 haloalkyl, and n is 0, 1, or 2; Z is piperidinyl, piperazinyl, or quinuclidinyl; ring B is a 5- or 6-membered aromatic heterocycle fused to ring A and is optionally substituted by a group -L-R wherein: L is a bond, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, S(O)n, C(O)n, or CONR<3>, wherein n is 0, 1, or 2, and R<3> is selected from hydrogen, C1-4 alkyl, and C1-4 haloalkyl; and R is C1-6 alkyl, C4-7 cycloalkyl, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 alkoxy, cyano, -NR<4>R<5>, aryl or hetaryl, wherein R<4> and R<5> are independently selected from hydrogen, C1-6 alkyl and C1-6 haloalkyl, or together with the nitrogen to which they are bonded form a piperidinyl, morpholino, or pyrolidinyl group, and the aryl and hetaryl groups are optionally substituted by halo, nitro, C1-4 alkyl, hydroxy, C1-4 alkoxy, cyano, -C(O)NR<6>R<7> or -NR<6>R<7> wherein R<6> and R<7> are as defined for R<4> and R<5> above, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in medicine, particularly in the treatment of thrombotic disorders.
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申请人 |
GLAXO GROUP LIMITED;ALLEN, DAVID, GEORGE;ELDRED, COLIN, DAVID;JUDKINS, BRIAN, DAVID;MITCHELL, WILLIAM, LEONARD;SCOPES, DAVID, IAN, CARTER |
发明人 |
ALLEN, DAVID, GEORGE;ELDRED, COLIN, DAVID;JUDKINS, BRIAN, DAVID;MITCHELL, WILLIAM, LEONARD;SCOPES, DAVID, IAN, CARTER |