| 摘要 |
PCT No. PCT/EP93/03054 Sec. 371 Date May 4, 1995 Sec. 102(e) Date May 4, 1995 PCT Filed Nov. 2, 1993 PCT Pub. No. WO94/10174 PCT Pub. Date May 11, 1994Compounds of formula (I): <IMAGE> (I) wherein Xg is O, S, SO, SO2, CH2, CH, N or NR wherein R is hydrogen or C1-6alkyl; A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms; R1g and R2g are hydrogen or C1-6alkyl; R3g is hydrogen, halo, C1-6alkyl, amino, nitro or C1-6alkoxy; R4g is hydrogen, halo, C1-6alkyl or C1-6alkoxy, Y is O or NH, or CO-Y together are a heterocyclic bioisostere; Z is of sub-formula: <IMAGE> wherein -(CH2)n1 is attached at carbon; and n1 is 0, 1, 2, 3 or 4; q is 0, 1, 2 or 3; Ra is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R7 wherein R7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R7 is C2-7alkoxycarbonyl or secondary or tertiary hydroxy substituted C1-6alkyl; and R6 is hydrogen or C1-6alkyl; are useful as 5HT4 receptor antagonists. |
