BENZOXAZINONE AND BENZOPYRIMIDINONE PIPERIDINYL TOCOLYTIC OXYTOCIN RECEPTOR ANTAGONISTS

摘要

Compounds of formula (17, in which X is -O-, -NH- and -NR8-; Y is -CH2- ,~-CHR8- and -C(R8)2-; R1 is camphor- 10-yl, C1-5 alkoxyl, styryl, hydroxystyryl, furyl, unsubstituted or substituted thienyl, naphthyl, indolyl, tetrahydronaphthyl, unsubstituted, mono- or di-substituted pyridyl, pyrazinyl, unsubstituted or substituted cyclohexyl where the substituent is R4, and unsubstituted or substituted phenyl where the substituents on phenyl are R5, R6 and R7; R2 is hydrogen, C1-5 alkoxy, C1-5 alkyl, amino, C1-5 alkylcarbonylamino, nitro or halogen; R3 is hydrogen, C1-5 alkoxycarbonyl, cyano or carbamoyl; R4 is one to two of hydrogen, oxo, hydroxy, C1-5 alkoxy, C1-5 alkoxycarbonylamino-C1-5 alkyl and amino-C1- 5 alkyl; R5, R6 are each independently selected from hydrogen, halogen, C1-5 alkyl, hydroxyl and C1-5 foxy; R7 is (a) or (b); W i s CO or SO2; and m is an integer from 0 to 1. Such compounds as useful as oxytocin and vasopressin receptor antagonists.