2-ureido-benzamide derivatives

摘要

This invention relates to 2-ureido-benzamide compounds of the formula : in which R<1> is H, halogen atom, (C1-C4)alkyl, (C1-C4)alkoxy or (C1-C4)dialkylamino and R<2> is H, halogen atom, hydroxy, nitro, (C1-C4)alkyl, (C1-C4)alkoxy or -(CH2)jNR<3>R<3>, wherein j is an integer of from 0 to 2, R<3> and R<4> are each independently H, (C1-C4)alkyl, (C1-C4)alkylsulfonyl or (C1-C4)alkylcarbamoyl, or R<3> and R<4> taken together with the N-atom to which they are linked can form a pyrrolidine, piperidine, morpholine, imidazole or pyrazole ring ; X is a (C3-C15)alkyl or -(CH2)kNR<5>R<6> group, wherein k is an integer of from 1 to 4 and R5 and R6 are each independently H, (C1-C6)alkyl or (C1-C4)alkoxycarbonyl ; and, Y is H or (C1-C4)alkyl and Z is or -(CH2)m-A<2> wherein m is an integer of from 0 to 4, Q is -CH2- or -CH2CH2-, A<1> is phenyl, benzyl, diphenylmethyl, pyridyl, imidazolyl, imidazolythio, dibenzoxepinyl or phenoxycarbonyl optionally carrying halogen atom, hydroxy, (C1-C7)alkyl, (C1-C4)alkoxy, (C1-C4)alkoxymethyl, phenyl or halogenophenyl, A<2> is phenyl, benzyl, diphenylmethyl, imidazolylthio, dibenzoxepinyl or phenoxycarbonyl optionally carrying halogen atom, hydroxy, (C1-C7)alkyl, (C1-C4)alkoxy, (C1-C4)alkoxymethyl, phenyl or halogenophenyl, R<7> is H or (C1-C4)alkyl and R<8> is (C1-C4)alkyl, or R<7> and R<8> taken together with the C-atom to which they are linked can form a cyclopentyl, cyclohexyl or cycloheptyl ring ; or, Y and Z taken together with the N-atom to which they are linked can form a ring wherein n is an integer of from 1 to 3 and B is phenyl, diphenylmethyl or dibenzocycloheptenyl optionally carrying halogen atom or (C1-C4)alkoxy ; and pharmaceutically acceptable acid addition salts thereof. Those compounds are useful as acyl-CoA:cholesterol acyltransferase inhibitors.