| 摘要 |
A compound of the formula: (see fig. I) and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo or H; X1 is CH2, CO, SO or SO2; X2 is CH2, or CO; Y is piperazinyl-(CH2)n-, 2,3,4,5,6,7-hexahydro-1H-1,4-diazepinyl-(CH2)n- or N(R5)-(CH2)n- wherein R5 is H or C1-4 alkyl, and n is 0, 1, 2, 3, or 4; R1 is selected from the following: (a) N-morpholino-C1-4alkylphenyl, C1-4 alkoxycarbonyl, C2-5acyl, dihydroimidazolyl, formamidino, guanidino or dihydroimidazolylamino, etc.; (b) hydrogen, C1-4alkyl, etc.; (c) piperidinyl; (d) C5-14 cycloalkyl, bicycloalkyl or tricycloalkyl; (e) C7-14 azacyclo-, azabicyclo- or azatricyclo-alkyl; and (f) C7-10 bicycloalkenyl, benzo C5-7 cycloalkyl or heterocyclic, etc., with proviso that when Y is piperazinyl, at least one of A1 and A2 is H; X2 is CH2; and/or R1 is a group selected from group (a); R2 is hydrogen, C1-4 alkyl, optionally substituted phenyl, or heterocyclic; and R3 andR4 are each C1-5 alkyl. The novel dihydropyridine compounds of this invention have excellent bradykinin antagonistic activity and are thus useful for the treatment of inflammation, cardiovascular diseas, pain, common cold, allergies, asthma, pancreatitis, burns, virus infection, head injury, multiple trauma or the like in mammalian, especially humans.
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