abstract |
A compound of formula (See Formula); and its pharmaceutically acceptable salts, wherein A1 and A2 are each halogen or H, X1 is CH2, SO or SO: X2 is CH2 or CO; Y is piperazinyl - (CH2) n-, 2.3.4.5.6.7-hexahydro-1H-1,4-diazepinyl- (CH2) no -N (R5) - (CH2) n-, where R5 is H or alkyl C1-4 and n is 0, 1, 2, 3 or 4: R1 is selected from the following: (a) N-morpholino-C1-4alkylphenyl, C1-4alkoxycarbonyl, (C2-5) acyl , dihydroimidazolyl, formamidino, guanidino or dihidroimidazolilamino, etc., (b) hydrogen, C1-4 alkyl, etc., (c) piperidinyl, (d) cycloalkyl, bicycloalkyl or C5-14 tricycloalkyl; (e) C7-14 azacyclo, azabicyclo- or azatriccycloalkyl: and (f) C7-10 bicycloalkenyl, C5-7 benzocycloalkyl or hetrocycle, etc. with the proviso that when Y is piperazinyl of A1 and A2 at least one is H: X2 is CH2; and / or R1 is a group selected from group (a): R2 is hydrogen, optionally substituted C1-4alkyl, or heterocycle; and R3 and R4 are each C1-5 alkyl; The new dihydropyridine compounds of this invention have excellent bradykinin antagonistic activity and are therefore useful for the treatment of inflammation, cardiovascular disease, pain, the common cold, allergies, asthma, pancreatitis, burns, viral infection, traumatic brain injury. , multiple trauma or the like in especially human mammals. |