Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-01-31
1999-01-19
Fan, Jane
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514255, 544365, 544362, C07D40106, A61K 31495
Patent
active
058614028
ABSTRACT:
A compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein A.sup.1 and A.sup.2 are each halo or H; X.sup.1 is CH.sub.2, CO, SO or SO.sub.2 ; X.sup.2 is CH.sub.2 or CO; Y is piperazinyl-(CH.sub.2).sub.n --, 2,3,4,5,6,7-hexahydro-1H-1,4-diazepinyl-(CH.sub.2).sub.n --or --N(R.sup.5)--(CH.sub.2).sub.n -- wherein R.sup.5 is H or C.sub.1-4 alkyl, and n is 0, 1, 2, 3, or 4; R.sup.1 is selected from the following: (a) N-morpholino-C.sub.1-4 alkylphenyl, C.sub.1-4 alkoxycarbonyl, C.sub.2-5 acyl, dihydroimidazolyl, formamidino, guanidino or dihydroimidazolylamino, etc.; (b) hydrogen, C.sub.1-4 alkyl, etc.; (c) piperidinyl; (d) C.sub.5-14 cycloalkyl, bicycloalkyl or tricycloalkyl; (e) C.sub.7-14 azacyclo-, azabicyclo- or azatricyclo-alkyl; and (f) C.sub.7-10 bicycloalkenyl, benzo C.sub.5-7 cycloalkyl or heterocyclic, etc., with proviso that when Y is piperazinyl, at least one of A.sup.1 and A.sup.2 is H; X.sup.2 is CH.sub.2 ; and/or R.sup.1 is a group selected from group (a); R.sup.2 is hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl, or heterocyclic; and R.sup.3 and R.sup.4 are each C.sub.1-5 alkyl. The novel dihydropyridine compounds of this invention have excellent bradykinin antagonistic activity and are thus useful for the treatment of inflammation, cardiovascular disease, pain, common cold, allergies, asthma, pancreatitis, burns, virus infection, head injury, multiple trauma or the like in mammalian, especially humans.
REFERENCES:
patent: 5162497 (1992-11-01), Coy et al.
patent: 5610142 (1997-03-01), Mavunkel et al.
Principles of Psychopharmacology Academic Press Clark et al. p. 166, 1970.
Dryer Mark
Fan Jane
Ginsburg Paul H.
Pfizer Pharmaceuticals, Inc.
Richardson Peter C.
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