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US 5,859,011 AGranted
Dihydropyridine derivatives as bradykinin antagonist
AssigneePfizer Inc.
InventorsFumitaka Ito, Hiroshi Kondo, David L. Hageman, John A. Lowe, III, Susumu Nakanishi, Fredric J. Vinick
Life of this patent
Estimating the term…
Abstract
Compound of formula (1) and their pharmaceutically acceptable salts wherein A1,A2,R1, R2,R3,R4,X are as defined in the specification have excellent bradykinin antagonistic activity. ##STR1##
Claims13
A compound of the formula:
- ##STR9## and its pharmaceutically acceptable salts, wherein A.sup.1 and A.sup.2 are each halo;
- X is a direct bond, CH.sub.2, CO, O, S, S(O) or S(O).sub.2 ;
- R.sup.1 is selected from the following:
- (a) hydrogen, C.sub.1-4 alkyl optionally substituted with one or two substituents selected from hydroxy, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, pyridyl, carbamoyl, pyrrolidinocarbonyl, propylaminocarbonyl, piperidinocarbonyl or morpholinocarbonyl;
- (b) piperidinyl optionally substituted on the nitrogen atom with C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl;
- (c) C.sub.5-14 cycloalkyl, bicycloalkyl or tricycloalkyl, optionally substituted with one or two substituents selected from oxo, hydroxy, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, methoxybenzamido or morpholino;
- (d) C.sub.7-14 azacyclo-, azabicyclo- or azatricyclo-alkyl, in which the nitrogen atom optionally has a substituent selected from C.sub.1-4 alkyl, benzyl optionally substituted with one or two substituents selected from halo and trihalo C.sub.1-4 alkyl, C.sub.1-4 alkyloxycarbonyl optionally substituted with one or two halogen atoms and C.sub.2-5 acyl;
- and
- (e) C.sub.7-10 bicycloalkenyl, benzo C.sub.5-7 cycloalkyl or heterocyclic selected from a monocyclic or bicyclic hydrocarbon group having 4 to 10 carbon atoms and 1 to 3 hetero atoms;
- R.sup.2 is hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted with one or two substituents selected from halo, C.sub.1-4 alkyl, trihalo C.sub.1-4 alkyl and C.sub.1-4 alkoxy, or heterocyclic selected from a monocyclic or bicyclic hydrocarbon group having 4 to 10 carbon atoms and 1 to 3 hetero atoms;
- selected from a monocyclic or bicyclic hydrocarbon group having 4 to 10 carbon atoms and 1 to 3 hetero atoms;
- and
- R.sup.3 and R.sup.4 are each C.sub.1-3 alkyl.
10 more elements
Dependencies are inferred from the claim text.