Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones
AssigneeAmerican Home Products Corporation
InventorsJohn A. Butera, Schuyler A. Antane
Life of this patent
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Abstract
The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; A is a substituted phenyl group containing one cyano substituent and one substituent selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
Claims8
A compound of the formula:
- ##STR11## wherein:
- R.sub.1 and R.sub.2 are, independent from each other, hydrogen, C.sub.1-10 straight chain alkyl, C.sub.3-10 branched chain alkyl or C.sub.3-10 cyclic or bicyclic alkyl;
- A is a substituted phenyl group of the following formula:
- ##STR12## wherein:
- R.sub.4 is cyano;
- R.sub.5 is cyano, nitro, amino, C.sub.1-6 alkyl, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkoxy, C.sub.1-6 perfluoroalkoxy, amino, C.sub.1-6 alkylamino, C.sub.2-12 dialkylamino, sulfamyl, C.sub.1-6 alkylsulfonamido, C.sub.6-12 arylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, arylcarboxamido containing 7 to 13 carbon atoms, C.sub.1-6 alkylsulfonyl, C.sub.1-6 perfluoroalkylsulfone, C.sub.6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl;
- or a pharmaceutically acceptable salt thereof.
A method for reducing the adverse effects of smooth muscle contractions which comprises administering, orally or parenterally, to a patient in need thereof, a compound of the formula:
- ##STR14## wherein:
- R.sub.1 and R.sub.2 are, independent from each other, hydrogen, C.sub.1-10 straight chain alkyl, C.sub.3-10 branched alkyl, or C.sub.3-10 cyclic or bicyclic alkyl;
- and,
- A is a substituted phenyl group of the following formula:
- ##STR15## wherein:
- R.sub.4 is cyano;
- R.sub.5 is cyano, nitro, amino, C.sub.1-6 alkyl, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkoxy, C.sub.1-6 perfluoroalkoxy, amino, C.sub.1-6 alkylamino, C.sub.2-12 dialkylamino, sulfamyl, C.sub.1-6 alkylsulfonamido, C.sub.6-12 arylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, arylcarboxamido containing 7 to 13 carbon atoms, C.sub.1-6 alkylsulfonyl, C.sub.1-6 perfluoroalkylsulfone, C.sub.6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.