PAF-antagonistic diazepines, methods of use

Claim 1

A method of treating an individual having a disorder responsive to PAF-antagonist activity which method comprises treating said individual with a therapeutically effective amount of a compound of formula ##STR100## wherein A is an anellated ring of the following formula ##STR101## R 1 and R 2 , are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl or an acid amide group; a saturated carbocyclic or heterocyclic ring condensed on, which may contain oxygen, sulphur or nitrogen as a heteroatom while the nitrogen-containing ring may carry an alkyl group at the nitrogen atom; halogen, trifluoromethyl, nitro, cyano, optionally substituted amino, alkylmercapto, alkylcarbonyl, alkoxy, alkyloxycarbonyl or an acid amide group; R 3 and R 4 , are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl, cyano or an acid amide group; R 5 and Z are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl or an acid amide group; R 6 is phenyl, optionally substituted, by methyl, methoxy, halogen, nitro or trifluoromethyl, or R 6 can be thienyl or α-pyridyl; Y is CO, CS or CH 2 ; and non-toxic, pharmaceutically acceptable acid addition salts thereof.

Claim 2

A method of treating an individual having a disorder responsive to PAF-antagonist activity which method comprises treating said individual with a therapeutically effective amount of a compound of formula ##STR100## wherein A is an anellated ring of the following formula ##STR101## R 1 and R 2 , are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl or an acid amide group; a saturated carbocyclic or heterocyclic ring condensed on, which may contain oxygen, sulphur or nitrogen as a heteroatom while the nitrogen-containing ring may carry an alkyl group at the nitrogen atom; halogen, trifluoromethyl, nitro, cyano, optionally substituted amino, alkylmercapto, alkylcarbonyl, alkoxy, alkyloxycarbonyl or an acid amide group; R 3 and R 4 , are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl, cyano or an acid amide group; R 5 and Z are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl or an acid amide group; R 6 is phenyl, optionally substituted, by methyl, methoxy, halogen, nitro or trifluoromethyl, or R 6 can be thienyl or α-pyridyl; Y is CO, CS or CH 2 ; and non-toxic, pharmaceutically acceptable acid addition salts thereof.