Recordati S.a. Chemical and Pharmaceutical Company

Recordati S.a.

Giorgio Bianchi

Dante Nardi

Amedeo Leonardi

Gabriele Graziani

Amedeo Leonardo

Gabriel Kraziani

Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.

Novel asymmetric diesters of

Antihypertensive diphenylpropyl aminopropyl ester of

Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.

N-(3,3-diphenylpropyl) aminoethyl esters of

##STR1## Esters I (Ar=3-nitrophenyl or 2,3-dichlorophenyl, A=C.sub.2 -C.sub.6 alkylene, R=C.sub.1 -C.sub.6 alkyl optionally C.sub.1 -C.sub.6 alkoxy monosubstituted, R.sub.1 =C.sub.1 -C.sub.4 alkyl) have antihypertensive activity and are effective against coronary heart diseases. They are prepared starting from the aldehyde ArCHO and esters of acetoacetic acid and 3-aminocrotonic acid. Pharmaceutical preparations containing them are also described.

Antihypertensive esters of 1,4-dihydro-2,6-dimethyl-3-(alkoxycarbonyl or

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Giorgio Bianchi