Asymmetric heterocyclic ester derivatives of 1,4-dihydropyridine

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514336, 546 15, 546283, 546284, 549 30, 549333, 549454, A61K 3144, C07D40512

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047105054

ABSTRACT:
The present invention relates to new asymmetric heterocyclic ester derivatives of 1,4-dihydropyridine-3,5-dicarboxylic acids of the formula: ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.4 -alkyl group; X and Y, which are identical or different, each represent O or S, at least one of the symbols X and Y being different from S; n is an integer equal to 1 or 2; and R.sub.2 and R.sub.3, which are identical or different, each represent H, CH.sub.3, CF.sub.3, C.sub.6 H.sub.5 or halogenophenyl, it being possible for R.sub.2 and R.sub.3, taken together, to form a 5-membered to 7-membered spirocycloaliphatic group with the C atom of the heterocyclic group to which they are bonded; and their optical iomers and diastereoisomers.
These new derivatives are useful as pharmaceuticals, in particular as vasodilators.

REFERENCES:
patent: 4545996 (1985-10-01), Lafon
Schramm et al. Nature vol. 303, Jun. 1983 pp. 535-537.
Nishihata, et al., "Adjuvent Effects of Glyceryl Esters of Acetoacetic Acid on Rectal Absorption of Insulin and Inulin in Rabbits" J. of Pharmacuetical Sciences, vol. 72, No. 3, 1983, pp. 290-285.
French Patent Office Report on Corresponding French Application 8502412.

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