Dihydro-3,5-dicarboxylates

Details Dihydro-3,5-dicarboxylates Dihydro-3,5-dicarboxylates

1986-04-16

1989-03-21

Fan, Jane T.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546321, C07D40112

Patent

active

048144550

ABSTRACT:
A series of compounds of the 1,4-dihydropyridine class with a 3-carboxylate group linked to an alkyleneaminoalkylene heteroatom have been prepared possessing the general formula ##STR1## wherein R.sup.2, R.sup.5 and R.sup.6 are independently selected from lower (C.sub.1-4)alkyl, hydroxy-lower-alkylene, lower alkoxy-lower-alkylene, lower alkylamino-lower-alkylene or lower dialkyl-amino-lower-alkylene; R.sup.7 is selected from hydrogen, lower alkyl, phenyl-lower-alkylene, or phenylthio-lower-alkylene; n is the integer 2 or 3; X is a chemical bond, --O--, --S--, ##STR2## or --NR.sup.9 -- wherein R.sup.9 is hydrogen, lower alkyl, phenyl, or phenyl-lower-alkylene with the proviso that when X is a chemical bond, Z is a 3-indolyl ring; and Z is selected from the group consisting of phenyl substituted with 1 to 3 substituents independently chosen from among hydrogen, lower alkyl, or lower alkoxy, phenyl-lower-alkylene, or 3-indolyl.
Compounds of this series possess calcium channel blocking properties, afford protection against ischemia and inhibit aggregation of blood platelets.

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Bossert, et al., "4-Aryldihydropyridines, A New Class of Highly Active Calcium Antagonists", Angew. Chem., Int. Ed. Engl. 20, (1981), pp. 762-769.
Schramm, et al., "Novel Dihydropyridines With Positive Inotropic Action Through Activation of CA.sup.2+ Channels:, Nature, 30, (9 Jun. 1983), pp. 535-537.
Chem. Abstracts. 98, 107166j (1983).
Derwent Abstract 83-798692/43 (Japanese Patent J5,8157,785-A Yoshitomi Pharm. Ind. KK).
Derwent Abstract 86-008339/02 (West German Patent DE 3522-579-A Toyama Chem. KK).

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