Fujirebio Inc.

Fujirebio Kabushiki Kaisha

Akiyoshi Kadoiri

Hiroshi Ikawa

Yasuko Konagai

Tetsuaki Yamaura

Noriko Kase

Yasuo Sekine

Nobuo Kobayashi

1,4-dihydropyridine derivatives and optically active 1,4-dihydropyridine derivatives with the following formula, having vasodilating activity based on calcium antagonism, and PAF antaognism, and methods of producing the same are disclosed: ##STR1## wherein (*) indicates a chiral center in the case of the optically active 1,4-dihydropyridine derivatives.

1,4-dihydropyridine derivatives and methods of producing the same

1,4-dihydropyridine derivatives and optically active 1,4-dihydropyridine derivatives with the following formula, having vasodilating activity based on calcium antagonism, and PAF antagonism, and methods of producing the same are disclosed: ##STR1## wherein (*) indicates a chiral center in the case of the optically active 1,4-dihydropyridine derivatives.

1, 4-Dihydropyridine derivatives and methods of producing the same

1,4-dihydropyridine derivatives

1,4-Dihydropyridine derivatives of formula: ##STR1## wherein Ar.sup.1 represents an aromatic hydrocarbon group or an aromatic heteromonocyclic or heterobicyclic group containing therein 1 to 3 atoms selected from the group consisting of oxygen, sulfur and nitrogen; R.sup.1 represents a hydrocarbon group which may have one or more substituents; A represents (i) a straight chain or branched chain unsaturated hydrocarbon group, (ii) a cyclic unsaturated hydrocarbon group, or (iii) a group selected from the group consisting of --R--O--N.dbd.CH--, --R--N.dbd.N--, --R--CH.dbd.N-- and --R--N.dbd.CH--, in which R is an alkylene group having 1 to 6 carbon atoms; B represents an alkylene or alkenylene group having 1 to 3 carbon atoms, which may have a substituent; Ar.sup.2 represents an aromatic hydrocarbon group or a heterocyclic group; Ar.sup.3 represents a heterocyclic group which may have one or more substituents; and n is 0 or 1, and the corresponding optical active 1,4-dihydropyridine derivatives, having an optically active cite as indicated by *, have both superior vasodilative and platelet aggregation inhibiting activities.

1,4-dihydropyridine derivatives of formula (I): ##STR1## wherein Ar.sup.1 and Ar.sup.2 each represent an unsubstituted or substituted aromatic hydrocarbon or aromatic heterocyclic group; and R.sup.1 represents --CO.sub.2 R.sup.2, --SO.sub.2 R.sup.3, --COR.sup.4, --CON(R.sup.5).sub.2, --CH--or --NO.sub.2 in which R.sup.2 is hydrogen, a straight chain, branched chain or cyclic saturated hydrocarbon group, which may have a substituent or a straight chain, branched chain or cyclic unsaturated hydrocarbon group having 2 to 10 carbon atoms, which may have a substituent, R.sup.3 is an alkyl group having 1 to 4 carbon atoms, R.sup.4 is an alkyl group having 1 to 4 carbon atoms or a phenyl group; and R.sup.5 is an alkyl group having 1 to 4 carbon atoms.

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Tokyo, Japan

Akiyoshi Kadoiri