US 5,494,909 A · Substituted oxazinoisoquinoline derivatives, pharmaceutical compositions containing them and process for preparing same

Substituted oxazinoisoquinoline derivatives, pharmaceutical compositions containing them and process for preparing same

AssigneeRichter Gedeon Vegyeszeti Gyar Rt.

InventorsJen Kobor, Laszlo Lazar, Imre Huber, Judit Arva, Laszlo Szporny, Bela Kiss, Egon Karpati, Eva Palosi, Zsolt Szombathelyi, Adam Sarkadi, Aniko Gere, Mihaly Bodo, Katalin Csomor, Judit Laszy, Zsolt Szentirmai, Erzsebet Lapis, Sandor Szabo, Gabor Bernath, Ferenc Fulop

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Abstract

New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.4 alkyl; one of R.sup.2 and R.sup.3 is C.sub.1 to C.sub.4 alkoxy and the other one is phenyl-C.sub.1 to C.sub.4 alkoxy optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus; and R.sup.4 is phenyl optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus, or their solvates, individual optically active and geometric isomers, mixtures of such isomers, as well as pharmaceutically acceptable acid addition salts thereof. The compounds of the Formula (I) are capable of inhibiting calcium uptake to brain cells and have a protective effect on hypobaric hypoxia.

Claims6

Dependent claims

A compound of the formula ##STR7## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, phenyl or phenyl-C.sub.1-4 alkyl;

one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy and the other one is phenyl-C.sub.1-4 alkoxy optionally substituted by C.sub.1-4 alkyl in the aromatic nucleus;
and
R.sup.4 is phenyl optionally substituted by C.sub.1-4 alkyl in the aromatic nucleus or a solvate, an individual optically active or geometric isomer thereof or a mixture of such isomers or a pharmaceutically acceptable acid addition salt thereof.

Dependencies are inferred from the claim text.