Otsuka Pharmaceutical Company, Limited

Kimiaki Oka

Minoru Uchida

Kazuyuki Nakagawa

Kamuyuki Nakagawa

Kazuyukip Nakagawa

2-oxyindole derivatives represented by the following general formula: ##STR1## where R.sub.1 is selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, benzyl and phenethyl; A is --CH.dbd.CH-- or ##STR2## wherein R.sub.2 or R.sub.3 may be the same or different and are selected from the group consisting of hydrogen and C.sub.1-4 alkyl; R.sub.6 and R.sub.7 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1-4 alkyl, benzyl, phenethyl and together with the nitrogen atom, a heterocyclic group selected from the group consisting of a piperidino, morpholino, piperazino or thiazolino group; and m and n each are zero or a positive integer with m+n being no more than 11. The 2-oxyindole derivatives have excellent effects on the inhibition of platelet aggregation.

Platelet aggregation inhibiting 2-oxyindoles, their compositions and

2-Oxyindole derivatives represented by the following general formula: ##STR1## where R.sub.1 is selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, benzyl and phenethyl; A is --CH.dbd.CH-- or ##STR2## wherein R.sub.2 or R.sub.3 may be the same or different and are selected from the group consisting of hydrogen and C.sub.1-4 alkyl; R.sub.4 is --OR.sub.5, wherein R.sub.5 is selected from the group consisting of hydrogen, C.sub.1-8 alkyl, cyclohexyl, benzyl and phenethyl, or ##STR3## wherein R.sub.6 and R.sub.7 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1-4 alkyl, benzyl, phenethyl and together with the nitrogen atom, a heterocyclic group selected from the group consisting of a piperidino, morpholino, piperazino or thiazolino group; and m and n each are zero or a positive integer with m+n being no more than 11. The 2-oxyindole derivatives have excellent effects on the inhibition of platelet aggregation.

Novel benzcycloamide derivatives represented by the general formula, ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or aralkyl; B is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; A is ##STR2## (wherein R.sub.2 and R.sub.3 may be the same or different and are respectively hydrogen or C.sub.1-4 alkyl) or --CH.dbd.CH--; R.sub.4 is --OR.sub.5 (wherein R.sub.5 is hydrogen, C.sub.1-8 alkyl, cycloalkyl or aralkyl) or ##STR3## (wherein R.sub.6 and R.sub.7 may be the same or different and are respectively hydrogen, C.sub.1-4 alkyl or aralkyl or may form together with the nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a nitrogen, oxygen or sulfur atom); and m and n each are zero or a positive integer and m + n is no more than 11. The benzcycloamide derivatives represented by the above-mentioned general formula (I) have excellent effects of inhibiting platelet aggregation and are useful as preventives for thrombosis and embolism.

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Tokushima, Japan

Kimiaki Oka