Yoshitomi Pharmaceutical Industries, Ltd.

Takemi Fukuda

Tetsuya Tahara

Takeshi Kawakita

Michihide Setoguchi

Yasuaki Chihara

Takanobu Kuroita

Mitsuyoshi Yasumoto

Kiyoharu Hayano

Ryuhei Iezawa

A benzazine compound, a geometrical isomer of said benzazine compound, an optical isomer of said benzazine compound, and a pharmaceutically acceptable salt of said benzazine compound, said benzazine compound being represented by formula (I): ##STR1## wherein each symbol is as defined in the specification. Said benzazine compounds exhibit 5-HT.sub.3 receptor antagonistic activity, and 5-HT.sub.1A receptor and/or 5-HT.sub.2 receptor and/or dopamine D.sub.2 receptor blocking activity so that they are useful as drugs for the prophylaxis or treatment of various digestive diseases vomiting and disturbances in central nervous systems and the like. The intermediates for said benzazine compounds are also disclosed.

Benzazine compounds and pharmaceutical uses thereof

Benzoxazine compounds of the formula: ##STR1## wherein each symbol is as defined in the specification. The compounds exhibit 5-HT.sub.3 receptor antagonistic activity so that they are useful as antiemetics and so on.

Benzoxazine compounds and pharmaceutical use thereof

Benzofuran- and benzopyran-carboxamide derivatives of the formula: ##STR1## wherein l is 1 or 2; X is hydrogen atom, amino group or halogen atom; Y is --S(O).sub.m --R.sup.3 wherein R.sup.3 is lower alkyl group and m is 0, 1 or 2, or ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom or lower alkyl group; R.sup.1 is hydrogen atom, lower alkyl group, arylthiomethyl group, halogenomethyl group or ##STR3## wherein R.sup.6 and R.sup.7 are the same or different and are each hydrogen atom or lower alkyl group or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom form a hetrocycle; R.sup.2 is hydrogen atom or lower alkyl group; and Z is ##STR4## wherein p is 2 or 3, R.sup.8 and R.sup.9 are the same or different and are each lower alkyl group or R.sup.8 and R.sup.9 together with the adjacent nitrogen atom form a heterocycle, or ##STR5## wherein q is 0 or 1, n is 1 or 2, R.sup.10 is lower alkyl group, lower alkenyl group, lower alkinyl group, aralkyl group or cycloalkyl group and R.sup.11 is hydrogen atom or lower alkyl group, their physiologically acceptable salts or their optical isomers, and a method of preparing same. These compounds are useful as psychotropic and antipsychotic agents.

Benzofuran- and benzopyran-carboxamide derivatives

Indole-3-carboxamide derivatives of the formula: ##STR1## inclusive of pharmaceutically acceptable acid addition salt and/or hydrate forms thereof, wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, phenyl which may be optionally substituted by halogen on the benzene ring or phenyl-C.sub.1-4 alkyl which may be optionally substituted by halogen on the benzene ring; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkoxy; R.sup.4 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, allyl or benzyl which may be optionally substituted by halogen on the benzene ring or by methyl on the .alpha.-carbon; R.sup.5 is hydrogen or C.sub.1-4 alkyl; m is 0 or 1; and n is an integer of 1 to 3, are useful as neuroleptic and anxiolytic drugs, and for the prevention and treatment of psychosomatic disturbances.

Neuroleptic indole-3-carboxamide derivatives

There are disclosed tetrahydrofuran compounds and analogs thereof of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein X is oxygen or sulfur, R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkyl or lower alkoxy, and Am is a group of the formula: ##STR2## wherein Z is oxygen or sulfur, R.sup.3 is hydrogen or halogen, R.sup.4 is hydrogen, lower alkyl or phenyl which may be substituted by 1 to 3 substituents at any position(s) on the phenyl nucleus, each substituent being independently selected from halogen, lower alkyl and lower alkoxy, and R.sup.5 is hydrogen or lower alkyl. Such compounds are useful as neuroleptics.

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Fukuoka, Japan

Takemi Fukuda