Meiji Seika Kaisha, Ltd.

Meiji Seika Kabushiki Kaisha

Other

Koichi Shudo

Schering Aktiengesellschaft

Meiji Seika Kaburhiki Kaisha

Fukio Konno

Yasuo Sato

Katsuyoshi Iwamatsu

Takashi Tsuruoka

Kiyoaki Katano

Hiroko Ogino

Kazuko Kobayashi

Tomoya Machinami

Megumi Yamada

Seiji Shibahara

Fumiya Hirano

Yasukatsu Yuda

Tamako Tomomoto

Shigeharu Inouye

Motohiro Nishio

Yasuyuki Ichimaru

Shigeharu Inoye

Naoki Yamazaki

Helmut Wachtel

Eiki Shitara

Michihiro Fujiwara

Naomi Osada

Tsuneyuki Yamamoto

Taiichiro Imanishi

Showa Ueki

Aiko Sawa

Masaaki Izumi

Yamazaki Naoki

Jun Nagura

Hiromi Watanabe

Kazuko Amano

This invention provides a serotonin 5-HTreceptor partial activator which has a serotonin 5-HTreceptor activating action, in addition to its serotonin 5-HTreceptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HTreceptor antagonism and serotonin 5-HTreceptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HTreceptor partial activators. In the above formula, Rto Rmay be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of Rand Rmay be linked together to form a ring structure, namely benzene ring; Rrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.

Serotonin 5-HT3 receptor partial activator

This invention provides a serotonin 5-HT,receptor partial activator which has a serotonin 5-HT,receptor activating action, in addition to its serotonin 5-HT,receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT,receptor antagonism and serotonin 5-HT,receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT,receptor partial activators.

Serotonin 5-HT3, receptor partial activator

This invention provides a serotonin 5-HT.sub.3 receptor partial activator which has a serotonin 5-HT.sub.3 receptor activating action, in addition to its serotonin 5-HT.sub.3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT.sub.3 receptor antagonism and serotonin 5-HT.sub.3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT.sub.3 receptor partial activators. ##STR1## In the above formula, R.sub.1 to R.sub.4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R.sub.1 and R.sub.2 may be linked together to form a ring structure, namely benzene ring; R.sub.5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.

Serotonin 5-HT.sub.3 receptor partial activator

A benzoxazole derivative of the formula (1) or (2) which has an alicyclic diamine group at the 2-position: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X.sup.-, m and n are defined herein. The compound shows excellent 5-HT.sub.3 receptor antagonism and is useful as an antiemetic agent, a peristalsis controlling agent, an analgesic agent, an antianxiety agent and a schizophrenia treating agent.

Benzoxazole derivatives

Pyridine derivatives having angiotensin II antagonism

Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which A, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;

Azole derivatives and anti-ulcerative composition containing same

A piperidine compound represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group having from 1 to 4 carbon atoms, a lower alkoxy group having from 1 to 4 carbon atoms, a hydroxymethyl group, --CO.sub.2 R.sup.3, or ##STR2## wherein R.sup.3 represents a hydrogen atom or a lower alkyl group having from 1 to 4 carbon atoms; R.sup.4 represents a hydroxyl group, a lower alkoxy group having from 1 to 4 carbon atoms or --NR.sup.6 R.sup.7 (wherein R.sup.6 and R.sup.7, which may be the same or different, each represent a hydrogen atom or a lower alkyl group having from 1 to 4 carbon atoms); and R.sup.5 represents a hydrogen atom, a lower alkanoyl group having from 1 to 4 carbon atoms, or a chlorobenzoyl group; R.sup.2 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted benzyl group, or a (2,2,6,6-tetramethylpiperidin-1-yl)ethyl group; and n represents 0 or an integer of 1 or 2, and an antiulcer composition containing said piperidine compound.

Piperidine compounds and antiulcer composition containing the same

Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which

Thiazolo [4,5-6] pyridine derivatives and anti-ulcerative composition

The invention relates to a method of treating dementia, such as cerebro-vascular dementia, for example, multiple infarct dementia and amyloid angiopathic dementia, cerebro-parenchymatous dementia, such as Alzheimer's dementia and Pick's disease, and dementia caused by brain tumor, hydrocephalus, hepatic meningitis, cerebral trauma, or cerebral function disorders, comprising administering rolipram.

Anti-dementia drug

Growing community of inventors

Kanagawa, Japan

Fukio Konno