Meiji Seika Kaisha, Ltd.

Other

Koichi Shudo

Megumi Yamada

Yasuo Sato

Katsuyoshi Iwamatsu

Fukio Konno

Kazuko Kobayashi

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.

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Kanagawa, Japan

Megumi Yamada