Serotonin 5-HT.sub.3 receptor partial activator

Details Serotonin 5-HT.sub.3 receptor partial activator Serotonin 5-HT.sub.3 receptor partial activator

1997-05-06

2000-03-14

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540575, 540603, A61N 4362, C07D24308, C07D40300

Patent

active

060373423

ABSTRACT:
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.

REFERENCES:
patent: 5631257 (1997-05-01), Iwamatsu et al.
Chemical Abstracts, vol. 80, No. 25, Jun. 24, 1974, abstract No. 146143x, p. 444.
Journal of Medicinal Chemistry, vol. 37, No. 9, Apr. 29, 1994, "Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties," by Antonio Monge et al. pp. 1320-1325.
Journal of Medicinal Chemistry, vol. 11, No. 5, Aug. 26, 1968, "Synthesis of 1,4-disubstituted piperazines", by Matthew Verderame, p. 1091.
Chimica Therapeutica, vol. 6, No. 2, Mar., 1971, Paris, "Aryl-2 benzoxazoles a action anti-inflammatoire", pp. 126-130.

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