Serotonin 5-HT3 receptor partial activator

Details Serotonin 5-HT3 receptor partial activator Serotonin 5-HT3 receptor partial activator

2005-03-15

2005-03-15

Weddington, Kevin E. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S252200, C514S254020, C514S374000, C514S376000, C514S377000

Reexamination Certificate

active

06867226

ABSTRACT:
This invention provides a serotonin 5-HT3receptor partial activator which has a serotonin 5-HT3receptor activating action, in addition to its serotonin 5-HT3receptor 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-HT3receptor antagonism and serotonin 5-HT3receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3receptor partial activators.In the above formula, R1to R4may 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 R1and R2may be linked together to form a ring structure, namely benzene ring; R5represents 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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Journal of Medicinal Chemistry, vol. 37, No. 9, Apr. 29, 1994, Synthesis of 2-piperazinylbenzothiazole and 2-piperazinyl benzoxazole 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.
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