Antiemetic N-(1-substituted-4,5-dihydro-1H-pyrazol-4-yl)benzamid

Details Antiemetic N-(1-substituted-4,5-dihydro-1H-pyrazol-4-yl)benzamid Antiemetic N-(1-substituted-4,5-dihydro-1H-pyrazol-4-yl)benzamid

1984-04-06

1985-10-15

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

548379, A61K 31415, C07D23106

Patent

active

045475180

ABSTRACT:
N-(1-Substituted-4,5-dihydro-1H-pyrazol-4-yl)benzamides having the general formula: ##STR1## wherein R is loweralkyl, cycloalkyl or phenylloweralkyl and R.sub.1 is selected from hydroxy, cyano, nitro, amino, methylamino, dimethylamino, halo, trifluoromethyl, loweralkyl, loweralkoxy, sulfamoyl or acetamido, and when n is more than 1 up to 3, R.sub.1 can be the same or different, are disclosed as having gastrokinetic and anti-emetic utility in animals and pharmaceutical compositions therefor. A process for preparing the compounds by oxidation of 1,2-disubstituted-N-(4-pyrazolidinyl)benzamides with a metal hypochlorite is disclosed.

REFERENCES:
patent: 3236858 (1966-02-01), Peterli et al.
patent: 3995044 (1976-11-01), Kabbe et al.
patent: 4207327 (1980-06-01), Lunsford et al.
Knorr et al., Ber., 26, p. 104, (1893).

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