Tocolytic oxytocin receptor antagonists

Details Tocolytic oxytocin receptor antagonists Tocolytic oxytocin receptor antagonists

1997-01-06

1998-03-10

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544 73, 544 92, C07D26512, A61K 31535

Patent

active

057261725

ABSTRACT:
This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery. A typical compound is as follows: ##STR1##

REFERENCES:
patent: 4344945 (1982-08-01), Teranishi et al.
patent: 5225402 (1993-07-01), Ogawa et al.
patent: 5356904 (1994-10-01), Freidinger et al.
Chemical Abstract 125:221854 for WO96/22775 (Aug. 1, 1996), Williams et al., with Registry file printout of compounds.
J. Med. Chem., "Communications to the Editor" (1995) 38, 4634-4636, Williams et al.
Am. J. Perinatol., "Treatment of Preterm Labor with the Oxytocin Antagonist Atosiban" (1996) 13, 143-146, Goodwin et al.
Am J. Obstet. Gynecol., "The effect of the oxytocin antagonist atosiban on preterm uterine activity in the human" (1994) 170, 474-478, Goodwin et al.

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