194982-54-2Relevant academic research and scientific papers
Tocolytic oxytocin receptor antagonists
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, (2008/06/13)
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 in mammals, especially humans. 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.
Nonpeptide oxytocin antagonists: Analogs of L-371,257 with improved potency
Williams, Peter D.,Bock, Mark G.,Evans, Ben E.,Freidinger, Roger M.,Gallicchio, Steven N.,Guidotti, Maribeth T.,Jacobson, Marlene A.,Michelle S, Kuo,Levy, Michelle R.,Edward V, Lis,Michelson, Stuart R.,Pawluczyk, Joseph M.,Perlow, Debra S.,Pettibone, Douglas J.,Quigley, Amy G.,Reiss, Duane R.,Salvatore, Christopher,Stauffer, Kenneth J.,Woyden, Carla J.
, p. 1311 - 1316 (2007/10/03)
Structure-activity studies on the oxytocin antagonist 1 (L-371,257; K(i) = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly improved potency in vitro and in vivo, e.g., compound 8 (L-374,943; K(i) = 1.4 nM).
