162045-86-5Relevant articles and documents
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).
Tocolytic oxytocin receptor antagonists
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, (2008/06/13)
Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is STR1 Y is --SO2 --, --(CH2)p -- or --CO--(CH2)p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R5, R6 or R7 ; R1 is hydrogen, cyano, phenyl,--CONHR2, --CONR2 R2, --(CH2)m --OR2, --(CH2)p --S(O)r --R2, --(CH2)m --CO2 R2, --(CH2)m --N3, --(CH2)m --NH2 or --(CH2)m --NR2 R2 ; R2 is hydrogen, C3-8 cycloalkyl or C1-5 alkyl; R5 and R6 are each independently selected from hydrogen, C1-5 alkoxy, halogen or --(CH2)n --N(R2)--C(O)--R18 ; R7 is hydrogen or STR2 R11 is selected from hydrogen, C1-5 alkylcarbonyl, STR3 or substituted C1-5 alkyl wherein said alkyl substituent is unsubstituted, mono-, di- or tri-substituted pyridyl wherein said substitutents on said pyridyl are independently selected from halogen, C1-5 alkyl or C1-5 alkoxyl; R13 is unsubstituted or substituted C1-10 alkyl wherein the substituent is selected from --N(R2)2, --NHR2 or imidazolyl; R14 and R15 are each independently selected from C1-5 alkyl, C1-5 alkoxy or halogen; R16 is hydrogen or oxo; R18 is C1-5 alkoxyl, unsubstituted or substituted C1-5 alkyl where said substituent is Het, unsubstituted or substituted C2-5 alkenyl where said subsituent is Het or Het; Het is benzimidazolyl, carboxymethyl-substituted benzimidazolyl or indolyl; m is an integer of from 1 to 5; p is an integer of from 1 to 3; and r is an integer of from 0 to 2. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
