162045-85-4Relevant academic research and scientific papers
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.
