| 摘要 |
Compounds of the formula X-Y-R, or the pharmaceutically acceptable salts and esters thereof, wherein X is <IMAGE> 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, -CONR2R2, -(CH2)m-OR2, -(CH2)p-S(O)r-R2, -(CH2)m-CO2R2, -(CH2)m-N3, -(CH2)m-NH2 or -(CH2)m-NR2R2; 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 <IMAGE> R11 is selected from hydrogen, C1-5 alkylcarbonyl, <IMAGE> 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.
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