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    • 10. 发明授权
    • Kappa-opiate agonists effective in the treatment of postoperative ileus
    • 卡帕阿片激动剂有效治疗术后肠梗阻
    • US5977161A
    • 1999-11-02
    • US27228
    • 1998-02-20
    • Andrew BarberChristoph SeyfriedGerd BartoszykRudolf Gottschlich
    • Andrew BarberChristoph SeyfriedGerd BartoszykRudolf Gottschlich
    • C07D207/08A61K31/135A61K31/165A61K31/40A61K31/4015A61K31/4025A61P1/00A61P1/04A61P29/00A61P43/00C07D207/12
    • A61K31/4025
    • Disclosed herein are pharmaceutical preparations which are suitable for the treatment of postoperative ileus and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sub.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 NH--, --CH.sub.2 --NA-- or a bondandHal is F, Cl, Br or I.
    • 本文公开了适用于治疗术后肠梗阻并含有至少一种其中R 1为Ar的式I化合物或具有3-7个C原子的环烷基或具有4-8个C原子的环烷基烷基,R2为Ar, 或R 1和R 2一起为R 3为H,OH,OA或A,R 4为A或可任选被Hal,OH,OA,CF 3,NO 2,NH 2,NHA,NHCOA,NHSO 2 A单取代或二取代的苯基和/或 NA2,R5分别为H,Hal,OH,OA,CF3,NH2,NHA,NA2,NHCOA,NHCONH2,NO2或亚甲二氧基的OH,CH2OH,R6和R7彼此独立地键合, A是具有1-7个C原子的烷基,Ar是可以在环中任选含有N,O或S原子的单环或双环芳族基团,并且可以被A, ,Hal,OH,OA,CF 3,NH 2,NHA,NA 2,NHCOA和/或NHCONH 2,D是CH 2,O,S,NH,NA,-CH 2 -CH 2 - , - CH = CH-, - CH 2 NH-, CH2-NA-或键,Hal为F,Cl,Br或I.