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    • 3. 发明授权
    • Derivatives of asimadoline with covalently bonded acids
    • 具有共价键的酸的阿莫达林的衍生物
    • US07385065B2
    • 2008-06-10
    • US10539256
    • 2003-11-25
    • Matthias WiesnerChristoph Seyfried
    • Matthias WiesnerChristoph Seyfried
    • C07D207/12
    • C07D207/12
    • The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of these derivatives for the preparation of a medicament, to the use of these derivatives for the preparation of a pharmaceutical composition, to a process for the preparation of the pharmaceutical compositions, to pharmaceutical compositions obtainable by this process, and to a process for the treatment of diseases which comprises the administration of the pharmaceutical composition.
    • 本发明涉及具有共价键的酸的N-甲基-N - [(1S)-1-苯基-2 - ((3S)-3-羟基吡咯烷-1-基)乙基] -2,2-二苯基乙酰胺的衍生物, 以及其盐,溶剂合物和前药,作为药物的衍生物,使用这些衍生物用于制备药物,将这些衍生物用于制备药物组合物的方法,用于制备 药物组合物,可通过该方法获得的药物组合物,以及用于治疗包括施用药物组合物的疾病的方法。
    • 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.