Kappa-opiate agonists for inflammatory bowel disorders
    59.
    发明授权
    Kappa-opiate agonists for inflammatory bowel disorders 失效
    卡帕酸激动剂用于炎症性肠病

    公开(公告)号:US5776972A

    公开(公告)日:1998-07-07

    申请号:US671502

    申请日:1996-06-27

    CPC分类号: A61K31/4025

    摘要: Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders 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, or R.sup.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 bond and Hal is F, Cl, Br or I; and/or physiologically acceptable salts and/or one of its glycosylated derivatives , and at least one physiologically acceptable excipient or auxiliary.

    摘要翻译: 适用于治疗炎症性肠病并含有至少一种式I g 3-7 C原子的化合物或具有4-8个C原子的环烷基烷基的药物制剂,R 2为Ar或R 1和R 2一起为“ R3是H,OH,OA或A,R4是A或可以被Hal,OH,OA,CF3,NO2,NH2,NHA,NHCOA,NHSO2A和/或NA2单取代或二取代的苯基,R5是OH, CH 2 OH,R 6和R 7各自独立地为H,Hal,OH,OA,CF 3,NH 2,NHA,NA 2,NHCOA,NHCONH 2,NO 2或亚甲二氧基,氧基与环上的相邻碳键合,A 是具有1-7个C原子的烷基,Ar是单环或双环芳族基团,其可以任选地在环中含有N,O或S原子,并且可以被A,Hal,OH,OA单取代,二取代或三取代 ,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-, - CH 2 - 或键,Hal为F,Cl,Br或I; 和/或生理上可接受的盐和/或其糖基化衍生物之一,和至少一种生理上可接受的赋形剂或辅助剂。