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    • 45. 发明授权
    • Derivatives of bicyclic aminoacids agents containing these compounds and
their use
    • 含有这些化合物的双环氨基酸试剂的衍生物及其用途
    • US4933361A
    • 1990-06-12
    • US346339
    • 1989-04-28
    • Hansjorg UrbachRainer HenningVolker TeetzRolf GeigerReinhard BeckerHolger Gaul
    • Hansjorg UrbachRainer HenningVolker TeetzRolf GeigerReinhard BeckerHolger Gaul
    • A61K38/55A61K31/40A61K31/403A61K31/404A61K38/00A61P7/10A61P9/08A61P9/12C07D209/02C07D209/08C07D209/32C07D209/34C07D209/42C07D209/52C07D215/22C07D215/227C07K1/02C07K1/113C07K5/02C07K5/06
    • C07D215/227C07D209/08C07D209/34C07D209/42C07D209/52C07K5/0222A61K38/00
    • Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0, 1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally be substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.6 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4 -alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process of the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.
    • 公开了式I的顺式,外转和反式化合物,其中n表示0,1或2,R 1表示氢,可任选被氨基取代的(C 1 -C 6) - 烷基,(C 1 -C 6 - (C 5 -C 9) - 环烷基,(C 5 -C 9) - 环烯基,(C 5 -C 7) - 环烷基 - (C 1 -C 4) - 烷基,芳基或 部分氢化的芳基,在每种情况下均可被(C 1 -C 2) - 烷基,(C 1 -C 2) - 烷氧基或卤素,芳基 - (C 1 -C 4) - 烷基取代, 在芳基/,单环或双环硫或氮和/或氮杂环基或天然存在的氨基酸的侧链中,R 2表示氢,(C 1 -C 6) - 烷基,(C 2 -C 6) - 烯基或芳基 - (C1-C4) - 烷基,Y表示氢或羟基,Z表示氢或Y,Z表示氧,X表示(C1-C6) - 烷基,(C2-C6) - 烯基,(C6-C9) 环烷基或芳基,其可以被(C 1 -C 4) - 烷基,(C 1 -C 4) - 烷氧基,羟基,卤素,硝基,氨基,(C 1 -C 4) 烷基氨基,二 - (C 1 -C 4 - 烷基氨基或亚甲二氧基或吲哚-3-基)或其生理上可接受的盐,其制备方法,含有它们的试剂,它们作为药物的用途和制备它们的中间体。