N-Acyl hexahydroindole-2-carboxylic acids and anti-hypertensive use
thereof
    2.
    发明授权
    N-Acyl hexahydroindole-2-carboxylic acids and anti-hypertensive use thereof 失效
    N-酰基六氢吲哚-2-羧酸及其抗高血压用途

    公开(公告)号:US4562202A

    公开(公告)日:1985-12-31

    申请号:US477333

    申请日:1983-03-21

    摘要: The invention relates to compounds of the formula I ##STR1## in which n denotes 0 or 1,R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, which each can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined in the aforegoing, a monocyclic or bicyclic sulfur or oxygen and/or nitrogen heterocyclic radical, or a side chain of a naturally occurring aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or arylalkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which is monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy or 3-indolyl,and their physiologically acceptable salts, processes for their preparation, agents containing these and their use as medicaments and also bicyclic amino acids as their intermediates and processes for their preparation.

    摘要翻译: 本发明涉及式I的化合物,其中n表示0或1,R表示氢,烷基或芳烷基,R1表示氢或烷基,其可任选被氨基,酰氨基或苯甲酰基氨基取代, ,环烷基,环烯基,环烷基烷基,芳基或部分氢化的芳基,其各自可以被烷基,烷氧基或卤素,芳基烷基或芳酰基烷基取代,二者可以在如上所定义的芳基中被取代,单环或双环硫 或氧和/或氮杂环基或天然存在的氨基酸的侧链,R 2表示氢,烷基,烯基或芳烷基,Y表示氢或羟基,Z表示氢或Y,Z一起表示氧,X表示烷基, 烯基,环烷基,芳基,其被烷基,烷氧基,羟基,卤素,硝基,氨基,烷基氨基,二烷基氨基或亚甲二氧基或3-吲哚基单取代或三取代,及其生理学 表盐,其制备方法,含有这些物质的药剂及其作为药物的用途以及双环氨基酸作为其中间体及其制备方法。

    Derivatives of bicyclic aminoacids agents containing these compounds and
their use
    8.
    发明授权
    Derivatives of bicyclic aminoacids agents containing these compounds and their use 失效
    含有这些化合物的双环氨基酸试剂的衍生物及其用途

    公开(公告)号:US4933361A

    公开(公告)日:1990-06-12

    申请号:US346339

    申请日:1989-04-28

    摘要: 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.

    摘要翻译: 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。

    Derivatives of cis, endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid,
and their use for treating hypertension
    10.
    发明授权
    Derivatives of cis, endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid, and their use for treating hypertension 失效
    顺式,内-2-氮杂双环[5.3.0]癸烷-3-羧酸的衍生物及其用于治疗高血压的用途

    公开(公告)号:US4714708A

    公开(公告)日:1987-12-22

    申请号:US561230

    申请日:1983-12-14

    摘要: The invention relates to derivatives of cis,endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid of the formula I ##STR1## in which R denotes hydrogen, alkyl, alkenyl or aralkyl, R.sup.1 denotes hydrogen, allyl, vinyl or a side chain of an optionally protected naturally occurring .alpha.-aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen, X denotes alkyl, alkenyl, cycloalkyl, aryl which can be substituted once, twice or three times by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, and their physiologically acceptable salts, a process for their preparation, agents containing them and their use.

    摘要翻译: 本发明涉及式I(I)的顺式,内-2-氮杂双环[5.3.0]癸烷-3-羧酸衍生物,其中R表示氢,烷基,烯基或芳烷基,R1表示氢, 烯丙基,乙烯基或任选保护的天然α-氨基酸的侧链,R2表示氢,烷基,烯基或芳烷基,Y表示氢或羟基,Z表示氢,或Y和Z一起表示氧,X表示烷基,烯基 烷氧基,羟基,卤素,硝基,氨基,烷基氨基,二烷基氨基或亚甲基二氧基取代一次,两次或三次的芳基,或表示吲哚-3-基,及其生理上可接受的盐, 他们的准备,包含他们的代理和他们的使用。