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    Phenoxy-substituted beta-carboline derivatives, their production and their use as drugs
    2.
    发明授权
    Phenoxy-substituted beta-carboline derivatives, their production and their use as drugs 失效
    苯氧基取代的β-咔啉衍生物，其生产和用作药物

    公开(公告)号：US4945090A

    公开(公告)日：1990-07-31

    申请号：US929861

    申请日：1986-11-13

    申请人： Ralph Schmiechen ,  Dieter Seidelmann ,  Andreas Huth ,  Herbert H. Schneider ,  David N. Stephens ,  Mogens Engelstoft ,  John B. Hansen ,  Erling Petersen

    发明人： Ralph Schmiechen ,  Dieter Seidelmann ,  Andreas Huth ,  Herbert H. Schneider ,  David N. Stephens ,  Mogens Engelstoft ,  John B. Hansen ,  Erling Petersen

    IPC分类号： A61K31/435 ,  A61P25/08 ,  A61P25/20 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Phenoxy-substituted beta-carbolines of the formula I ##STR1## X is COOR.sup.3, CONHC.sub.1-3 -alkyl or oxadiazolyl of the formula ##STR2## R.sup.2 is H, lower alkyl or cycloalkyl, R.sup.3 is lower alkyl,R.sup.4 is hydrogen, lower alkyl or lower alkoxyalkyl,R.sup.1 is hydrogen, halogen, lower alkyl, lower alkoxy, acyl, phenyl, C.sub.2-5 alkylenedioxy, trifluoromethyl, nitrilo, nitro, lower alkoxycarbonyl, azido, SO.sub.2 R.sup.6, SO.sub.2 NR.sup.7 R.sup.8, or NR.sup.9 R.sup.10,R.sup.6 is lower alkyl,R.sup.7 and R.sup.8 independently are lower alkyl or together with the nitrogen atom form a hetero ring,R.sup.9 and R.sup.10 independently are hydrogen, lower alkyl, acyl or together with the nitrogen atom form a hetero ring system,with the proviso that X is not COOEt, if ##STR3## is 5-phenoxy and R.sup.4 is methyl or ##STR4## is 6-(4-methoxyphenoxy) and R.sup.4 is methoxymethyl have valuable pharmacological properties.

    摘要翻译： 式I的苯氧基取代的β-咔啉（I）X是下式的COOR3，CONHC1-3-烷基或恶二唑基，R 2是H，低级烷基或环烷基，R 3是低级烷基，R 4是氢 低级烷基或低级烷氧基烷基，R1为氢，卤素，低级烷基，低级烷氧基，酰基，苯基，C2-5亚烷基二氧基，三氟甲基，次氮基，硝基，低级烷氧基羰基，叠氮基，SO2R6，SO2NR7R8或NR9R10，R6为低级烷基 ，R7和R8独立地是低级烷基或与氮原子一起形成杂环，R9和R10独立地是氢，低级烷基，酰基或与氮原子一起形成杂环体系，条件是X不是COOEt （a）为5-苯氧基，R4为甲基或（b）为6-（4-甲氧基苯氧基），R4为甲氧基甲基具有有价值的药理学性质。

    Isoxazole-.beta.-carboline derivatives
    3.
    发明授权
    Isoxazole-.beta.-carboline derivatives 失效
    异恶唑-β-咔啉衍生物

    公开(公告)号：US4933345A

    公开(公告)日：1990-06-12

    申请号：US237368

    申请日：1988-08-29

    申请人： Andreas Huth ,  Dieter Rahtz ,  Ralph Rohde ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Herbert Schneider ,  David N. Stephens ,  John B. Hansen ,  Mogens Engelstoft ,  Preben Olsen

    发明人： Andreas Huth ,  Dieter Rahtz ,  Ralph Rohde ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Herbert Schneider ,  David N. Stephens ,  John B. Hansen ,  Mogens Engelstoft ,  Preben Olsen

    IPC分类号： A61K31/435 ,  A61K31/437 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： .beta.-Carbolines of general Formula I ##STR1## wherein Y represents the residue ##STR2## and R.sup.a and R.sup.b, being identical or different, mean respectively hydrogen, C.sub.1-6 -alkoxy, phenyl, C.sub.3-7 -cyclo-alkyl, optionally substituted C.sub.1-6 -alkyl or C.sub.1-6 -alkoxycarbonyl, and R.sup.c and R.sup.d, being identical or different, mean respectively hydrogen or C.sub.1-6 -alkyl or jointly a linkage, andR.sup.4 is hydrogen, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl andR.sup.5 is hydrogen, halogen, OR.sup.6, NR.sup.7 R.sup.8 or CH R.sup.9 R.sup.10 wherein R.sup.6 means C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or an optionally substituted aralkyl, aryl or hetaryl residue, R.sup.7 and R.sup.8, being identical or different, represent hydrogen, C.sub.1-6 -alkyl, C.sub.3-6 -alkenyl, or jointly with the nitrogen atom a saturated heterocyclic five- or six-membered ring which optionally contains a further hetero atom, R.sup.9 means hydrogen or C.sub.1-6 -alkyl, R.sup.10 means hydrogen, C.sub.1-6 -alkyl, OR.sup.11 or NR.sup.12 R.sup.13 wherein R.sup.11 means C.sub.1-6 -alkyl, R.sup.12 and R.sup.13 are identical or different and mean hydrogen, C.sub.1-6 -alkyl or jointly with the nitrogen atom a saturated heterocyclic five- or six-membered ring optionally containing a further hetero atom, are useful to treat epilepsy or anxiety.

    摘要翻译： 其中Y表示残基，且R a和R b相同或不同，分别表示氢，C 1-6 - 烷氧基，苯基，C 3-7 - 环烷基， 任选取代的C 1-6 - 烷基或C 1-6 - 烷氧基羰基，R c和R d相同或不同，分别表示氢或C 1-6 - 烷基或联合键，并且R 4是氢，C 1-6 - 烷基或C 1 - R6-烷氧基-C1-6-烷基，R5为氢，卤素，OR6，NR7R8或CH R9R10，其中R6表示C1-6烷基，C3-7-环烷基或任选取代的芳烷基，芳基或杂芳基，R7和 R8相同或不同，表示氢，C 1-6 - 烷基，C 3-6 - 烯基，或与氮原子一起为饱和杂环五元或六元环，任选地含有另外的杂原子，R9表示氢或 C 1-6 - 烷基，R 10表示氢，C 1-6 - 烷基，OR 11或NR 12 R 13，其中R 11表示C 1-6 - 烷基，R 12和R 13相同或不同，表示氢，C 1-6 - 烷基或联合 氮原子饱和的杂环五或六元环任选地含有另外的杂原子，可用于治疗癫痫或焦虑。

    Tetrahydro-beta-carbolines, and their use as drugs
    8.
    发明授权
    Tetrahydro-beta-carbolines, and their use as drugs 失效
    四氢-β-咔啉，它们用作药物

    公开(公告)号：US4855295A

    公开(公告)日：1989-08-08

    申请号：US915357

    申请日：1986-10-06

    申请人： Helmut Biere ,  Mogens Engelstoft ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen ,  Dieter Seidelmann ,  David N. Stephens

    发明人： Helmut Biere ,  Mogens Engelstoft ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen ,  Dieter Seidelmann ,  David N. Stephens

    IPC分类号： A61K31/435 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： 5,6,7,8-tetrahydro-beta-carbolines derivatives of formula I ##STR1## wherein R.sup.1 is an oxadiazolyl radical of the formula ##STR2## COOR.sup.3 or CONR.sup.4 R.sup.5, R.sup.2 is H, lower alkyl or cycloalkyl,R.sup.3 is H or lower alkyl,R.sup.4 and R.sup.5 are H or lower alkyl, whereby R.sup.4 and R.sup.5 cannot be hydrogen at the same time, or R.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 5- or 6-member ring, which additionally can contain a heteroatom, andR.sup.A is hydrogen, .dbd.O, cycloalkyl, --COOR.sup.3 with R.sup.3 having the above-mentioned meanings, or lower alkyl, which optionally can be substituted by OH, halogen, lower alkoxy, phenyl, phenyloxy, --NR.sup.4 R.sup.5, whereby R.sup.4 and R.sup.5 have the above-mentioned meanings, and R.sup.B can be hydrogen, lower alkyl or lower alkoxyalkyl,have valuable pharmacological properties.

    摘要翻译： 式I的5,6,7,8-四氢-β-咔啉衍生物其中R 1是下式的恶二唑基，COOR 3或CONR 4 R 5，R 2是H，低级烷基或环烷基，R 3是 H或低级烷基，R 4和R 5是H或低级烷基，其中R 4和R 5不能同时为氢，或者R 4和R 5与相邻的氮原子一起形成5-或6-元环，其另外可以含有 杂原子，RA是氢，= O，环烷基，具有上述含义的R 3的-COOR 3或任选被OH，卤素，低级烷氧基，苯基，苯氧基，-NR 4 R 5取代的低级烷基，其中R 4 并且R 5具有上述含义，RB可以是氢，低级烷基或低级烷氧基烷基，具有有价值的药理学性质。

    Benzodiazepine antagonistic .beta.-carboline derivatives and compositions thereof
    9.
    发明授权
    Benzodiazepine antagonistic .beta.-carboline derivatives and compositions thereof 失效
    苯并二氮对抗β-咔啉衍生物及其组合物

    公开(公告)号：US4600715A

    公开(公告)日：1986-07-15

    申请号：US623671

    申请日：1984-06-22

    申请人： Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Dieter Rahtz ,  Mogens Engelstoft ,  Claus T. Braestrup

    发明人： Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Dieter Rahtz ,  Mogens Engelstoft ,  Claus T. Braestrup

    IPC分类号： C07D471/10 ,  A61K31/435 ,  A61K31/437 ,  A61P25/00 ,  A61P25/18 ,  C07D471/04 ,  A61K31/68 ,  A61K31/535 ,  C07D403/06 ,  C07D471/06

    CPC分类号： C07D471/04

    摘要： .beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.3 is ##STR2## wherein R.sup.5 is C.sub.1-5 alkyl, R.sup.6 is lower alkyl, aralkyl, or alkoxyalkyl of up to 7 carbon atoms, and R.sup.7 and R.sup.8 are hydrogen C.sub.1-5 alkyl, or, collectively with the amido nitrogen atom, piperidino,R.sup.4 is hydrogen, C.sub.1-3 alkyl, or CH.sub.2 OR.sup.9 wherein R.sup.9 is C.sub.1-3 alkyl, atoms, andR.sup.A is --COOR.sup.10 ##STR3## wherein R.sup.10 is hydrogen, lower alkyl, alkoxyalkyl or alkenyl of up to 5 carbon atoms, or benzyl, or X is oxygen or sulfur, and R.sup.11 and R.sup.12 each are hydrogen, lower alkyl or alkenyl or, collectively with the amido nitrogen atom, represent a hetero ring, are prepared by conventional methods and exhibit, inter alia, an effect on the central nervous system and are suitable for use as psychopharmaceuticals.

    摘要翻译： 通式Ⅰ的咔啉衍生物，其中R 3是R 5是C 1-5烷基，R 6是至多7个碳原子的低级烷基，芳烷基或烷氧基烷基，R 7和R 8是氢 C 1-5烷基，或与酰氨基氮原子一起为哌啶子基，R 4为氢，C 1-3烷基或CH 2 OR 9，其中R 9为C 1-3烷基，原子，RA为-COOR 10，其中R 10为氢， 至多5个碳原子的低级烷基，烷氧基烷基或链烯基，或苄基，或X为氧或硫，R11和R12各自为氢，低级烷基或烯基，或与酰氨基氮原子一起为杂环 通过常规方法制备并显示出对中枢神经系统的影响，并且适合用作心理药物。

    .beta.-carbolines and their use as medicinal agents
    10.
    发明授权
    .beta.-carbolines and their use as medicinal agents 失效
    β-咔啉及其作为药物的用途

    公开(公告)号：US4894377A

    公开(公告)日：1990-01-16

    申请号：US3179

    申请日：1987-01-14

    申请人： Dieter Seidelmann ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Claus T. Braestrup ,  Mogens Engelstoft

    发明人： Dieter Seidelmann ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Claus T. Braestrup ,  Mogens Engelstoft

    IPC分类号： A61K31/404 ,  A61K31/435 ,  A61K31/437 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  C07D213/40 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： .beta.-Carbolines of general Formula I ##STR1## wherein R.sup.3 is ##STR2## or --COOR", wherein R' is C.sub.1-3 alkyl or C.sub.3-6 cycloalkyl and R" is C.sub.1-4 alkyl; R.sup.4 is hydrogen, methyl, ethyl or methoxymethyl; and R.sup.A is ##STR3## wherein X is C.sub.1-12 straight-chain, branched-chain, saturated or unsaturated alkyl or a corresponding alkyl group with a CH.sub.2 -group substituted by a carbonyl group and R"" is one or more of fluorine, chlorine, bromine, or iodine, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-5 acyloxy, phenyl, C.sub.2-5 alkylenedioxy, trifluoromethyl, nitrilo, nitro or --NR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V, which can be the same or different are hydrogen, C.sub.1-3 alkyl, C.sub.1-5 acyl or phenyl, or collectively with the amido nitrogen atom form a 3- to 6-membered hetero ring, which are prepared conventionally by esterifying a corresponding compound wherein R.sup.A is H or R.sup.3 is --COOH, exhibit effects on the central nervous system and can be used as psychorharmaceuticals.

    摘要翻译： 其中R 3是“或”-COOR“，其中R'是C 1-3烷基或C 3-6环烷基，R”是C 1-4烷基的通式I的化合物< R4是氢，甲基，乙基或甲氧基甲基; 并且RA是，其中X是C 1-12直链，支链，饱和或不饱和的烷基或具有被羰基取代的CH 2 - 的相应烷基，并且R“ 氟，氯，溴或碘，C1-3烷基，C1-3烷氧基，C1-5酰氧基，苯基，C2-5亚烷基二氧基，三氟甲基，次氮基，硝基或-NRIVRV，其中RIV和RV可以相同或 不同的是氢，C 1-3烷基，C 1-5酰基或苯基，或与酰氨基氮原子一起形成3至6元杂环，其通常通过酯化相应的化合物，其中RA是H或R3是 -COOH表现出对中枢神经系统的作用，可用作精神药物。