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    Benzodiazepine antagonistic .beta.-carboline derivatives and compositions thereof
    1.
    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
    2.
    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。

    Pharmacologically active 3-substituted beta-carbolines
    4.
    发明授权
    Pharmacologically active 3-substituted beta-carbolines 失效

    公开(公告)号：US4435403A

    公开(公告)日：1984-03-06

    申请号：US331740

    申请日：1981-12-17

    申请人： Claus T. Braestrup ,  Jogen A. Christensen ,  Mogens Engelstoft ,  Gunter Neef ,  Ulrich Eder ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Dieter Palenschat

    发明人： Claus T. Braestrup ,  Jogen A. Christensen ,  Mogens Engelstoft ,  Gunter Neef ,  Ulrich Eder ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Dieter Palenschat

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/675 ,  A61P25/00 ,  A61P25/20 ,  C07D209/08 ,  C07D209/20 ,  C07D471/04 ,  C07F9/6561 ,  C07D487/14

    CPC分类号： C07D471/04 ,  C07D209/08 ,  C07D209/20 ,  C07F9/6561

    摘要： 3-substituted beta-carbolines of the formula ##STR1## wherein R.sup.C is hydrogen, lower alkyl, alkoxyalkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms, aralkyl of up to 8 C-atoms, or (CH.sub.2).sub.n OR.sup.20wherein R.sup.20 is alkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms or aralkyl of up to 8 C-atoms and n is an integer of 1 to 3;Y is oxygen, two hydrogen atoms or NOR.sup.1,wherein R.sup.1 is hydrogen, lower alkyl, aryl or aralkyl of up to 6 C-atoms, COR.sup.2, wherein R.sup.2 is lower alkyl of up to 6 C-atoms,or Y is CHCOOR.sup.3, wherein R.sup.3 is hydrogen or lower alkylor Y is NNR.sup.4 R.sup.5,wherein R.sup.4 and R.sup.5 can be the same or different and each is hydrogen, lower alkyl, C.sub.6-10 -aryl, C.sub.7-10 -aralkyl or CONR.sup.6 R.sup.7,wherein R.sup.6 and R.sup.7 can be the same or different and each is hydrogen or lower alkyl or R.sup.4 and R.sup.5 together with the connecting N-atom, for a 5- or 6-membered heterocyclic ring which optionally may also contain an O-atom or up to 3 N-atoms and which optionally may be substituted by a lower alkyl group;Z is hydrogen, or alkoxy or aralkoxy each of up to 10 C-atoms and each optionally substituted by hydroxy, or Z is alkyl of up to 6 C-atoms, C.sub.6-10 -aryl or C.sub.7-10 -aralkyl each of which may optionally be substituted by a COOR.sup.8 -- or a CONR.sup.9 R.sup.10 group,wherein R.sup.8 is alkyl of up to 6 C-atoms, and R.sup.9 and R.sup.10 can be the same or different and each is hydrogen or alkyl of up to 6 C-atoms;or Z is NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are as defined above;or Z is NR.sup.11 CHR.sup.12 R.sup.13,wherein R.sup.11 and R.sup.12 each is hydrogen or together form a N.dbd.C double bond,wherein R.sup.13 is C.sub.1-10 -alkyl or NR.sup.14 R.sup.15,wherein R.sup.14 and R.sup.15 are the same or different and each is hydrogen, OH or alkyl or alkoxy each of up to 6 C-atoms,or wherein R.sup.12 and R.sup.13 together are oxygen, in which case, R.sup.11 is hydrogen;or Z is COOR.sup.2 wherein R.sup.2 is as defined above;or Y and Z, together with the connecting C-atom, may form a 5- or 6-membered heterocyclic ring which contains an O-atom, adjoining O- and N-atoms or up to 4 N atoms and which optionally may be substituted by a lower alkyl group, hydroxy or oxo have valuable psychotropic properties which make them useful for example as tranquilizers.

    .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders
    6.
    发明授权
    .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders 失效
    可用于治疗焦虑和相关疾病的β-咔啉-3-羧酸衍生物

    公开(公告)号：US5010077A

    公开(公告)日：1991-04-23

    申请号：US188145

    申请日：1988-04-25

    申请人： Claus T. Braestrup ,  Mogens C. Nielsen ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Henning Schou ,  Ulrich Eder ,  Gunter Neef ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen

    发明人： Claus T. Braestrup ,  Mogens C. Nielsen ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Henning Schou ,  Ulrich Eder ,  Gunter Neef ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen

    IPC分类号： C07D471/04 ,  C07H13/10

    CPC分类号： C07D471/04 ,  C07H13/10

    摘要： A .beta.-carbolin-3-carboxylic acid derivative of the formula ##STR1## wherein: X is oxygen, sulphur or NR.sup.10, wherein R.sup.10 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkenyl, C.sub.3-7 -cycloalkyl or C.sub.3-7 -cycloalkenyl;R.sup.3 is (a) C.sub.1-10 -alkoxy, C.sub.1-10 -alkenyloxy, C.sub.6-10 -aryloxy, C.sub.7-11 -aralkoxy or C.sub.8-12 -aralkenyloxy, each optionally substituted with one or more hydroxy groups, halogen atoms, CF.sub.3 groups, C.sub.1-10 -alkoxy groups or C.sub.2-4 -alkenyloxy groups or each optionally substituted with an amino, di-C.sub.1-6 -alkylamino, C.sub.1-10 -alkoxycarbonyl or C.sub.1-10 -alkenyloxycarbonyl group; or (b) NR.sup.11 R.sup.12, wherein R.sup.11 and R.sup.12 are the same or different and each is (i) hydrogen, (ii) hydroxy, (iii) C.sub.1-10 -alkyl, (iv) C.sub.2-10 -alkenyl, (v) C.sub.6-10 -aryl, (vi) C.sub.7-11 -aralkyl, (vii) C.sub.8-12 -aralkenyl, (viii) C.sub.3-7 -cycloalkyl, or (ix) C.sub.3-7 -cycloalkenyl, each of groups (iii)-(ix) optionally substituted with hydroxy, carboxamido, carboxy, C.sub.1-10 -alkoxycarbonyl or C.sub.1-10 -alkenyloxycarbonyl; or (x) amino optionally substituted with C.sub.1-10 -alkyl, C.sub.2-10 -alkenyl, C.sub.6-10 -aryl, C.sub.7-11 -aralkyl, C.sub.8-12 -aralkenyl, C.sub.3-7 -cycloalkyl or C.sub.3-7 -cycloalkenyl; or wherein R.sup.11 and R.sup.12 together with the connecting nitrogen atom form a 5-, 6- or 7-membered heterocyclic ring, which may also contain one additional N or one O atom, and which may be optionally substituted with the same groups of substituents listed for groups (iii)-(ix) above, with the proviso that R.sup.11 and R.sup.12 cannot both be hydroxy; or wherein X and R.sup.3 together represent a single nitrogen atom;R.sup.4 is hydrogen, C.sub.1-10 -alkyl, C.sub.2-10 -alkenyl, C.sub.3-7 -cycloalkyl, C.sub.3-7 -cycloalkenyl, C.sub.7-10 -aralkyl, C.sub.8-10 -aralkenyl, phenyl, C.sub.7-10 -alkoxyphenyl or C.sub.8-10 -alkenyloxyphenyl;R.sup.A is F, Cl, Br, I, NO.sub.2, NR.sup.13 R.sup.14, NHCOR.sup.13, CN, COOR.sup.13, OR.sup.13, SCH.sub.3 or SO.sub.2 NR.sup.11 R.sup.12, wherein R.sup.13 and R.sup.14 each is hydrogen or C.sub.1-6 -alkyl optionally substituted with hydroxy or halogen; and wherein R.sup.11 and R.sup.12 are as defined above, and wherein there may be 1-4 identical or different R.sup.A 's; andR.sup.9 is hydrogen, C.sub.1-8 -alkyl, C.sub.1-8 -alkenyl, C.sub.1-8 -alkoxycarbonyl, C.sub.1-8 -alkenyloxycarbonyl, or C.sub.1-8 -alkenyloxy;with the proviso that R.sup.11 and R.sup.12 are not both hydrogen, when X is oxygen and when R.sup.4, R.sup.A and R.sup.9 each is hydrogen; that one of R.sup.11 and R.sup.12 is not hydrogen when the other is amino and when X is oxygen and R.sup.4, R.sup.A and R.sup.9 each are hydrogen; and that R.sup.4, R.sup.A and R.sup.9 each is not hydrogen when X is oxygen and R.sup.3 is OCH.sub.3.have valuable pharmacological properties.

    Substituted .beta.-carbolines, and use thereof as medicinal agents
    7.
    发明授权
    Substituted .beta.-carbolines, and use thereof as medicinal agents 失效
    取代的β-咔啉，并将其用作药物

    公开(公告)号：US4623649A

    公开(公告)日：1986-11-18

    申请号：US654594

    申请日：1984-09-26

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

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

    IPC分类号： A61K31/435 ,  A61P25/00 ,  C07D471/04 ,  A61K31/33

    CPC分类号： C07D471/04

    摘要： Novel substituted .beta.-carboline derivatives of Formula I ##STR1## wherein R.sup.3 is an oxadiazolyl residue of the formula ##STR2## wherein R.sup.5 stands for lower alkyl of up to 3 carbon atoms or an ester ##STR3## with R.sup.6 being hydrogen or lower alkyl of up to 3 carbon atoms, R.sup.4 is hydrogen, lower alkyl of up to 3 carbon atoms, or CH.sub.2 OR.sup.9 wherein R.sup.9 is lower alkyl of up to 3 carbon atoms,R.sup.A is phenyl or a hydrocarbon residue containing 2-10 carbon atoms which can be cyclic or acyclic, saturated or unsaturated, branched or unbranched, and which can optionally be substituted by oxo, formyl OH, O-alkyl of up to 3 carbon atoms or phenyl, and wherein, in a cyclic hydrocarbon residue, a CH.sub.2 -group can be replaced by oxygen,exhibit an effect on the central nervous system and thus are suitable as psychopharmaceuticals.

    摘要翻译： 式I的新型取代的β-咔啉衍生物其中R 3是下式的恶二唑基残基，其中R 5表示至多3个碳原子的低级烷基，或者R 6表示氢或 最多3个碳原子的低级烷基，R4是氢，至多3个碳原子的低级烷基或CH2OR9，其中R9是至多3个碳原子的低级烷基，RA是苯基或含2-10个碳原子的烃基， 可以是环状或非环状，饱和或不饱和的，支链或非支链的，并且其可任选被氧代，甲酰基OH，至多3个碳原子的O-烷基或苯基取代，并且其中在环状烃残基中， 组可以被氧代替，对中枢神经系统有影响，因此适合作为心理药物。

    Substituted 5H-pyrimido[5,4-b]indoles
    8.
    发明授权
    Substituted 5H-pyrimido[5,4-b]indoles 失效
    取代的5H-嘧啶并[5,4-b]吲哚

    公开(公告)号：US4564610A

    公开(公告)日：1986-01-14

    申请号：US562248

    申请日：1983-12-16

    申请人： Dieter Rahtz ,  Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Herbert H. Schneider ,  Claus T. Braestrup

    发明人： Dieter Rahtz ,  Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Herbert H. Schneider ,  Claus T. Braestrup

    IPC分类号： A61K31/505 ,  A61P25/00 ,  C07D209/42 ,  C07D487/04 ,  C07F9/6561

    CPC分类号： C07D487/04 ,  C07D209/42 ,  C07F9/6561

    摘要： Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.2 wherein R is C.sub.1-5 -alkyl, exhibit strong affinity for binding to benzodiazepine receptors.The novel compounds are suitable for use in psychopharmaceutical preparations.

    摘要翻译： 取代的式I的5H-嘧啶并[5,4-b]吲哚其中R 2是卤素; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; C 1-5 - 烷基，环烷基，芳烷基或芳基; ORI，nn为0,1或2，或其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基的SO nRI; 其中RII和RIII是氢，C1-5-烷基，C3-5-烯基，环烷基，芳烷基，芳基，或具有连接的N-原子的5-或6-元杂环; RA为氢; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; 卤素，硝基，ORI，nn为0,1或2的SO nRI，其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基; 其中RII和RIII是氢，C1-5烷基，环烷基，C3-5-烯基，芳烷基，芳基，或具有连接的N-原子的5或6元杂环; 或其中R为C 1-5 - 烷基的PO（OR）2表现出对苯并二氮杂受体结合的强亲合力。 新型化合物适用于精神药物制剂。

    Oxadiazolyl-imidazo-[1,4]benzodiazepines and their use in treatment of diseases of the central nervous system
    10.
    发明授权
    Oxadiazolyl-imidazo-[1,4]benzodiazepines and their use in treatment of diseases of the central nervous system 失效
    恶二唑基 - 咪唑并[1,4]苯并二氮杂类及其在治疗中枢神经系统疾病中的应用

    公开(公告)号：US4507313A

    公开(公告)日：1985-03-26

    申请号：US551818

    申请日：1983-11-15

    申请人： Claus T. Braestrup ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Frank Waetjen

    发明人： Claus T. Braestrup ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Frank Waetjen

    IPC分类号： A61K31/55 ,  A61P25/00 ,  C07D487/04 ,  A61K31/555 ,  C07D521/00

    CPC分类号： C07D487/04

    摘要： New oxadiazolyl-imidazo-[1,4]benzodiazepine derivatives having benzodiazepine receptor activity have the formula ##STR1## R' is hydrogen, chlorine, fluorine or nitro in the 7- or 8-position, R.sup.1 is hydrogen or lower alkyl of up to 3 carbon atoms,R.sup.3 is the oxadiazolyl grouping of the formula ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms and A B is a grouping of the formula ##STR3## wherein R.sup.5 is hydrogen or methyl and R'" is hydrogen or chlorine. The compounds possess valuable pharmacological properties. In particular, they act on the central nervous system and are suitable for use in psychopharmaceutical preparations.

    摘要翻译： 具有苯并二氮杂受体活性的新的恶二唑基 - 咪唑并[1,4]苯并二氮杂衍生物在7-或8-位上具有式R 1是氢，氯，氟或硝基，R 1是氢或低级烷基，直到 3个碳原子，R3是式“IMAGE”的恶二唑基，其中R“是具有至多3个碳原子的低级烷基，AB是下式的基团：其中R 5是氢或甲基，R” 是氢或氯。 该化合物具有有价值的药理学性质。 特别是它们作用于中枢神经系统，适用于心理制剂。