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    .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders
    12.
    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.

    Process for the preparation of 4-alkoxyalkyl .beta.-carbolines
    19.
    发明授权
    Process for the preparation of 4-alkoxyalkyl .beta.-carbolines 失效
    4-烷氧基烷基β-咔啉的制备方法

    公开(公告)号：US4945163A

    公开(公告)日：1990-07-31

    申请号：US238086

    申请日：1988-08-30

    申请人： Andreas Huth ,  Dieter Rahtz ,  Ralph Rohde ,  Ralph Schmiechen ,  Dieter Seidelmann

    发明人： Andreas Huth ,  Dieter Rahtz ,  Ralph Rohde ,  Ralph Schmiechen ,  Dieter Seidelmann

    IPC分类号： B01J27/12 ,  C07B61/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： A process is disclosed for the preparation of 4-alkoxyalkyl .beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is an optionally substituted aliphatic hydrocarbon residue,R.sup.3 is lower alkyl, andR.sup.A is hydrogen, halogen, COOR.sup.4 or OR.sup.5, R.sup.4 meaning lower alkyl and R.sup.5 meaning hydrogen, lower alkyl, cycloalkyl, or optionally substituted pheny,by reaction of a compound of Formula II in the presence of AgBF.sub.4 with an alcohol of the formula R.sup.2 OH wherein R.sup.2 has the meanings given above.

    摘要翻译： 公开了用于制备通式I的4-烷氧基烷基β-咔啉衍生物的方法，其中R1是氢或甲基，R2是任选取代的脂族烃残基，R3是低级烷基，RA是氢，卤素 COOR4或OR5，R4表示低级烷基，R5表示氢，低级烷基，环烷基或任选取代的苯基，通过式Ⅱ化合物在AgBF 4存在下与式R 2 OH的醇反应，其中R2具有给定的含义 以上。

    Isoxazole-.beta.-carboline derivatives
    20.
    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。