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    Isoxazole-.beta.-carboline derivatives
    2.
    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。

    Imidazole derivatives
    4.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号：US4952698A

    公开(公告)日：1990-08-28

    申请号：US189511

    申请日：1988-04-11

    申请人： Helmut Biere ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Herbert H. Schneider ,  David N. Stephens

    发明人： Helmut Biere ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Herbert H. Schneider ,  David N. Stephens

    IPC分类号： A61K31/415 ,  A61P21/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/20 ,  C07D233/90 ,  C07D413/00 ,  C07D413/04

    CPC分类号： C07D413/04 ,  C07D233/90

    摘要： Imidazole derivatives of general formula I ##STR1## wherein R.sup.1 represents hydrogen or halogen in the o-, m- or p-position, and the halogen can occur once or repeatedly in the phenyl radical,R.sup.4 represents ##STR2## with R.sup.6 and R.sup.9 representing hydrogen or a straight or branched alkyl group with 1 to 6 carbon atoms, R.sup.7 and R.sup.8 are the same or different and represent hydrogen or a straight or branched alkyl group with 1 to 6 carbon atoms or R.sup.7 and R.sup.8 together with the nitrogen atom represent a saturated heterocyclic five-membered or six-membered ring optionally containing another heteroatom, andR.sup.5 represents hydrogen, an alkyl group with 1 to 6 carbon atoms or an alkoxyalkyl group with 1 to 6 carbon atoms, which are suitable as psychopharmaceuticals, are described.

    摘要翻译： PCT No.PCT / DE87 / 00342 Sec。 371日期：1988年4月11日 102（e）日期1988年4月11日PCT提交1987年7月30日PCT公布。 公开号WO88 / 01268 PCT 日期：1988年2月25日。通式I的咪唑衍生物其中R 1表示氢或卤素在邻 - ，间或对 - 位和卤素可以在苯基中一次或重复出现， R 4表示，其中R 6和R 9表示氢或具有1至6个碳原子的直链或支链烷基，R 7和R 8相同或不同，表示氢或具有1至6个碳原子的直链或支链烷基 碳原子或R 7和R 8与氮原子一起表示任选含有其它杂原子的饱和杂环五元或六元环，R 5表示氢，具有1至6个碳原子的烷基或具有1至6个碳原子的烷氧基烷基 描述了适合作为心理药物的碳原子。

    Phenoxy-substituted beta-carboline derivatives, their production and their use as drugs
    6.
    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。

    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。