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29 条记录 (耗时 0.031 秒)

    Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith
    11.
    发明授权
    Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith 失效
    恶二唑基咪唑并二氮杂衍生物药物组合物及其处理方法

    公开(公告)号：US4670433A

    公开(公告)日：1987-06-02

    申请号：US837100

    申请日：1986-03-06

    申请人： Frank Watjen ,  Mogens Engelstoft ,  John B. Hansen ,  Leif H. Jensen

    发明人： Frank Watjen ,  Mogens Engelstoft ,  John B. Hansen ,  Leif H. Jensen

    IPC分类号： C07D20060101 ,  C07D271/06 ,  C07D487/04 ,  C07D487/14 ,  A61K31/555

    CPC分类号： C07D271/06 ,  C07D487/04 ,  C07D487/14

    摘要： New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 - cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.

    摘要翻译： 具有式“IMAGE”的新的恶二唑基咪唑并二氮杂衍生物，其中R 3具有式“IMAGE”，其中R“是氢，C 1-6烷基C 1-6烷氧基甲基或C 3-6 - 环烷基; R4是氢; R5是C1-6烷基或R4和R5一起形成2-4元亚烷基桥; RA是C 1-6烷基，C 1-6烷氧基或C 1-3三氟烷基，其药物组合物及其处理方法。 化合物和药物组合物可用于改善，缓解或消除与苯二氮卓类受体相关的中枢神经系统疾病，特别是抗惊厥药，抗焦虑药，催眠药和嗜酸剂。

    .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.

    Pharmacologically active 3-substituted beta-carbolines
    14.
    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.

    Oxadiazolyl-imidazo-[1,4]benzodiazepines and their use in treatment of diseases of the central nervous system
    20.
    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。