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11. 发明授权

US5700808A 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters 失效
标题翻译： 5-或6-取代的β-咔啉-3-羧酸酯
公开(公告)号：US5700808A
公开(公告)日：1997-12-23
申请号：US245278
申请日：1994-05-18
申请人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert Hans Schneider , Mogens Engelstoft , Bondo John Hansen , Frank Waetjen , Tage Honore
发明人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert Hans Schneider , Mogens Engelstoft , Bondo John Hansen , Frank Waetjen , Tage Honore
IPC分类号： C07D487/04 , A61K31/435 , A61K31/437 , A61P25/18 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, and R.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.
摘要翻译：式I的5-或6-取代的β-咔啉-3-羧酸酯其中R 1是氢，次氮基，卤素，低级烷基或低级烷氧基，R 3是任选被取代的支链C 3-6烷基通过卤素或任选被甲基取代的C 3-6环烷基是有价值的药物。

12. 发明授权

US4778800A 3-oxadiazole and 3-carboxylic acid beta-carboline derivatives, and their use as psychotropic agents 失效
标题翻译： 3-恶二唑和3-羧酸β-咔啉衍生物，以及它们作为精神药物的用途
公开(公告)号：US4778800A
公开(公告)日：1988-10-18
申请号：US929866
申请日：1986-11-13
申请人： Andreas Huth , Ralph Schmiechen , David N. Stephens , Mogens Engelstoft , Frank Waetjen , John B. Hansen , Leif H. Jensen
发明人： Andreas Huth , Ralph Schmiechen , David N. Stephens , Mogens Engelstoft , Frank Waetjen , John B. Hansen , Leif H. Jensen
IPC分类号： A61K31/435 , A61P25/08 , A61P25/20 , C07D471/04 , A61K31/40
CPC分类号： C07D471/04
摘要： Compounds of formula I ##STR1## wherein X is COOR.sup.3 or an oxadiazolyl radical of the formula orR.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.A is -CHR.sup.1 -Z-R.sup.5,Z is sulfur or oxygen,R.sup.1 is lower alkyl or optionally substituted phenyl, and R.sup.5 is hydrogen, phenyl or optionally substituted lower alkyl,and wherein each compound can contain 1 or 2 R.sup.A radicals have valuable pharmacological properties.
摘要翻译：式I的化合物其中X为COOR 3或下式的二恶唑基或R 2为H，低级烷基或环烷基，R 3为低级烷基，R 4为氢，低级烷基或低级烷氧基烷基，RA为-CHR 1 -Z-R5，Z是硫或氧，R1是低级烷基或任选取代的苯基，R 5是氢，苯基或任选取代的低级烷基，并且其中每个化合物可以含有1或2个RA基团具有有价值的药理学性质。

13. 发明授权

US4371536A .beta.-Carbolin-3-carboxylic acid derivatives 失效
标题翻译： β-链球蛋白-3-羧酸衍生物
公开(公告)号：US4371536A
公开(公告)日：1983-02-01
申请号：US182244
申请日：1980-08-28
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 , A61K31/435 , C07D487/14
CPC分类号： C07D471/04 , C07H13/10
摘要： A .beta.-carbolin-3-carboxylic acid derivative of the formula ##STR1## has valuable pharmacological properties when administered to patients, e.g. humans as a drug, have been shown to possess interesting tranquilizing activity.
摘要翻译：当向患者施用时，式“IMAGE”的β-咔啉-3-羧酸衍生物具有有价值的药理学性质。人类作为药物，已被证明具有有趣的镇静活动。

14. 发明授权

US5010077A .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders 失效
标题翻译：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.

15. 发明授权

US4645773A .beta.-carboline-3-oxadiazolyl derivatives, and their use as psychotropic agents 失效
标题翻译： β-咔啉-3-恶二唑基衍生物及其作为精神药物的用途
公开(公告)号：US4645773A
公开(公告)日：1987-02-24
申请号：US734219
申请日：1985-05-15
申请人： Mogens Engelstoft , Tage Honore , Frank Watjen , Erling N. Petersen , Andreas Huth
发明人： Mogens Engelstoft , Tage Honore , Frank Watjen , Erling N. Petersen , Andreas Huth
IPC分类号： A61K31/435 , A61P25/00 , A61P25/20 , A61P39/02 , C07D471/04 , A61K31/395
CPC分类号： C07D471/04
摘要： New .beta.-carboline-3-oxadiazolyl derivatives have the general formula I: ##STR1## wherein X is ##STR2## and wherein R.sup.4, R.sup.A and R have specified meanings. These new compounds exhibit surprising psychotropic properties.
摘要翻译：新的β-咔啉-3-恶二唑基衍生物具有通式I：其中X是<和>，其中R4，RA和R具有特定含义。这些新化合物表现出惊人的精神药性。

16. 发明授权

US4670433A Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith 失效
标题翻译：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。

17. 发明授权

US4772696A Oxadiazolyl imidazobenzodiazepine process 失效
标题翻译：恶二唑咪唑并二氮杂法
公开(公告)号：US4772696A
公开(公告)日：1988-09-20
申请号：US942162
申请日：1986-12-16
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 , C07D521/00
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.

18. 发明授权

US4745112A Oxadiazolylimidazobenzodiazepine, compositions, and method III 失效
标题翻译：恶二唑并咪唑并苯并二氮杂，组合物和方法III
公开(公告)号：US4745112A
公开(公告)日：1988-05-17
申请号：US856945
申请日：1986-04-28
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： C07D271/06 , C07D487/04 , C07D487/14 , A61K31/55
CPC分类号： C07D271/06 , C07D487/04 , C07D487/14
摘要： The application discloses novel benzodiazepine agonist compounds, namely, compounds having the formula ##STR1## wherein X is F, CF.sub.3, CH.sub.3, or CN, pharmaceutical compositions thereof, and a method of ameliorating central nervous system ailments therewith, especially convulsions and anxiolytic states. A novel intermediate and process for their production are also disclosed.
摘要翻译：该申请公开了新的苯并二氮激动剂化合物，即具有式“IMAGE”的化合物，其中X为F，CF 3，CH 3或CN，其药物组合物，以及改善其中枢神经系统疾病，特别是惊厥和抗焦虑状态的方法。还公开了一种用于其生产的新型中间体和方法。

19. 发明授权

US4622321A Oxadiazolylimidazobenzodiazepine, compositions, and method 失效
标题翻译：恶二唑并咪唑并二氮杂，组合物和方法
公开(公告)号：US4622321A
公开(公告)日：1986-11-11
申请号：US816731
申请日：1986-01-06
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： A61K31/55 , C07D20060101 , C07D271/06 , C07D487/04 , C07D487/14
CPC分类号： C07D271/06 , C07D487/04 , C07D487/14
摘要： The application discloses a novel benzodiazepine agonist compound, namely, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5,6-dihydro-5-methyl-6-oxo-4H-imidazo [1,5-a][1,4]benzodiazepine, pharmaceutical compositions thereof, and a method of ameliorating central nervous system ailments therewith, especially convulsions and anxiolytic states. A novel intermediate and process for its production are also disclosed.

20. 发明授权

US4622320A Oxadiazolylimidazobenzodiazepine, compositions, and method 失效
标题翻译：恶二唑并咪唑并二氮杂，组合物和方法
公开(公告)号：US4622320A
公开(公告)日：1986-11-11
申请号：US816732
申请日：1986-01-06
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： A61K31/55 , C07D20060101 , C07D271/06 , C07D487/04 , C07D487/14
CPC分类号： C07D271/06 , C07D487/04 , C07D487/14
摘要： The application discloses novel benzodiazepine agonist compounds, namely, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5,6-dihydro-5-methyl-6-oxo-7-halo-4H-imidazo [1,5-a][1,4]benzodiazepines, pharmaceutical compositions thereof, and a method of ameliorating central nervous system ailments therewith, especially convulsions and anxiolytic states. A novel intermediate and process for their production are also disclosed.
摘要翻译：本申请公开了新的苯并二氮类激动剂化合物，即3-（5-环丙基-1,2,4-恶二唑-3-基）-5,6-二氢-5-甲基-6-氧代-7H-4H-4H 咪唑并[1,5-a] [1,4]苯并二氮杂及其药物组合物，以及改善中枢神经系统疾病的方法，特别是惊厥和抗焦虑状态。还公开了一种用于其生产的新型中间体和方法。

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