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1. 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。

2. 发明授权

US5414002A 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：US5414002A
公开(公告)日：1995-05-09
申请号：US416629
申请日：1989-10-03
申请人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert H. Schneider , Mogens Engelstoft , Bondo J. Hansen , Frank Waetjen , Tage Honore
发明人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert H. Schneider , Mogens Engelstoft , Bondo J. Hansen , Frank Waetjen , Tage Honore
IPC分类号： C07D487/04 , A61K31/435 , A61K31/437 , A61P25/18 , C07D471/04
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, andR.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R1是氢，次氮基，卤素，低级烷基或低级烷氧基，R3是支链C 3-6烷基，其任选地被卤素或任选被甲基取代的C 3-6环烷基是有价值的药物。

3. 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。

4. 发明授权

US4960777A Heteroaryloxy-.beta.-carboline derivatives, their preparation and their use as medicinal agents 失效
标题翻译：异丙酰氧基-β-咔啉衍生物，其制备及其作为药剂的用途
公开(公告)号：US4960777A
公开(公告)日：1990-10-02
申请号：US409899
申请日：1989-09-20
申请人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , David Stephens , Mogens Engelstoft , John B. Hansen
发明人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , David Stephens , Mogens Engelstoft , John B. Hansen
IPC分类号： A61K31/435 , A61K31/495 , A61K31/505 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04
摘要： Heteroaryloxy-.beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is an optionally substituted heteroaryl residue,R.sup.2 is hydrogen, lower alkyl or lower alkoxyalkyl,X is a COOR.sup.3 -group wherein R.sup.3 means H or lower alkyl, or represents a CONR.sup.4 R.sup.5 -group wherein R.sup.4 and R.sup.5 mean respectively hydrogen or lower alkyl, R.sup.4 and R.sup.5 being capable of forming, together with the nitrogen atom, a 5- to 6-membered heterocycle, or means an oxadiazolyl residue of the formula ##STR2## wherein R.sup.6 means hydrogen, lower alkyl or cycloalkyl, are valuable pharmaceuticals.

5. 发明授权

US4600715A Benzodiazepine antagonistic .beta.-carboline derivatives and compositions thereof 失效
标题翻译：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。

6. 发明授权

US4894377A .beta.-carbolines and their use as medicinal agents 失效
标题翻译： 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。

7. 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.

8. 发明授权

US4596808A Pharmacologically active 3-substituted beta-carbolines useful as tranquilizers 失效
标题翻译：药理活性的3-取代的β-咔啉可用作镇定剂
公开(公告)号：US4596808A
公开(公告)日：1986-06-24
申请号：US556869
申请日：1983-12-01
申请人： Claus T. Braestrup , Jogen A. Christensen , Mogens Engelstoft , Guenter 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 , Guenter 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.A is H, F, Cl, Br, I, NO.sub.2, CN, CH.sub.3, CF.sub.3, SCH.sub.3, NR.sup.16 R.sup.17 or NHCOR.sup.16,wherein R.sup.16 and R.sup.17 are the same or different and each is hydrogen or alkyl, alkenyl or alkynyl each of up to 6 C-atoms, aralkyl or cycloalkyl each of up to 10 C-atoms,or wherein R.sup.16 and R.sup.17 together form a saturated or unsaturated 3-7 membered heterocyclic ring;said compounds possess valuable psychotropic properties which make them useful for example as tranquilizers.

9. 发明授权

US4435403A 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.

10. 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。

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