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1. 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。

2. 发明授权

US4623649A Substituted .beta.-carbolines, and use thereof as medicinal agents 失效
标题翻译：取代的β-咔啉，并将其用作药物
公开(公告)号：US4623649A
公开(公告)日：1986-11-18
申请号：US654594
申请日：1984-09-26
申请人： Andreas Huth , Ralph Schmiechen , Dieter Rahtz , Dieter Seidelmann , Claus T. Braestrup
发明人： Andreas Huth , Ralph Schmiechen , Dieter Rahtz , Dieter Seidelmann , Claus T. Braestrup
IPC分类号： A61K31/435 , A61P25/00 , C07D471/04 , A61K31/33
CPC分类号： C07D471/04
摘要： Novel substituted .beta.-carboline derivatives of Formula I ##STR1## wherein R.sup.3 is an oxadiazolyl residue of the formula ##STR2## wherein R.sup.5 stands for lower alkyl of up to 3 carbon atoms or an ester ##STR3## with R.sup.6 being hydrogen or lower alkyl of up to 3 carbon atoms, R.sup.4 is hydrogen, lower alkyl of up to 3 carbon atoms, or CH.sub.2 OR.sup.9 wherein R.sup.9 is lower alkyl of up to 3 carbon atoms,R.sup.A is phenyl or a hydrocarbon residue containing 2-10 carbon atoms which can be cyclic or acyclic, saturated or unsaturated, branched or unbranched, and which can optionally be substituted by oxo, formyl OH, O-alkyl of up to 3 carbon atoms or phenyl, and wherein, in a cyclic hydrocarbon residue, a CH.sub.2 -group can be replaced by oxygen,exhibit an effect on the central nervous system and thus are suitable as psychopharmaceuticals.
摘要翻译：式I的新型取代的β-咔啉衍生物其中R 3是下式的恶二唑基残基，其中R 5表示至多3个碳原子的低级烷基，或者R 6表示氢或最多3个碳原子的低级烷基，R4是氢，至多3个碳原子的低级烷基或CH2OR9，其中R9是至多3个碳原子的低级烷基，RA是苯基或含2-10个碳原子的烃基，可以是环状或非环状，饱和或不饱和的，支链或非支链的，并且其可任选被氧代，甲酰基OH，至多3个碳原子的O-烷基或苯基取代，并且其中在环状烃残基中，组可以被氧代替，对中枢神经系统有影响，因此适合作为心理药物。

3. 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。

4. 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.

5. 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.

6. 发明授权

US4564610A Substituted 5H-pyrimido[5,4-b]indoles 失效
标题翻译：取代的5H-嘧啶并[5,4-b]吲哚
公开(公告)号：US4564610A
公开(公告)日：1986-01-14
申请号：US562248
申请日：1983-12-16
申请人： Dieter Rahtz , Andreas Huth , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert H. Schneider , Claus T. Braestrup
发明人： Dieter Rahtz , Andreas Huth , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert H. Schneider , Claus T. Braestrup
IPC分类号： A61K31/505 , A61P25/00 , C07D209/42 , C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07D209/42 , C07F9/6561
摘要： Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.2 wherein R is C.sub.1-5 -alkyl, exhibit strong affinity for binding to benzodiazepine receptors.The novel compounds are suitable for use in psychopharmaceutical preparations.
摘要翻译：取代的式I的5H-嘧啶并[5,4-b]吲哚其中R 2是卤素; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; C 1-5 - 烷基，环烷基，芳烷基或芳基; ORI，nn为0,1或2，或其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基的SO nRI; 其中RII和RIII是氢，C1-5-烷基，C3-5-烯基，环烷基，芳烷基，芳基，或具有连接的N-原子的5-或6-元杂环; RA为氢; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; 卤素，硝基，ORI，nn为0,1或2的SO nRI，其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基; 其中RII和RIII是氢，C1-5烷基，环烷基，C3-5-烯基，芳烷基，芳基，或具有连接的N-原子的5或6元杂环; 或其中R为C 1-5 - 烷基的PO（OR）2表现出对苯并二氮杂受体结合的强亲合力。新型化合物适用于精神药物制剂。

7. 发明授权

US4731358A .beta.-carbolines and their use as tranquilizers 失效
标题翻译： β-咔啉及其作为镇定剂的用途
公开(公告)号：US4731358A
公开(公告)日：1988-03-15
申请号：US902855
申请日：1986-09-02
申请人： Andreas Huth , Dieter Rahtz , Dieter Seidelmann , Helmut Schmiechen , Helmut Biere , Claus T. Braestrup
发明人： Andreas Huth , Dieter Rahtz , Dieter Seidelmann , Helmut Schmiechen , Helmut Biere , Claus T. Braestrup
IPC分类号： A61K31/435 , A61P25/00 , A61P25/20 , C07D209/10 , C07D209/14 , C07D209/16 , C07D471/04 , C07F9/40 , C07F9/6561 , A61K31/395 , C07F9/32
CPC分类号： C07D471/04 , C07D209/10 , C07D209/14 , C07D209/16 , C07F9/4015 , C07F9/6561
摘要： New substituted .beta.-carbolines of formula I ##STR1## wherein R.sup.3 is hydrogen or a non-carboxyl based substituent, and R.sup.4-9 have various meanings,are valuable pharmaceutical products with long lasting action on the central nervous system.
摘要翻译：其中R3是氢或非羧基取代基，R4-9具有各种含义的式Ⅰ的新取代的β-咔啉是对中枢神经系统持久作用的有价值的药物产品。

8. 发明授权

US4757070A 3-oxadiazolyl-5-aminoalkyl-beta-carboline derivatives compositions and use 失效
标题翻译： 3-恶二唑基-5-氨基烷基-β-咔啉衍生物组合物和用途
公开(公告)号：US4757070A
公开(公告)日：1988-07-12
申请号：US130049
申请日：1987-12-08
申请人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , David N. Stephens
发明人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , David N. Stephens
IPC分类号： A61K31/435 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of formula I ##STR1## wherein n is 0 or 1,R.sup.1 is hydrogen or lower alkyl,R.sup.2 and R.sup.3 each independently is hydrogen, optionally substituted lower alkyl, acyl or aryl, or together with the nitrogen atom form a 5-6-member heterocycle,R.sup.4 is hydrogen, lower alkyl or lower alkoxyalkyl andX is COOR.sup.6, CO--NR.sup.7 R.sup.8, or an oxadiazolyl radical of the formula ##STR2## wherein R.sup.5 is H, lower alkyl or cycloalkyl,R.sup.6 is H or lower alkyl,R.sup.7 and R.sup.8 each independently is hydrogen, optionally substituted lower alkyl, acyl or aryl, orR.sup.7 and R.sup.8 together with the nitrogen atom can form a 5-6-member heterocycle,are valuable drugs, e.g., have psychotropic activity.
摘要翻译：式I的化合物其中n为0或1，R 1为氢或低级烷基，R 2和R 3各自独立地为氢，任选取代的低级烷基，酰基或芳基，或与氮原子一起形成5-6元芳基， R 4是氢，低级烷基或低级烷氧基烷基，X是COOR 6，CO-NR 7 R 8或下式的恶二唑基，其中R 5是H，低级烷基或环烷基，R 6是H或低级烷基，R 7和 R8各自独立地是氢，任选取代的低级烷基，酰基或芳基，或者R 7和R 8与氮原子一起可以形成5-6元杂环，是有价值的药物，例如具有精神活性。

9. 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.

10. 发明授权

US06288065B1 Quinoxaline-carboxylic acid derivatives 失效
标题翻译：喹喔啉羧酸衍生物
公开(公告)号：US06288065B1
公开(公告)日：2001-09-11
申请号：US09102649
申请日：1998-06-23
申请人： Andreas Huth , Ralph Schmiechen , Ilse Beetz , Ingrid Schumann , Lechoslaw Turski , Peter Andreas Loschmann , David Norman Stephens , Dieter Seidelmann , Martin Kruger , Dieter Rahtz , Peter Holscher
发明人： Andreas Huth , Ralph Schmiechen , Ilse Beetz , Ingrid Schumann , Lechoslaw Turski , Peter Andreas Loschmann , David Norman Stephens , Dieter Seidelmann , Martin Kruger , Dieter Rahtz , Peter Holscher
IPC分类号： C07D24144
CPC分类号： C07D241/44 , C07F9/650994
摘要： The disclosure relates to quinoxaline derivates of Formula I wherein R1, R4, R5, R6, R7 and R8 are defined in the disclosure, as well as their production and use in medicinal agents.
摘要翻译：本公开涉及式I的喹喔啉衍生物，其中R1，R4，R5，R6，R7和R8在本公开内容中定义，以及它们在药物中的生产和用途。

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