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31. 发明授权

US5091427A Piperazinediones having a psychotropic action 失效
标题翻译：具有心理行为的管理员
公开(公告)号：US5091427A
公开(公告)日：1992-02-25
申请号：US401842
申请日：1989-09-01
申请人： Wolf-Ulrich Nickel , Rainer Henning , Wolfgang Ruger , Ulrich Lerch , Hansjorg Urbach , Franz Hock , Gabriele Wiemer
发明人： Wolf-Ulrich Nickel , Rainer Henning , Wolfgang Ruger , Ulrich Lerch , Hansjorg Urbach , Franz Hock , Gabriele Wiemer
IPC分类号： A61K31/495 , A61P25/00 , A61P25/28 , C07D241/08 , C07D403/04 , C07D405/04 , C07D455/04 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D513/04 , C07K1/113 , C07K5/06
CPC分类号： C07D487/04 , C07D241/08
摘要： The invention relates to compounds of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.4 represent optionally substituted aliphatic, alicyclic, alicyclic-aliphatic, aromatic, araliphatic, heteroaromatic or heteroaromatic-aliphatic radicals, with R.sup.2, if not already covered by the above-mentioned definitions, denoting the side-chain, which is protected if necessary, of a naturally occurring .alpha.-amino acid, R.sup.4 can additionally represent ##STR2## R.sup.3 denotes an optionally substituted aliphatic, alicyclic, aromatic or araliphatic radical, or R.sup.3 and R.sup.4 form, together with the atoms carrying them, a mono-, bi- or tricyclic heterocyclic ring system,agents containing these, and the use thereof as pharmaceuticals having a psychotropic action for the prophylaxis of disorders of the central nervous system, especially having a nootropic action for the treatment of cognitive dysfunctions.
摘要翻译：本发明涉及式I（I）的化合物，其中R 1，R 2和R 4表示任选取代的脂族，脂环族，脂环族 - 脂族，芳族，芳脂族，杂芳族或杂芳族 - 脂族基团，其中R2，如果不是由上述定义所涵盖，表示如果必要的话保护的侧链，天然存在的α-氨基酸，R4可以另外表示任选取代的脂族，脂环族，芳族或芳脂族基团，或R3和R4与携带它们的原子一起形成单环，双环或三环杂环体系，含有它们的试剂，以及作为具有用于预防中枢神经系统疾病的精神作用的药物的用途，特别是具有用于治疗认知功能障碍的向推动作用。

32. 发明授权

US5043346A Amino acid esters, pharmaceuticals containing them, and the use thereof in learning disorders 失效
标题翻译：氨基酸酯，含有它们的药物及其在学习障碍中的用途
公开(公告)号：US5043346A
公开(公告)日：1991-08-27
申请号：US340656
申请日：1989-04-20
申请人： Franz Hock , Josef Scholtholt , Hansjorg Urbach , Rainer Henning , Ulrich Lerch , Wolf-Ulrich Nickel , Wolfgang Ruger
发明人： Franz Hock , Josef Scholtholt , Hansjorg Urbach , Rainer Henning , Ulrich Lerch , Wolf-Ulrich Nickel , Wolfgang Ruger
IPC分类号： C07C219/02 , A61K38/00 , A61P25/28 , C07K1/02 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , A61K38/005
摘要： The invention relates to amino acid esters of the formula I ##STR1## in which n is 2 and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning indicated in the description, to a process and intermediates for the preparation thereof, to agents containing them, and the use thereof.
摘要翻译：本发明涉及式I（I）的氨基酸酯，其中n为2，R 1，R 2，R 3，R 4和R 5具有说明书所示的含义，涉及制备方法和中间体含有它们的试剂及其用途。

33. 发明授权

US5114962A New amino acid esters, a process for their preparation, medicaments containing them, and the use thereof 失效
标题翻译：新的氨基酸酯，其制备方法，含有它们的药物及其用途
公开(公告)号：US5114962A
公开(公告)日：1992-05-19
申请号：US540634
申请日：1990-06-19
申请人： Wolfgang Ruger , Hansjorg Urbach , Reinhard Becker , Franz Hock
发明人： Wolfgang Ruger , Hansjorg Urbach , Reinhard Becker , Franz Hock
IPC分类号： C07D317/34 , A61K38/00 , A61K38/55 , A61P25/28 , A61P29/00 , C07D317/36 , C07D317/40 , C07D405/12 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0222 , A61K38/00
摘要： New amino acid esters, a process for their preparation, medicaments containing them, and the use thereof The invention relates to amino acid esters of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 denote hydrogen or a defined radical, R.sup.4 together with R.sup.5 and the atoms carrying them form a heterocyclic ring system, to a process for their preparation, to agents containing them, and to the use thereof.
摘要翻译：新氨基酸酯，其制备方法，含有它们的药物及其用途本发明涉及式I（I）的氨基酸酯，其中n为1或2，R 1，R 2，R 2和 R3表示氢或定义的基团，R4与R5一起，携带它们的原子形成杂环体系，其制备方法，含有它们的试剂及其用途。

34. 发明授权

US5231084A Compounds having a cognition adjuvant action, agents containing them, and the use thereof for the treatment and prophylaxis of cognitive dysfuncitons 失效
标题翻译：具有认知辅助作用的化合物，含有它们的药剂及其用于治疗和预防认知功能障碍的用途
公开(公告)号：US5231084A
公开(公告)日：1993-07-27
申请号：US711719
申请日：1991-06-07
申请人： Franz Hock , Josef Scholtholt , Hansjorg Urbach , Rainer Henning , Ulrich Lerch , Wolf-Ulrich Nickel , Wolfgang Ruger
发明人： Franz Hock , Josef Scholtholt , Hansjorg Urbach , Rainer Henning , Ulrich Lerch , Wolf-Ulrich Nickel , Wolfgang Ruger
IPC分类号： A61K38/00 , C07K5/02
CPC分类号： C07K5/0222 , A61K38/00
摘要： The invention relates to new comoounds having a cognition adjuvant action, to the use of ACE inhibitors as medicaments having a cognition adjuvant action, to agents containing them, and to the use thereof for the treatment and prophylaxis of cognitive dysfunctions.
摘要翻译：本发明涉及具有认知辅助作用的新物质，ACE抑制剂用作具有认知辅助作用的药物，含有它们的药剂，以及其用于治疗和预防认知功能障碍的用途。

35. 发明授权

US5055483A Novel amino acid glycerides, learning medicaments containing them and their use 失效
标题翻译：新型氨基酸果糖，含有他们及其使用的学习药物
公开(公告)号：US5055483A
公开(公告)日：1991-10-08
申请号：US299186
申请日：1989-01-19
申请人： Wolfgang Ruger , Hansjorg Urbach , Reinhard Becker , Franz Hock
发明人： Wolfgang Ruger , Hansjorg Urbach , Reinhard Becker , Franz Hock
IPC分类号： A61K38/55 , A61K38/00 , A61P9/12 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0222 , A61K38/00
摘要： The invention relates to amino acid esters of the formula ##STR1## in which n=1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 denote hydrogen or a defined radical, R.sup.4 together with R.sup.5 and the atoms carrying them form a heterocyclic ring system, processes for their preparation, agents containing them and their use.
摘要翻译：本发明涉及式（I）的氨基酸酯，其中n = 1或2，R 1，R 2，R 2和R 3表示氢或定义的基团，R 4与R 5一起并且携带它们的原子形成杂环环系统，其制备过程，含有它们的试剂及其用途。

36. 发明授权

US4558065A Derivatives of tricyclic aminoacids, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation 失效
标题翻译：三环氨基酸的衍生物，其制备方法，含有这些化合物的药剂及其用途，以及新的双环氨基酸作为其中间体及其制备方法
公开(公告)号：US4558065A
公开(公告)日：1985-12-10
申请号：US550531
申请日：1983-11-10
申请人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
发明人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
IPC分类号： C07D209/70 , A61K31/40 , A61K31/403 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D209/58 , C07D221/22 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , A61K37/00
CPC分类号： C07D209/58 , C07D221/22 , C07K5/0222 , A61K38/00
摘要： The invention relates to new derivatives of tricyclic aminoacids, of the formula I ##STR1## in which n denotes 0 or 1, A denotes --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen, or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, or alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, or aralkyl or aroylalkyl, both of which can be substituted as defined above, or a monocyclic or bicyclic S-, O- and/or N-heterocyclene radical, or a side chain of a naturally occurring aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and physiologically acceptable salts thereof, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation.
摘要翻译：本发明涉及式I（I）的三环氨基酸的新衍生物，其中n表示0或1，A表示-CH = CH-或-CH 2 -CH 2 - ，R表示氢，烷基或芳烷基， R 1表示氢或烷基，其可任选被氨基，酰氨基或苯甲酰基氨基取代，或链烯基，环烷基，环烯基，环烷基烷基，芳基或部分氢化的芳基，其各自可被烷基，烷氧基或卤素取代，或芳烷基或芳基烷基，二者可以如上所定义，或可被保护的单环或双环S-，O-和/或N-杂环烯基或天然存在的氨基酸的侧链，R 2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z表示氧，X表示烷基，烯基，环烷基，芳基，可以被烷基，烷氧基单，二或三取代，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基和/或亚甲二氧基，或 3-吲哚基及其生理学上可接受的盐，其制备方法，含有这些化合物的试剂及其用途，以及新的双环氨基酸作为其中间体及其制备方法。

37. 发明授权

US4591598A Derivatives of 2-azabicyclo[3.1.0]hexane-3-carboxylic acid, and hypotensive use thereof 失效
标题翻译： 2-氮杂双环[3.1.0]己烷-3-羧酸的衍生物及其降血压用途
公开(公告)号：US4591598A
公开(公告)日：1986-05-27
申请号：US627639
申请日：1984-07-03
申请人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
发明人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
IPC分类号： A61K31/40 , A61K31/403 , A61K31/405 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D209/52 , C07D221/04 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K14/81 , C07D209/02
CPC分类号： C07D221/04 , C07D209/52 , C07K5/0222 , A61K38/00
摘要： The invention relates to compounds of the formula I ##STR1## in which n denotes 0 or 1, R denotes hydrogen, alkyl, alkenyl or aralkyl, R.sup.1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, aralkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined previously, a monocyclic or bicyclic S- or O- and/or N-heterocyclic radical or a side chain of an aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen, X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, acylamino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and to a process for their preparation, agents containing them and and their use, and to 2-azabicyclo[3.1.0]hexane derivatives as intermediates, and a process for their preparation.
摘要翻译：本发明涉及式I的化合物，其中n表示0或1，R表示氢，烷基，链烯基或芳烷基，R1表示氢或烷基，其可任选被氨基，酰氨基或苯甲酰氨基，烯基，环烷基，环烯基，环烷基烷基，芳基或部分氢化的芳基，其各自可以被烷基，烷氧基或卤素取代，芳烷基或芳酰基烷基，它们都可以在如前定义的芳基中被取代，单环或双环 S-或O-和/或N-杂环基或氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z一起表示氧，X表示烷基，烯基，环烷基，芳基，其可以被烷基，烷氧基，羟基，卤素，硝基，氨基，酰氨基，烷基氨基，二烷基氨基和/或亚甲二氧基或3-吲哚基单取代或三取代，准备，代理含有它们及其用途，以及作为中间体的2-氮杂双环[3.1.0]己烷衍生物及其制备方法。

38. 发明授权

US4920144A Derivatives of bicyclic amino acids, agents containing them and their use as hypotensives 失效
标题翻译：双环氨基酸的衍生物，含有它们的药剂及其作为假药的用途
公开(公告)号：US4920144A
公开(公告)日：1990-04-24
申请号：US332338
申请日：1989-04-03
申请人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
发明人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
IPC分类号： C07D521/00 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D209/52 , C07K1/02 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/068 , C07K14/81
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： The invention relates to new derivatives of the bicyclic amino acids of the formula I ##STR1## in which n denotes 0, 1 or 2, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, optionally substituted aryl or partially hydrogenated aryl, aryl-(C.sub.1 to C.sub.4)-alkyl or aroyl-C.sub.1 -alkyl, both of which can be substituted, a monocyclic or bicyclic heterocyclic radical or a side chain of a naturally occurring amino acid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, X denotes alkyl, alkenyl, cycloalkyl or aryl which can be substituted, or 3-indolyl, and to their salts, to a process for their preparation, to agents containing them, and to their use.
摘要翻译：本发明涉及式I（I）的双环氨基酸的新衍生物，其中n表示0,1或2，R表示氢，烷基或芳烷基，R 1表示氢或烷基，烯基，环烷基，环烯基，环烷基烷基，任选取代的芳基或部分氢化的芳基，芳基 - （C 1 -C 4） - 烷基或芳酰基-C 1 - 烷基，它们都可被取代，单环或双环杂环基或天然存在的氨基酸的侧链，R 2表示氢，烷基，链烯基或芳烷基，X表示可被取代的烷基，链烯基，环烷基或可被取代的芳基，及其盐，其制备方法，含有它们的试剂，以及它们使用。

39. 发明授权

US4614805A Bicyclic amino acids as intermediates in the preparation of tricyclic amino acids and processes for their preparation 失效
标题翻译：双环氨基酸作为制备三环氨基酸的中间体及其制备方法
公开(公告)号：US4614805A
公开(公告)日：1986-09-30
申请号：US773077
申请日：1985-09-06
申请人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
发明人： Hansjorg Urbach , Rainer Henning , Reinhard Becker
IPC分类号： C07D209/70 , A61K31/40 , A61K31/403 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D209/58 , C07D221/22 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C07D209/56
CPC分类号： C07D209/58 , C07D221/22 , C07K5/0222 , A61K38/00
摘要： The invention relates to new derivatives of tricyclic aminoacids, of the formula I ##STR1## in which n denotes 0 or 1, A denotes --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen, or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, or alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, or aralkyl or aroylalkyl, both of which can be substituted as defined above, or a monocyclic or bicyclic S--, O-- and/or N-heterocyclene radical, or a side chain of a naturally occurring aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and physiologically acceptable salts thereof, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation.
摘要翻译：本发明涉及式I（I）的三环氨基酸的新衍生物，其中n表示0或1，A表示-CH = CH-或-CH 2 -CH 2 - ，R表示氢，烷基或芳烷基， R 1表示氢或烷基，其可任选被氨基，酰氨基或苯甲酰基氨基取代，或链烯基，环烷基，环烯基，环烷基烷基，芳基或部分氢化的芳基，其各自可被烷基，烷氧基或卤素取代，或芳烷基或芳基烷基，二者可以如上所定义，或单环或双环的S-，O-和/或N-杂环基，或可被保护的天然存在的氨基酸的侧链，R 2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z表示氧，X表示烷基，烯基，环烷基，芳基，可以被烷基，烷氧基单，二或三取代，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基和/或亚甲二氧基，或 3-吲哚基及其生理学上可接受的盐，其制备方法，含有这些化合物的试剂及其用途，以及新的双环氨基酸作为其中间体及其制备方法。

40. 发明授权

US4857520A Fused azepinone and azocinone derivatives, processes for their preparation, agents containing them and their use, and intermediates in their preparation 失效
标题翻译：稠合氮杂酮和azocinone衍生物，其制备方法，含有它们的试剂及其用途及其制备中间体
公开(公告)号：US4857520A
公开(公告)日：1989-08-15
申请号：US155595
申请日：1988-02-12
申请人： Hansjorg Urbach , Rainer Henning , Bernward Scholkens , Reinhard Becker
发明人： Hansjorg Urbach , Rainer Henning , Bernward Scholkens , Reinhard Becker
IPC分类号： C07D223/32 , A61K31/395 , A61K31/445 , A61K31/55 , A61K38/00 , A61P9/00 , A61P9/12 , A61P27/02 , A61P27/06 , A61P43/00 , C07D225/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07K5/02
CPC分类号： C07K5/0222 , A61K38/00
摘要： The invention relates to compounds of the formula I ##STR1## in which m denotes 1 or 2 and n denotes, 0, 1 or 2; R.sup.1 and R.sup.2 denote identical or different radicals from the series comprising hydrogen, optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, partly hydrogenated aryl and optionally substituted aralkyl; R.sup.3 and R.sup.4 denote identical or different radicals from the series comprising hydrogen, alkyl, alkenyl and optionally substituted aralkyl; Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxo, and X denotes optionally substituted alkyl, alkenyl, cycloalkyl, optionally substituted 4-piperidinyl, optionally substituted aryl or indolyl, processes for their preparation, medicaments containing these compounds and their use, and to intermediates in their preparation.
摘要翻译：本发明涉及式I（I）的化合物，其中m表示1或2，n表示0,1或2; R 1和R 2表示与包含氢，任选取代的烷基，烯基，环烷基，环烯基，环烷基烷基，部分氢化的芳基和任选取代的芳烷基的系列相同或不同的基团; R3和R4表示与包含氢，烷基，烯基和任选取代的芳烷基的系列相同或不同的基团; Y表示氢或羟基，Z表示氢，或Y和Z一起表示氧代，X表示任选取代的烷基，烯基，环烷基，任选取代的4-哌啶基，任选取代的芳基或吲哚基，其制备方法，含有这些化合物的药物和他们的使用，以及中间人的准备。

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