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1. 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。

2. 发明授权

US4879403A Process for the preparation of cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids 失效
标题翻译：顺式，内-2-氮杂双环[3.3.0] - 辛烷-3-羧酸的制备方法
公开(公告)号：US4879403A
公开(公告)日：1989-11-07
申请号：US267753
申请日：1988-11-02
申请人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
发明人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-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 or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译：其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或可以被保护的天然存在的α-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表示氧，X表示烷基，烯基或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法，含有这些化合物的药剂及其用途。

3. 发明授权

US5061722A Cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids, a process for their preparation, agents containing these compounds and their use 失效
标题翻译：（3.3.0）-OCTANE-3-羧酸，其制备方法，包含这些化合物的试剂及其用途
公开(公告)号：US5061722A
公开(公告)日：1991-10-29
申请号：US296513
申请日：1989-01-12
申请人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
发明人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and 2 denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译：其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或可以被保护的天然存在的α-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表示氧，X表示烷基，烯基或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法，含有这些化合物的药剂及其用途。

4. 发明授权

US4727160A Method for making 2-azabicyclo-[3.3.0]-octane-3-carboxylic acids 失效
标题翻译：制备2-氮杂双环[3.3.0] - 辛烷-3-羧酸的方法
公开(公告)号：US4727160A
公开(公告)日：1988-02-23
申请号：US658902
申请日：1984-10-09
申请人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
发明人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-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 or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译：其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或可以被保护的天然存在的α-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表示氧，X表示烷基，烯基或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法，含有这些化合物的药剂及其用途。

5. 发明授权

US5053519A Cis, endo-2-azabicyclo-[3.3.0]-octane-5-carboxylic acids 失效
标题翻译： CIS，ENDO-2-AZABICYCLO-（3.3.0）-OCTANE-5-CARBOXYLIC ACIDS
公开(公告)号：US5053519A
公开(公告)日：1991-10-01
申请号：US318519
申请日：1989-02-28
申请人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
发明人： Volker Teetz , Rolf Geiger , Hansjorg Urbach , Reinhard Becker , Bernward Scholkens
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-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 or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译：其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或可以被保护的天然存在的α-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表示氧，X表示烷基，烯基或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法，含有这些化合物的药剂及其用途。

6. 发明授权

US4562202A N-Acyl hexahydroindole-2-carboxylic acids and anti-hypertensive use thereof 失效
标题翻译： N-酰基六氢吲哚-2-羧酸及其抗高血压用途
公开(公告)号：US4562202A
公开(公告)日：1985-12-31
申请号：US477333
申请日：1983-03-21
申请人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Hans Wissmann , Reinhard Becker
发明人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Hans Wissmann , Reinhard Becker
IPC分类号： A61K31/403 , A61K31/404 , A61K31/405 , A61K38/00 , A61K38/55 , A61P9/12 , C07D209/42 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , A61K31/40
CPC分类号： C07K5/0222 , C07D209/42 , 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 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, which each can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined in the aforegoing, a monocyclic or bicyclic sulfur or oxygen and/or nitrogen heterocyclic radical, or a side chain of a naturally occurring aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or arylalkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which is monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy or 3-indolyl,and their physiologically acceptable salts, processes for their preparation, agents containing these and their use as medicaments and also bicyclic amino acids as their intermediates and processes 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，酰氨基或苯甲酰基氨基取代，，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，芳基烷基或芳酰基烷基取代，二者可以在如上所定义的芳基中被取代，单环或双环硫或氧和/或氮杂环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，Z一起表示氧，X表示烷基，烯基，环烷基，芳基，其被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基或3-吲哚基单取代或三取代，及其生理学表盐，其制备方法，含有这些物质的药剂及其作为药物的用途以及双环氨基酸作为其中间体及其制备方法。

7. 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。

8. 发明授权

US5366994A Use of a combination of angiotensin-converting enzyme inhibitor and calcium antagonist for the treatment of proteinuria 失效
标题翻译：使用血管紧张素转换酶抑制剂和钙拮抗剂的组合来治疗蛋白尿
公开(公告)号：US5366994A
公开(公告)日：1994-11-22
申请号：US057516
申请日：1993-05-06
申请人： Reinhard Becker , Rainer Henning , Volker Teetz , Hansjorg Urbach
发明人： Reinhard Becker , Rainer Henning , Volker Teetz , Hansjorg Urbach
IPC分类号： A61K38/55 , A61K31/275 , A61K31/277 , A61K31/40 , A61K31/401 , A61K31/41 , A61K31/425 , A61K31/455 , A61K31/47 , A61K31/55 , A61K45/06 , A61P3/00 , A61P3/14 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00
CPC分类号： A61K38/556
摘要： A combination of angiotensin-converting enzyme inhibitors and calcium antagonists for the treatment of proteinuria is disclosed. The invention relates to the prevention and therapy of proteinuria by administration of a combination of ACE inhibitor and calcium antagonist.
摘要翻译：公开了用于治疗蛋白尿的血管紧张素转换酶抑制剂和钙拮抗剂的组合。本发明涉及通过施用ACE抑制剂和钙拮抗剂的组合来预防和治疗蛋白尿。

9. 发明授权

US4975453A Combination of angiotensin converting enzyme inhibitors with potassium channel modulators and use thereof in pharmaceuticals 失效
标题翻译：血管紧张素转换酶抑制剂与钾通道调节剂的组合及其在药物中的应用
公开(公告)号：US4975453A
公开(公告)日：1990-12-04
申请号：US357822
申请日：1989-05-26
申请人： Reinhard Becker , Rainer Henning , Hansjorg Urbach , Volker Teetz , Heinrich C. Englert , Dieter Mania
发明人： Reinhard Becker , Rainer Henning , Hansjorg Urbach , Volker Teetz , Heinrich C. Englert , Dieter Mania
IPC分类号： A61K31/40 , A61K38/55 , A61K45/06 , A61P25/02
CPC分类号： A61K38/556
摘要： Combination of angiotensin converting enzyme inhibitors with potassium channel modulators and use thereof in pharmaceuticals.The invention relates to combinations of angiotensin converting enzyme inhibitors with potassium channel modulators, processes for their preparation and use thereof as medicaments.
摘要翻译：血管紧张素转换酶抑制剂与钾通道调节剂的组合及其在药物中的应用。本发明涉及血管紧张素转换酶抑制剂与钾通道调节剂的组合，其制备方法和用途作为药物。

10. 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。

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