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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US5256687A Pharmaceutical composition for the treatment of high blood pressure 失效
标题翻译：用于治疗高血压的药物组合物
公开(公告)号：US5256687A
公开(公告)日：1993-10-26
申请号：US979390
申请日：1992-11-19
申请人： Reinhard Becker , Rolf Geiger , Rainer Henning , Volker Teetz , Hansjorg Urbach
发明人： Reinhard Becker , Rolf Geiger , Rainer Henning , Volker Teetz , Hansjorg Urbach
IPC分类号： A61K31/40 , A61K31/635 , A61K31/34 , A61K31/405
CPC分类号： A61K31/40 , A61K31/635 , Y10S514/869
摘要： The invention relates to a pharmaceutical composition comprising an angiotensin converting enzyme inhibitor (trandolpril or pamipril) and a loop diuretic (Furosemide or piretanide), and to their use for the treatment of high blood pressure.
摘要翻译：本发明涉及包含血管紧张素转换酶抑制剂（群多普利或帕米普尔）和环利尿剂（呋塞米或吡雷尼亚）的药物组合物及其用于治疗高血压的药物组合物。

6. 发明授权

US5101039A Azabicycloamino carboxylic acid intermediates 失效
标题翻译：羧甲基纤维素羧酸中间体
公开(公告)号：US5101039A
公开(公告)日：1992-03-31
申请号：US468567
申请日：1990-01-23
申请人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Rolf Geiger , Reinhard Becker , Holger Gaul
发明人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Rolf Geiger , Reinhard Becker , Holger Gaul
IPC分类号： A61K38/55 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P7/10 , A61P9/08 , A61P9/12 , C07D209/02 , C07D209/08 , C07D209/32 , C07D209/34 , C07D209/42 , C07D209/52 , C07D215/22 , C07D215/227 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06
CPC分类号： C07D215/227 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/52 , C07K5/0222 , A61K38/00
摘要： Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0, 1 or 2, R.sub.1 denotes hydrogen (C.sub.1 -C.sub.6)-alkyl which can optionally be substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, [which can be substituted as defined previously in the aryl radical], a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 - C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4 -alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process of the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.

7. 发明授权

US5008400A Bicyclic aminoacids as intermediates 失效
标题翻译：双环氨基酸作为中间体
公开(公告)号：US5008400A
公开(公告)日：1991-04-16
申请号：US673605
申请日：1984-11-21
申请人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Rolf Geiger , Reinhard Becker , Holger Gaul
发明人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Rolf Geiger , Reinhard Becker , Holger Gaul
IPC分类号： A61K38/55 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P7/10 , A61P9/08 , A61P9/12 , C07D209/02 , C07D209/08 , C07D209/32 , C07D209/34 , C07D209/42 , C07D209/52 , C07D215/22 , C07D215/227 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06
CPC分类号： C07D215/227 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/52 , C07K5/0222 , A61K38/00
摘要： Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0,1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally by substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.2 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 - C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4)-alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process for the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.

8. 发明授权

US4933361A Derivatives of bicyclic aminoacids agents containing these compounds and their use 失效
标题翻译：含有这些化合物的双环氨基酸试剂的衍生物及其用途
公开(公告)号：US4933361A
公开(公告)日：1990-06-12
申请号：US346339
申请日：1989-04-28
申请人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Rolf Geiger , Reinhard Becker , Holger Gaul
发明人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Rolf Geiger , Reinhard Becker , Holger Gaul
IPC分类号： A61K38/55 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P7/10 , A61P9/08 , A61P9/12 , C07D209/02 , C07D209/08 , C07D209/32 , C07D209/34 , C07D209/42 , C07D209/52 , C07D215/22 , C07D215/227 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06
CPC分类号： C07D215/227 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/52 , C07K5/0222 , A61K38/00
摘要： Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0, 1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally be substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.6 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4 -alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process of the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.
摘要翻译：公开了式I的顺式，外转和反式化合物，其中n表示0,1或2，R 1表示氢，可任选被氨基取代的（C 1 -C 6） - 烷基，（C 1 -C 6 - （C 5 -C 9） - 环烷基，（C 5 -C 9） - 环烯基，（C 5 -C 7） - 环烷基 - （C 1 -C 4） - 烷基，芳基或部分氢化的芳基，在每种情况下均可被（C 1 -C 2） - 烷基，（C 1 -C 2） - 烷氧基或卤素，芳基 - （C 1 -C 4） - 烷基取代，在芳基/，单环或双环硫或氮和/或氮杂环基或天然存在的氨基酸的侧链中，R 2表示氢，（C 1 -C 6） - 烷基，（C 2 -C 6） - 烯基或芳基 - （C1-C4） - 烷基，Y表示氢或羟基，Z表示氢或Y，Z表示氧，X表示（C1-C6） - 烷基，（C2-C6） - 烯基，（C6-C9）环烷基或芳基，其可以被（C 1 -C 4） - 烷基，（C 1 -C 4） - 烷氧基，羟基，卤素，硝基，氨基，（C 1 -C 4）烷基氨基，二 - （C 1 -C 4 - 烷基氨基或亚甲二氧基或吲哚-3-基）或其生理上可接受的盐，其制备方法，含有它们的试剂，它们作为药物的用途和制备它们的中间体。

9. 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。

10. 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。

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