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1. 发明授权

US5684016A Method of treating cardiac insufficiency 失效
标题翻译：治疗心功能不全的方法
公开(公告)号：US5684016A
公开(公告)日：1997-11-04
申请号：US445543
申请日：1995-05-22
申请人： Rainer Henning , Hansjorg Urbach , Volker Teetz , Rolf Geiger , Bernward Scholkens
发明人： Rainer Henning , Hansjorg Urbach , Volker Teetz , Rolf Geiger , Bernward Scholkens
IPC分类号： A61K38/00 , A61K38/55 , C07K5/02 , A61K31/47 , C07D217/26
CPC分类号： C07K5/0222 , A61K38/556
摘要： The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 and R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
摘要翻译：本发明涉及通过使用其中n为1或2的式I（I）的化合物治疗心功能不全的方法，R 1，R 2，R 2和R 3相同或不同，并且各自表示氢或有机基团并且R4和R5与携带它们的原子一起形成单环，双环或三环杂环体系。本发明还涉及式I化合物和含有这些化合物用于治疗上述疾病的药剂。

2. 发明授权

US5403856A Method of treating cardiac insufficiency using angiotensin-converting enzyme inhibitors 失效
标题翻译：使用血管紧张素转换酶抑制剂治疗心功能不全的方法
公开(公告)号：US5403856A
公开(公告)日：1995-04-04
申请号：US188745
申请日：1994-01-31
申请人： Rainer Henning , Hansjorg Urbach , Volker Teetz , Rolf Geiger , Bernward Scholkens
发明人： Rainer Henning , Hansjorg Urbach , Volker Teetz , Rolf Geiger , Bernward Scholkens
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07K5/02 , C07K5/06 , C12N9/99 , A61K31/40
CPC分类号： A61K38/556 , C07K5/0222 , Y10S514/913
摘要： The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
摘要翻译：本发明涉及通过使用其中n为1或2的式I（I）的化合物治疗心功能不全的方法，R 1，R 2，R 2和R 3相同或不同，并且各自表示氢或有机基团和R4 R5与携带它们的原子一起形成单环，双环或三环杂环体系。本发明还涉及式I化合物和含有这些化合物用于治疗上述疾病的药剂。

3. 发明授权

US5158959A Decahydroisoquinoline carboxylic acids 失效
标题翻译：十氢异喹啉羧酸
公开(公告)号：US5158959A
公开(公告)日：1992-10-27
申请号：US565900
申请日：1983-12-27
申请人： Rolf Geiger , Volker Teetz , Hansjorg Urbach , Bernward Scholkens , Rainer Henning
发明人： Rolf Geiger , Volker Teetz , Hansjorg Urbach , Bernward Scholkens , Rainer Henning
IPC分类号： A61K38/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61K31/472 , A61P9/12 , C07D209/42 , C07D217/26 , C07D233/64 , C07D241/20 , C07D307/54 , C07D309/10 , C07D317/66 , C07D333/24 , C07D335/02 , C07D339/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/078 , C07K14/81
CPC分类号： C07K5/0222 , C07D217/26 , A61K38/00
摘要： What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.
摘要翻译：所公开的是下式的氨基酸化合物，其中n为0或1，及其盐，所述化合物和具有降血压性质的盐; 制备化合物的方法; 含有该化合物或盐的药物组合物; 以及使用化合物和盐治疗高血压。

4. 发明授权

US5011940A Process for the preparation of bicyclic amino carboxylic acids, intermediates in this process, and their use 失效
标题翻译：制备双环氨基羧酸的方法，该方法中的中间体及其用途
公开(公告)号：US5011940A
公开(公告)日：1991-04-30
申请号：US214457
申请日：1988-07-01
申请人： Hansjorg Urbach , Rainer Henning
发明人： Hansjorg Urbach , Rainer Henning
IPC分类号： C07C233/47 , C07C237/04 , C07C271/22 , C07D209/42 , C07D209/52
CPC分类号： C07D209/52 , C07C271/22 , C07D209/42 , C07C2101/10 , Y02P20/55
摘要： The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which n denotes 1, 2 or 3, R denotes acyl, and R.sup.1 denotes alkyl, cycloalkyl, aralkyl or another carboxyl protective group, which comprises radical cyclization of compounds of the formula II ##STR2## in which n, R and R.sup.1 are as defined above, and Hal denotes chlorine, bromine or iodine, to intermediates in this process, and to their use.
摘要翻译：本发明涉及制备式I化合物（I）的方法，其中n表示1,2或3，R表示酰基，R 1表示烷基，环烷基，芳烷基或其它羧基保护基，其中包括式II（II）化合物的自由基环化，其中n，R和R 1如上所定义，Hal表示氯，溴或碘，在此过程中涉及它们的用途。

5. 发明授权

US4912128A Novel pyrrolidine-2-(1,3-dicarbonyl) derivatives, a process for their preparation, agents containing them, and their use 失效
标题翻译：新型吡咯烷-2-（1,3-二羰基）衍生物，其制备方法，含有它们的试剂及其用途
公开(公告)号：US4912128A
公开(公告)日：1990-03-27
申请号：US179312
申请日：1988-04-08
申请人： Rainer Henning , Franz Hock , Hansjorg Urbach
发明人： Rainer Henning , Franz Hock , Hansjorg Urbach
IPC分类号： A61K31/40 , A61K31/401 , A61K31/44 , A61P25/18 , A61P43/00 , C07D207/08 , C07D207/16 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D207/08 , C07D207/16 , C07D401/14
摘要： Novel pyrrolidine-2-(1,3-dicarbonyl) derivatives, a process for their preparation, agents containing them, and their useThe invention relates to pyrrolidine derivatives of the general formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meaning specified in the description, X denotes oxygen, imino or alkylimino,m is 0-5, n is 0-2 and s is 0 or 1, a process for their preparation, agents containing them, and their use.
摘要翻译：新型吡咯烷-2-（1,3-二羰基）衍生物，其制备方法，含有它们的试剂及其用途本发明涉及通式为“IMAGE”的吡咯烷衍生物，其中R1，R2，R3，R4， R5和R6具有说明书中规定的含义，X表示氧，亚氨基或烷基亚氨基，m为0-5，n为0-2，s为0或1，其制备方法，含有它们的试剂及其用途。

6. 发明授权

US4691022A Process for the preparation of monocyclic, bicyclic and tricyclic aminoacids 失效
标题翻译：制备单环，双环和三环氨基酸的方法
公开(公告)号：US4691022A
公开(公告)日：1987-09-01
申请号：US623200
申请日：1984-06-21
申请人： Rainer Henning , Hansjorg Urbach
发明人： Rainer Henning , Hansjorg Urbach
IPC分类号： C07D207/16 , C07D207/20 , C07D209/08 , C07D209/42 , C07D209/52 , C07D209/54 , C07D209/72 , C07D209/96 , C07C103/52
CPC分类号： C07D209/54 , C07D207/16 , C07D207/20 , C07D209/08 , C07D209/42 , C07D209/52
摘要： The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which R represents hydrogen, alkyl or aralkyl, and R.sup.1 to R.sup.6 denote identical or different radicals hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aralkyl or aryl, both being monosubstituted, disubstituted or trisubstituted in the aryl moiety by alkyl, alkoxy, hydroxyl, halogen, nitro, methylenedioxy and/or cyano, or in which two of the radicals R.sup.1 to R.sup.6, together with the carbon atom(s) bearing them form a monocyclic or bicyclic ring system, and the remaining radicals are hydrogen, which process comprises converting, with an oxidizing agent in the presence of a silver salt, a pyrrolidine derivative of the formula II into a .DELTA..sup.1 -pyrroline derivative of the formula III, reacting the latter with hydrogen cyanide or a metal cyanide to form a nitrile of the formula IV, and subjecting the latter to solvolysis with a compound of the formula ROH.
摘要翻译：本发明涉及一种制备式I化合物的方法，其中R代表氢，烷基或芳烷基，R1至R6表示相同或不同的基团氢，烷基，环烷基，环烷基烷基，环烯基烷基，芳烷基或芳基两者在芳基部分中被烷基，烷氧基，羟基，卤素，硝基，亚甲二氧基和/或氰基单取代，二取代或三取代，或其中两个基团R1至R6与带有它们的碳原子一起形成单环或双环系统，其余基团是氢，该方法包括用银盐存在下的氧化剂将式II的吡咯烷衍生物转化为式III的DELTA 1-吡咯啉衍生物使后者与氰化氢或金属氰化物反应以形成式IV的腈，并使其后者与式ROH的化合物溶剂解。

7. 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。

8. 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。

9. 发明授权

US4525301A Process for the preparation of N-alkylated dipeptides and their esters 失效
标题翻译：制备N-烷基化二肽及其酯的方法
公开(公告)号：US4525301A
公开(公告)日：1985-06-25
申请号：US604220
申请日：1984-04-26
申请人： Rainer Henning , Hansjorg Urbach
发明人： Rainer Henning , Hansjorg Urbach
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/435 , A61K31/47 , A61K31/472 , A61K38/00 , A61P9/12 , A61P43/00 , C07C231/00 , C07D207/16 , C07D209/30 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/54 , C07D209/72 , C07D211/60 , C07D217/16 , C07D217/26 , C07D221/22 , C07D277/20 , C07D277/30 , C07K1/00 , C07K1/08 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C07C103/52
CPC分类号： C07C309/00 , C07K5/0222 , Y10S530/80
摘要： The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which n is 1 or 2, R represents hydrogen, an aliphatic, cycloaliphatic, aromatic, araliphatic, cycloaliphatic-aliphatic radical or a radical OR.sup.a or SR.sup.2, in which R.sup.a denotes alkyl, aryl or heteroaryl, R.sup.1 denotes hydrogen, an aliphatic, cycloaliphatic-aliphatic, aromatic, araliphatic, heteroaromatic radical or an aminoacid side chain, R.sup.2 and R.sup.3 are identical or different and denote hydrogen, an aliphatic, cycloaliphatic, aromatic or araliphatic radical, and R.sup.4 +R.sup.5, together with the atoms carrying them, form a heterocyclic ring system, which comprises reacting trifluoromethanesulfonic acid derivatives of the formulae II or III with aminoacid esters of the formulae IV or V respectively. The invention also relates to compounds of the formula III and a process for their preparation.
摘要翻译：本发明涉及制备式I化合物（I）的方法，其中n为1或2，R为氢，脂族，脂环族，芳族，芳脂族，环脂族 - 脂族基或基团ORa 或SR2，其中Ra表示烷基，芳基或杂芳基，R1表示氢，脂族，脂环族 - 脂族，芳族，芳脂族，杂芳族基团或氨基酸侧链，R2和R3相同或不同，表示氢，脂环族，芳族或芳脂族基团，以及R4 + R5与携带它们的原子一起形成杂环体系，其包括将式II或III的三氟甲磺酸衍生物与式IV或V的氨基酸分别反应。本发明还涉及式III的化合物及其制备方法。

10. 发明授权

US5360791A Renin-inhibiting aminodiol derivatives 失效
标题翻译：肾素抑制性氨基二醇衍生物
公开(公告)号：US5360791A
公开(公告)日：1994-11-01
申请号：US1221
申请日：1993-01-06
申请人： Rainer Henning , Hansjorg Urbach , Dieter Ruppert , Bernward Scholkens
发明人： Rainer Henning , Hansjorg Urbach , Dieter Ruppert , Bernward Scholkens
IPC分类号： A61K38/00 , C07D401/12 , C07K5/02 , C07K5/065 , A61K37/02 , C07K5/08
CPC分类号： C07D401/12 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06078 , A61K38/00
摘要： The invention relates to compounds of the formula I ##STR1## in which A denotes a radical of the formula II ##STR2## in which E denotes a CH.sub.2 group or an NR.sup.9 radical,G denotes a radical from the group comprising S, SO, SO.sub.2, O, CO, CS or a direct bond,B denotes an amino acid,D denotes a heterocycle andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.9 are defined in the description, and their salts.The invention in addition relates to a process for the preparation of the compounds of the formula I and their use as pharmaceuticals.
摘要翻译：本发明涉及式I的化合物，其中A表示式II的基团，其中E表示CH 2基团或NR 9基团，G表示包括S，SO的基团，SO 2，O，CO，CS或直接键，B表示氨基酸，D表示杂环，R 1，R 2，R 3，R 4，R 5，R 6和R 9在说明书中定义，及其盐。本发明还涉及制备式I化合物及其作为药物的用途的方法。

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