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1. 发明授权

US4234584A Substituted phenylpiperazine derivatives 失效
标题翻译：取代的苯基哌嗪衍生物
公开(公告)号：US4234584A
公开(公告)日：1980-11-18
申请号：US44948
申请日：1979-06-04
申请人： Rudolf Lattrell , Wilhelm Bartmann , Hermann Gerhards
发明人： Rudolf Lattrell , Wilhelm Bartmann , Hermann Gerhards
IPC分类号： C07D209/08 , C07D209/34 , C07D215/38 , A61K31/495 , C07D401/12
CPC分类号： C07D209/08 , C07D209/34 , C07D215/38
摘要： Phenylpiperazine derivatives of the formula I ##STR1## in which R.sup.1 denotes hydrogen or C.sub.1 -C.sub.6 alkyl,R.sup.2 denotes hydrogen or one or several, identical or different substituents selected from the group of C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, trifluoromethyl, hydroxy, nitro, amino and methylene-dioxy,R.sup.3 denotes hydrogen, hydroxy, C.sub.1 -C.sub.6 alkanoyloxy, andn is 1 or 2,and the physiologically acceptable salts thereof, processes for their manufacture and medicaments containing or consisting of said compounds.
摘要翻译：式I的苯基哌嗪衍生物，其中R 1表示氢或C 1 -C 6烷基，R 2表示氢或一个或多个相同或不同的选自C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，三氟甲基，羟基，硝基，氨基和亚甲基二氧基，R 3表示氢，羟基，C 1 -C 6烷酰氧基，n为1或2，以及其生理学上可接受的盐，其制备方法和含有或由所述化合物组成的药物。

2. 发明授权

US4746661A Phenylpiperazine propyloxyquinolinones and methods for sedating and inhibiting aggression in livestock therewith 失效
标题翻译：苯基哌嗪丙氧基喹啉酮及镇静镇静牲畜的侵害方法
公开(公告)号：US4746661A
公开(公告)日：1988-05-24
申请号：US21523
申请日：1987-02-26
申请人： Rudolf Lattrell , Peter Klatt , Hermann Gerhards , Fritz Bauer
发明人： Rudolf Lattrell , Peter Klatt , Hermann Gerhards , Fritz Bauer
IPC分类号： A61K31/47 , A61K31/495 , A61P25/20 , C07D209/34 , C07D215/22 , C07D215/227 , C07D401/12
CPC分类号： C07D215/227 , C07D209/34
摘要： New substituted phenylpiperazine derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the indicated meaning, and their physiologically tolerated salts and a process for their preparation are described. The compounds exhibit sedative and aggression-inhibiting effects on livestock. Furthermore, compounds of the formula I' ##STR2## in which n, A, R.sup.2, R.sup.3 and R.sup.4 have the indicated meanings, and their physiologically tolerated salts are claimed for the sedation and inhibition of aggression of livestock.
摘要翻译：描述了其中R1和R2具有指定含义的式I（I）的新的取代的苯基哌嗪衍生物及其生理学耐受盐及其制备方法。该化合物对家畜表现出镇静和侵袭抑制作用。此外，其中n，A，R2，R3和R4具有指定含义的式I'（I'）化合物及其生理上耐受的盐被要求用于镇静和抑制家畜侵袭。

3. 发明授权

US4470989A Neuroleptic n-oxacyclyl-alkylpiperidine derivatives 失效
标题翻译：神经精氨酸正氧杂环烷基 - 烷基哌啶衍生物
公开(公告)号：US4470989A
公开(公告)日：1984-09-11
申请号：US389677
申请日：1982-06-18
申请人： Rainer Henning , Rudolf Lattrell , Hermann Gerhards
发明人： Rainer Henning , Rudolf Lattrell , Hermann Gerhards
IPC分类号： C07D405/14 , A61K20060101 , A61K31/335 , A61K31/35 , A61K31/41 , A61K31/415 , A61K31/435 , A61K31/443 , A61K31/445 , A61P25/00 , C07D20060101 , C07D211/00 , C07D235/02 , C07D319/00 , C07D405/00 , C07D405/06 , C07D409/00 , C07D411/00 , C07D411/06 , C07D411/14
CPC分类号： C07D405/14
摘要： Neuroleptically active compounds of the formula ##STR1## wherein R.sup.6 and R.sup.10 are --H or CH.sub.3 ; R.sup.7 and R.sup.8 are independently --H, --F, --Cl, or --CH.sub.3 ; and R.sup.9 is --F, --Cl, --CH.sub.3, or --OCH.sub.3.
摘要翻译：其中R 6和R 10为-H或CH 3的具有下式的神经荧光活性化合物： R 7和R 8独立地为-H，-F，-Cl或-CH 3; 且R 9为-F，-Cl，-CH 3或-OCH 3。

4. 发明授权

US5440046A Substituted imidazoles 失效
标题翻译：取代的咪唑
公开(公告)号：US5440046A
公开(公告)日：1995-08-08
申请号：US250491
申请日：1994-05-27
申请人： Adalbert Wagner , Rainer Henning , Hermann Gerhards , Bernward Scholkens , Jean-Paul Vevert , Jean-Claude Caille
发明人： Adalbert Wagner , Rainer Henning , Hermann Gerhards , Bernward Scholkens , Jean-Paul Vevert , Jean-Claude Caille
IPC分类号： A61K31/415 , A61K31/38 , A61K31/40 , A61K31/41 , A61K31/4155 , A61K31/4164 , A61K31/423 , A61K31/437 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/495 , A61K31/505 , A61K31/519 , A61P9/12 , A61P29/00 , A61P43/00 , C07D233/64 , C07D233/84 , C07D233/90 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D487/04 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds of the formula ##STR1## in which X, Y and Z are identical or different and are N or CR.sup.2, L is an alkylene radical, q is 0 or 1, and A is the radical of a fused heterobicyclic compound. The invention furthermore relates to a process for preparing the said compounds, agents containing these, and the use thereof for angiotensin II receptors.
摘要翻译：本发明涉及其中X，Y和Z相同或不同且为N或CR2的式“IMAGE”的化合物，L为亚烷基，q为0或1，A为稠合杂双环化合物的基团。本发明还涉及制备所述化合物的方法，含有它们的药剂及其用于血管紧张素II受体的方法。

5. 发明授权

US4696913A Novel peptides which are active on the central nervous system and have an action on the cholinergic system 失效
标题翻译：在中枢神经系统上有活性并对胆碱能系统有作用的新型肽
公开(公告)号：US4696913A
公开(公告)日：1987-09-29
申请号：US902615
申请日：1986-09-02
申请人： Rolf Geiger , Hermann Gerhards , Hansjorg Kruse
发明人： Rolf Geiger , Hermann Gerhards , Hansjorg Kruse
IPC分类号： C07K5/04 , A61K38/00 , A61K38/22 , A61P25/00 , C07K5/00 , C07K5/068 , C07K7/00 , C07K7/06 , C07K14/685 , C07K14/695 , A61K37/02 , C07K5/10
CPC分类号： C07K14/695 , C07K14/685 , C07K14/6955 , C07K5/06086 , A61K38/00
摘要： The invention relates to peptides of the formula IR.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 (I)in which R.sup.4 denotes an acyl group, R.sup.5 denotes D-Lys or Lys, A.sup.6 denotes the radical of phenylalanine, N-methylphenylalanine, 4-alkoxyphenylalanine or 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, and R.sup.7 denotes a basic radical, processes for their preparation and their use.
摘要翻译：本发明涉及式ⅠR4-A5-A6-A7（Ⅰ）的肽，其中R4表示酰基，R5表示D-Lys或Lys，A6表示苯丙氨酸，N-甲基苯丙氨酸，4-烷氧基苯丙氨酸或4- 1,2,3,4-四氢异喹啉-3-羧酸，R7表示碱性基团，其制备方法及其用途。

6. 发明授权

US4277470A Heterocyclic spiro-linked amidines, compositions and use thereof 失效
标题翻译：杂环螺连脒，其组合物和用途
公开(公告)号：US4277470A
公开(公告)日：1981-07-07
申请号：US123200
申请日：1980-02-21
申请人： Manfred Forsch , Wolfgang Schaub , Hermann Gerhards
发明人： Manfred Forsch , Wolfgang Schaub , Hermann Gerhards
IPC分类号： A61K31/40 , A61K31/403 , A61P25/24 , A61P25/26 , C07C205/05 , C07D209/96 , C07D401/04 , C07D401/14 , C07D413/04 , C07D471/10 , A61K31/54 , C07D207/22 , C07D295/00
CPC分类号： C07D471/10 , C07C205/05 , C07D209/96
摘要： Heterocyclic, spiro-linked amidines of the formula I ##STR1## and their physiologically acceptable salts, in which (a) n is 1 or 2; (b) R.sup.1 and R.sup.2 are hydrogen or alkyl radicals which, together with the nitrogen atom, can form a 5-, 6- or 7-membered ring which can be substituted by C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.2 -alkoxy, hydroxyl or C.sub.1 -C.sub.4 -alkoxy-carbonyl groups and in which one of the carbon atoms can also be replaced by an oxygen, sulfur or nitrogen atom, it being possible for the nitrogen atom to be substituted by hydrogen, by the formyl group or by a phenyl radical, which can in turn be monosubstituted or polysubstituted by a C.sub.1 to C.sub.4 -alkyl group or an alkoxy, methylenedioxy, hydroxyl, halogen, nitro or amino group, or it being possible for the nitrogen atom to be substituted by a C.sub.1 -C.sub.4 -alkyl group, or in which R.sup.1 represents hydrogen and R.sup.2 represents a C.sub.5 -C.sub.8 -cycloalkyl radical which can be substituted by C.sub.1 -C.sub.4 -dialkylamino groups; (c) R.sup.3 is hydrogen or methyl and (d) R.sup. 4 denotes a phenyl radical which is optionally monosubstituted or polysubstituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, methylenedioxy, hydroxyl, halogen, cyano, nitro, trifluoromethyl, amino, C.sub.2 -C.sub.5 -acylamino or mono- or di-C.sub.1 -C.sub.4 -alkylamino groups, or a thiophene radical, their stereoisomers and optical isomers, processes for their preparation and antidepressive medicaments containing these compounds.
摘要翻译：式（I）的杂环，螺相连的脒和它们的生理上可接受的盐，其中（a）n为1或2; （b）R 1和R 2是氢或烷基，其与氮原子一起可以形成可被C 1 -C 3烷基，C 1 -C 2烷氧基，羟基取代的5-，6-或7-元环或C 1 -C 4 - 烷氧基 - 羰基，并且其中一个碳原子也可以被氧，硫或氮原子替代，氮原子可被氢取代，甲酰基或甲酰基取代苯基，其又可以被C1至C4-烷基或烷氧基，亚甲二氧基，羟基，卤素，硝基或氨基单取代或多取代，或者氮原子可被C1-C4 - 烷基，或其中R1表示氢，R2表示可被C1-C4二烷基氨基取代的C5-C8-环烷基; （c）R 3是氢或甲基，（d）R 4表示苯基，其任选被C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，亚甲二氧基，羟基，卤素，氰基，硝基，三氟甲基，氨基，C 2 -C 5酰基氨基或单或二C 1 -C 4烷基氨基或噻吩基团，它们的立体异构体和光学异构体，其制备方法和含有这些化合物的抗抑郁药物。

7. 发明授权

US5648333A Peptides having bradykinin antagonist action 失效
标题翻译：具有缓激肽拮抗作用的肽
公开(公告)号：US5648333A
公开(公告)日：1997-07-15
申请号：US487442
申请日：1995-06-07
申请人： Stephan Henke , Hiristo Anagnostopulos , Gerhard Breipohl , Jochen Knolle , Jens Stechl , Bernward Scholkens , Hans-Wolfram Fehlhaber , Hermann Gerhards , Franz Hock
发明人： Stephan Henke , Hiristo Anagnostopulos , Gerhard Breipohl , Jochen Knolle , Jens Stechl , Bernward Scholkens , Hans-Wolfram Fehlhaber , Hermann Gerhards , Franz Hock
IPC分类号： A61K38/00 , C07K7/18 , A61K38/17
CPC分类号： C07K7/18 , A61K38/00 , Y10S514/803
摘要： Peptides of the formula IA-B-C-E-F-K-P-G-M-F'-I (I),wherein the terms A, B, C, E, F, K, P, G, M, F', and I are defined in the specification, have bradykinin antagonist action. Their therapeutic utility includes all pathological states which are mediated, caused or supported by bradykinin and bradykinin-related peptides.
摘要翻译：其中术语A，B，C，E，F，K，P，G，M，F'和I在本说明书中定义的式IA-BCEFKPGM-F'-I（I）的肽具有缓激肽拮抗作用。它们的治疗用途包括缓激肽和缓激肽相关肽介导，引起或支持的所有病理状态。

8. 发明授权

US5604251A Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain and their use as angitensin II receptors 失效
标题翻译：咪唑衍生物与联苯基磺酰脲或联苯基磺酰氨基酸侧链及其作为血管紧张素II受体的用途
公开(公告)号：US5604251A
公开(公告)日：1997-02-18
申请号：US479561
申请日：1995-06-07
申请人： Holger Heitsch , Rainer Henning , Adalbert Wagner , Hermann Gerhards , Reinhard Becker , Bernward Sch olkens
发明人： Holger Heitsch , Rainer Henning , Adalbert Wagner , Hermann Gerhards , Reinhard Becker , Bernward Sch olkens
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/64 , A61P9/10 , A61P9/12 , C07D233/84 , C07D233/86 , C07D233/90 , A61K31/505 , A61K31/42 , C07D403/12 , C07D403/14
CPC分类号： C07D233/84 , C07D233/90
摘要： Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain, process for their preparation and their useCompounds of the formula (I) ##STR1## in which R.sup.1 is, for example, ethyl,R.sup.2 is, for example, methyl,n is, for example, zero,R.sup.3 is, for example, COOH, andR.sup.4 is, for example, SO.sub.2 NHCONHCH.sub.3are highly active antagonists of angiotensin II receptors.
摘要翻译：咪唑衍生物与联苯基磺酰脲或联苯磺酰氨基甲酸酯侧链，其制备方法及用途式（I）化合物其中R 1为例如甲基，R 2为例如甲基，n为例如为0，R3为例如COOH，R4为例如SO2NHCONHCH3，为血管紧张素II受体的高效拮抗剂。

9. 发明授权

US5597803A Bradykinin peptides with modifications at the N terminus 失效
标题翻译：在N末端具有修饰的缓激肽肽
公开(公告)号：US5597803A
公开(公告)日：1997-01-28
申请号：US373464
申请日：1995-01-17
申请人： Gerhard Breipohl , Stephan Henke , Jochen Knolle , Bernward Scholkens , Hans-Georg Alpermann , Hermann Gerhards , Klaus Wirth
发明人： Gerhard Breipohl , Stephan Henke , Jochen Knolle , Bernward Scholkens , Hans-Georg Alpermann , Hermann Gerhards , Klaus Wirth
IPC分类号： A61K38/00 , A61K38/04 , A61K38/08 , A61P43/00 , C07K7/06 , C07K7/18 , C07K5/00 , C07K7/00
CPC分类号： C07K7/18 , A61K38/00 , Y02P20/55
摘要： Peptides of the formula IZ-P-A-B-C-E-F-K-(D)Q-G-M-F'-I (I)and the physiologically tolerated salts thereof, are described.They have an excellent bradykinin-antagonistic action.They are obtained by reacting reacting a fragment with a C-terminal free carboxyl group or its activated derivative with a corresponding fragment with an N-terminal free amino group or assembling the peptide stepwise, where appropriate eliminating in the compound obtained in this way one or more protective groups introduced temporarily to protect other functionalities, and where appropriate converting the compounds of the formula I obtained in this way into the physiologically tolerated salt thereof.
摘要翻译：描述了式I Z-P-A-B-C-E-F-K-（D）Q-G-M-F'-I（I）的肽及其生理上耐受的盐。它们具有优异的缓激肽拮抗作用。它们是通过使片段与C末端游离羧基或其活化衍生物与具有N-末端游离氨基的相应片段反应或逐步组装肽而得到的，如果合适，则以这种方式获得的化合物中的一种或临时引入更多的保护基团以保护其它官能团，并且在适当的地方将由此获得的式I化合物转化为其生理上耐受的盐。

10. 发明授权

US5444068A Imidazopyridine derivatives as angiotensin II receptor antagonists, pharmaceuticals, and treatment of hypertension therewith 失效
标题翻译：咪唑并吡啶衍生物作为血管紧张素II受体拮抗剂，药物和治疗高血压
公开(公告)号：US5444068A
公开(公告)日：1995-08-22
申请号：US165655
申请日：1993-12-13
申请人： Holger Heitsch , Adalbert Wagner , Heinz-Werner Kleemann , Hermann Gerhards , Bernward Scholkens
发明人： Holger Heitsch , Adalbert Wagner , Heinz-Werner Kleemann , Hermann Gerhards , Bernward Scholkens
IPC分类号： A61K31/33 , A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/4375 , A61K31/44 , A61K31/495 , A61K31/505 , A61P9/10 , A61P9/12 , C07D235/06 , C07D235/08 , C07D235/22 , C07D235/24 , C07D403/10 , C07D409/06 , C07D471/04 , C07D487/04 , C07D519/00 , A61K31/535
CPC分类号： C07D409/06 , C07D235/08 , C07D471/04 , C07D487/04
摘要： Imidazo-fused iso- and heterocycles, process for their preparation, compositions containing them and their useA compound of the formula ##STR1## in which the symbols have the following meaning: X is a monocyclic radical having 3,4 or 5 ring atoms,R.sup.1,R.sup.2,R.sup.3,R.sup.4,R.sup.12 and R.sup.13 are, for example, an alkyl radical,q is zero or 1,L is, for example, a methylene group andA is the radical, for example, of a heterocycleare highly active as antagonists of angiotensin II receptors. They can be used as pharmaceuticals or diagnostics.
摘要翻译：咪唑稠合的异 - 和杂环，它们的制备方法，含有它们的组合物及其用途下式符号具有以下含义的式“IMAGE”的化合物：X是具有3,4或5个环原子的单环基团， R1，R2，R3，R4，R12和R13是例如烷基，q为0或1，L为例如亚甲基，A为自由基，例如杂环为高活性作为血管紧张素II受体的拮抗剂。它们可以用作药物或诊断。

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