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1. 发明授权

US4665016A Chromogenic compounds, a process for their preparation and their use 失效
标题翻译：显色化合物，其制备方法及其用途
公开(公告)号：US4665016A
公开(公告)日：1987-05-12
申请号：US843919
申请日：1986-03-21
申请人： Helmut Heber , Reinhard Eberle , Volker Teetz
发明人： Helmut Heber , Reinhard Eberle , Volker Teetz
IPC分类号： G01N33/52 , C07K1/06 , C07K5/00 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/10 , C07K5/103 , C07K5/117 , C07K7/06 , C07K14/745 , C12Q1/37 , C12Q1/56 , G01N33/50 , C12Q1/38
CPC分类号： C07K7/06 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/1002 , C07K5/101 , C07K5/1024 , C12Q1/37 , C12Q1/56 , C12Q2337/10 , C12Q2337/12 , Y02P20/55 , Y10S930/28
摘要： Chromogenic compounds of the formula I ##STR1## and a process for their preparation are described, X denoting a hydrogen atom, a protective group customarily used in peptide chemistry or a group which irreversibly blocks the terminal amino group,A and P being identical or different and denoting an alpha-, beta- or gamma-amino acid which is composed of 2 to 15 carbon atoms with up to 3 nitrogen atoms, 2 sulfur atoms and 6 oxygen atoms, the side-chain of which can be substituted, and P also denoting a dipeptide formed from amino acids of these types,B denoting arginine, homoarginine, lysine, homolysine, ornithine or histidine andR denoting a substituent in the 2- or 3-position.The compounds can be used as substrates for the direction and the quantitative determination of hydrolytic enzymes of enzyme class 3.4.21.
摘要翻译：描述了式I（I）的显色化合物及其制备方法，X表示氢原子，肽化学中通常使用的保护基或不可逆阻断末端氨基的基团，A和P为相同或不同，并且表示由具有至多3个氮原子，2个硫原子和6个氧原子的2至15个碳原子组成的α-，β-或γ-氨基酸，其侧链可以被取代，并且P还表示由这些类型的氨基酸形成的二肽，B表示精氨酸，高精氨酸，赖氨酸，高赖氨酸，鸟氨酸或组氨酸，R表示2-或3-位的取代基。该化合物可用作酶类3.4.21的水解酶的方向和定量测定的底物。

2. 发明授权

US4508644A Chromogenic compounds, a process for their preparation and their use 失效
标题翻译：显色化合物，其制备方法及其用途
公开(公告)号：US4508644A
公开(公告)日：1985-04-02
申请号：US554942
申请日：1983-11-25
申请人： Helmut Heber , Reinhard Eberle , Volker Teetz
发明人： Helmut Heber , Reinhard Eberle , Volker Teetz
IPC分类号： G01N33/52 , C07K1/06 , C07K5/00 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/10 , C07K5/103 , C07K5/117 , C07K7/06 , C07K14/745 , C12Q1/37 , C12Q1/56 , G01N33/50 , C07C103/52
CPC分类号： C07K7/06 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/1002 , C07K5/101 , C07K5/1024 , C12Q1/37 , C12Q1/56 , C12Q2337/10 , C12Q2337/12 , Y02P20/55 , Y10S930/28
摘要： Chromogenic compounds of the formula I ##STR1## and a process for their preparation are described, X denoting a hydrogen atom, a protective group customarily used in peptide chemistry or a group which irreversibly blocks the terminal amino group,A and P being identical or different and denoting an alpha-, beta- or gamma-amino acid which is composed of 2 to 15 carbon atoms with up to 3 nitrogen atoms, 2 sulfur atoms and 6 oxygen atoms, the side-chain of which can be substituted, and P also denoting a dipeptide formed from amino acids of these types,B denoting arginine, homoarginine, lysine, homolysine, ornithine or histidine andR denoting a substituent in the 2- or 3-position.The compounds can be used as substrates for the detection and the quantitative determination of hydrolytic enzymes of enzyme class 3.4.21.
摘要翻译：描述了式I（I）的显色化合物及其制备方法，X表示氢原子，肽化学中通常使用的保护基或不可逆阻断末端氨基的基团，A和P为相同或不同，并且表示由具有至多3个氮原子，2个硫原子和6个氧原子的2至15个碳原子组成的α-，β-或γ-氨基酸，其侧链可以被取代，并且P还表示由这些类型的氨基酸形成的二肽，B表示精氨酸，高精氨酸，赖氨酸，高赖氨酸，鸟氨酸或组氨酸，R表示2-或3-位的取代基。该化合物可用作酶类3.4.21的水解酶的检测和定量测定的底物。

3. 发明授权

US4457866A Chromogenic compounds and their use as enzyme substrates 失效
标题翻译：显色化合物及其作为酶底物的用途
公开(公告)号：US4457866A
公开(公告)日：1984-07-03
申请号：US435610
申请日：1982-10-19
申请人： Hermann E. Karges , Helmut Heber , Rainer Uhmann , Volker Teetz , Rolf Geiger
发明人： Hermann E. Karges , Helmut Heber , Rainer Uhmann , Volker Teetz , Rolf Geiger
IPC分类号： E04F15/02 , C07K5/04 , C07K5/062 , C07K5/072 , C07K5/083 , C07K5/087 , C07K5/103 , C07K5/107 , C07K7/06 , C12Q1/37 , C07C103/52 , C12Q1/00
CPC分类号： C07K7/06 , C07K5/06026 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06095 , C07K5/06104 , C07K5/0808 , C07K5/0812 , C07K5/1013 , C07K5/1016 , C12Q1/37 , C12Q2337/12 , Y10S530/802 , Y10S930/28
摘要： What are disclosed are chromogenic peptides useful as substrates for the detection and determination of enzymes having a hydrolytic action and methods for detecting and determining enzymes with such peptides.
摘要翻译：所公开的是可用作检测和测定具有水解作用的酶的底物的显色肽以及用这些肽检测和测定酶的方法。

4. 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。

5. 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。

6. 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。

7. 发明授权

US5068351A Process for the preparation of n octahydropenta (6) pyrrole carboxylates 失效
标题翻译：制备N-甲基吗啉的方法（6）羧甲基纤维素
公开(公告)号：US5068351A
公开(公告)日：1991-11-26
申请号：US560004
申请日：1990-07-27
申请人： Volker Teetz , Hans Wissmann , Hansjorg Urbach
发明人： Volker Teetz , Hans Wissmann , Hansjorg Urbach
IPC分类号： C07K14/81 , A61K38/55 , A61P43/00 , C07K1/10 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/078
CPC分类号： C07K5/0222
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 denotes hydrogen or an organic radical, R.sup.1 denotes an organic radical, R.sup.2 and R.sup.3 are identical or different and denote hydrogen or an organic radical, and R.sup.4 and R.sup.5, together with the atoms bearing them, form a monocyclic, bicyclic or tricyclic heterocyclic ring system having 5 to 15 carbon atoms, which process comprises reacting compounds of the formula II defined in the description with compounds of the formula IV defined in the description, in the presence of phosphinic anhydrides of the formula III, where appropriate eliminating radicals which have been introduced to protect other functional groups and, where appropriate, esterifying free carboxyl groups in a manner known per se.
摘要翻译：本发明涉及一种制备式I化合物（I）的方法，其中n为1或2，R表示氢或有机基团，R1表示有机基团，R2和R3相同或不同并且表示氢或有机基团，并且R 4和R 5与带有它们的原子一起形成具有5至15个碳原子的单环，双环或三环杂环体系，该方法包括使在描述中定义的式II化合物在描述中定义的式IV化合物，在式III的次膦酸酐存在下，其中适当地除去已经引入以保护其它官能团的基团，并且在适当的情况下以本身已知的方式酯化游离羧基。

8. 发明授权

US4797471A Peptide derivatives having an inhibitory action on hydroxylating enzymes, a process for their preparation, agents containing them, and their use 失效
标题翻译：对羟化酶具有抑制作用的肽衍生物，其制备方法，含有它们的药剂及其用途
公开(公告)号：US4797471A
公开(公告)日：1989-01-10
申请号：US941066
申请日：1986-12-12
申请人： Volker Teetz , Stephan Henke , Dietrich Brocks , Hartmut Hanauske-Abel , Volkmar Gunzler
发明人： Volker Teetz , Stephan Henke , Dietrich Brocks , Hartmut Hanauske-Abel , Volkmar Gunzler
IPC分类号： C07K5/08 , C07K5/09 , C07K14/81
CPC分类号： C07K5/0815
摘要： The invention relates to peptide derivatives of the formula ##STR1## in which ##STR2## represents an acyl radical, B represents the radical of a dipeptide composed of a N.sup..omega. -acylated basic .alpha.-amino acid and another .alpha.-amino acid, and W represents hydroxyl or optionally substituted amino, to a process for their preparation, to agents containing them, and to their use.
摘要翻译：本发明涉及式“IMAGE”的肽衍生物，其中“IMAGE”表示酰基，B表示由Nω-酰化的碱式α-氨基酸和另一种α-氨基酸组成的二肽的基团，W表示W 表示羟基或任选取代的氨基，其制备方法，含有它们的试剂及其用途。

9. 发明授权

US4677192A Process for the separation of mixtures of insulin, insulin derivatives and, where appropriate, impurities 失效
标题翻译：分离胰岛素，胰岛素衍生物和适当的杂质的混合物的方法
公开(公告)号：US4677192A
公开(公告)日：1987-06-30
申请号：US804325
申请日：1985-12-04
申请人： Rainer Obermeier , Volker Teetz , Jurgen Ludwig
发明人： Rainer Obermeier , Volker Teetz , Jurgen Ludwig
IPC分类号： A61K38/28 , C07G15/00 , C07K1/14 , C07K1/16 , C07K1/20 , C07K14/575 , C07K14/62 , C07K14/625 , A61K37/26 , C07K7/40
CPC分类号： C07K14/625
摘要： A method for separating insulin or certain insulin derivatives from mixtures containing the same by chromatography of the mixture on a column filled with silica gel having a particle size between 40 and 500 microns with an eluant mixture comprising chloroform, methanol, water and triethylamine.
摘要翻译：一种通过色谱法分离胰岛素或某些胰岛素衍生物的方法，该混合物在填充有40-500微米粒度的硅胶柱上，用含有氯仿，甲醇，水和三乙胺的洗脱剂混合物进行色谱分离。

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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