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2. 发明授权

US5807875A Amino acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：氨基酸衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5807875A
公开(公告)日：1998-09-15
申请号：US763504
申请日：1996-12-11
申请人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Henri Doods , Heike Andrea Wieland , Klaus-Dieter Willim , Jurgen Krause , Horst Dollinger , Franz Esser , Gerd Schnorrenberg , Michael Entzeroth , Wolfgang Wienen
发明人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Henri Doods , Heike Andrea Wieland , Klaus-Dieter Willim , Jurgen Krause , Horst Dollinger , Franz Esser , Gerd Schnorrenberg , Michael Entzeroth , Wolfgang Wienen
IPC分类号： A61K31/155 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/4245 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/454 , A61K31/47 , A61K38/00 , A61P9/12 , A61P43/00 , C07C237/22 , C07C237/42 , C07C255/60 , C07C257/12 , C07C257/14 , C07C257/18 , C07C259/10 , C07C259/18 , C07C261/04 , C07C275/40 , C07C279/10 , C07C279/12 , C07C279/14 , C07C279/18 , C07C279/36 , C07C307/02 , C07C307/10 , C07C311/08 , C07C311/15 , C07C311/19 , C07C311/39 , C07C311/42 , C07D209/14 , C07D209/16 , C07D209/42 , C07D209/44 , C07D211/28 , C07D213/38 , C07D213/55 , C07D215/12 , C07D215/38 , C07D223/20 , C07D233/24 , C07D233/48 , C07D233/54 , C07D233/64 , C07D233/66 , C07D233/72 , C07D233/88 , C07D235/06 , C07D235/08 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D271/06 , C07D271/07 , C07D295/15 , C07D333/20 , C07D333/36 , C07D401/12 , C07D471/04 , C07K5/072 , C07C273/00 , C07C275/00
CPC分类号： C07D233/64 , C07C237/22 , C07C237/42 , C07C255/60 , C07C257/12 , C07C257/14 , C07C257/18 , C07C259/10 , C07C259/18 , C07C261/04 , C07C275/40 , C07C279/14 , C07C279/18 , C07C279/36 , C07C307/02 , C07C307/10 , C07C311/08 , C07C311/19 , C07C311/39 , C07C311/42 , C07D209/16 , C07D209/42 , C07D209/44 , C07D213/38 , C07D215/38 , C07D223/20 , C07D233/24 , C07D233/48 , C07D233/72 , C07D233/88 , C07D235/06 , C07D249/12 , C07D249/14 , C07D271/07 , C07D295/15 , C07D333/20 , C07D471/04 , C07K5/06095 , A61K38/00 , C07C2101/08 , C07C2101/14 , C07C2103/18 , C07C2103/74
摘要： Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-�(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.
摘要翻译：氨基酸衍生物，适用于治疗肥胖症。以下化合物是以下类别的示例：（R，S）-N 2 - （二苯基乙酰基）-N - [（4-羟基苯基）甲基] -N 5 - （1H-咪唑-2-基） - 甲硅烷基酰胺。

3. 发明授权

US6114390A Amino acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：氨基酸衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US6114390A
公开(公告)日：2000-09-05
申请号：US950113
申请日：1997-10-14
申请人： Wolfhard Engel , Wolfgang Eberlein , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim , Michael Entzeroth , Wolfgang Wienen
发明人： Wolfhard Engel , Wolfgang Eberlein , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim , Michael Entzeroth , Wolfgang Wienen
IPC分类号： A61K38/00 , C07C257/18 , C07C275/24 , C07C275/56 , C07C279/14 , C07C279/24 , C07C279/36 , C07C307/06 , C07C311/35 , C07D209/08 , C07D209/18 , C07D209/24 , C07D209/42 , C07D209/44 , C07D223/20 , C07D233/26 , C07D233/36 , C07D233/72 , C07D233/88 , C07D235/06 , C07D235/08 , C07D239/46 , C07D249/14 , C07D271/06 , C07D307/85 , C07K5/078 , A61K31/17 , C07C275/14
CPC分类号： C07D235/06 , C07C257/18 , C07C275/24 , C07C275/56 , C07C279/14 , C07C279/24 , C07C279/36 , C07C307/06 , C07C311/35 , C07D209/08 , C07D209/18 , C07D209/24 , C07D209/42 , C07D209/44 , C07D223/20 , C07D233/26 , C07D233/36 , C07D233/72 , C07D233/88 , C07D235/08 , C07D239/47 , C07D249/14 , C07D271/06 , C07D307/85 , C07K5/06139 , A61K38/00
摘要： NPY-antagonistic compounds of the formula ##STR1## Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate;(B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate;(C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide-trifluoracetate;(D) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl)phenyl]methyl]-argininamide-trifluoroacetate;(E) (R,S)-N.sup.5 -(Aminoiminomethyl)-N.sup.2 -(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N.sup.5 -methyl-ornithinamide-hydrochloride;(F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N.sup.2 -(diphenyl-acetyl)-argininamide-diacetate;(G) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-argininamide-bis-(trifluoroacetate); and,(H) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylamino-carbonylaminomethyl)phenyl]methyl]-argininamide-trifluoroacetate.
摘要翻译：式（A）（R）-N - [[4-（氨基羰基氨基甲基）苯基]甲基] -N2-双（4-羟基苯基）乙酰基] - 炔丙酰胺 - 三氟乙酸盐; （B）（R）-N - [[4-（氨基羰基氨基甲基）苯基]甲基] -N 2 - [双（4-氯苯基）乙酰基] - 炔丙酰胺 - 三氟乙酸盐; （C）（R）-N - [[4-氨基羰基氨基甲基）苯基]甲基] -N2-（二苯基乙酰基） - 炔丙酰胺 - 三氟乙酸盐; （D）（R）-N2-（二苯基乙酰基）-N - [[4-（乙氧基羰基甲基氨基 - 羰基氨基甲基）苯基]甲基] - 炔丙酰胺 - 三氟乙酸盐; （E）（R，S）-N5-（氨基亚氨基甲基）-N2-（二苯基乙酰基）-N - [（4-羟基苯基）甲基] -N5-甲基 - 鸟氨酰胺 - 盐酸盐; （F）（R）-N - [[4-（氨基羰基甲基）苯基]甲基] -N2-（二苯基 - 乙酰基） - 鸟氨酰胺 - 二乙酸酯; （G）（R）-N2-（二苯基乙酰基）-N - [[4-（乙基氨基羰基氨基 - 甲基） - 苯基]甲基] - 炔丙酰胺 - 双 - （三氟乙酸盐）和（H）（R）-N2-（二苯基乙酰基）-N - [[4-（乙氧基羰基氨基 - 羰基氨基甲基）苯基]甲基] - 炔丙酰胺 - 三氟乙酸盐。

4. 发明授权

US5641772A Condensed diazepinones, processes for preparing them and agents containing these compounds for treating diseases of the central nervous system and for promoting cerebral blood circulation 失效
标题翻译：浓缩二氮杂酮，其制备方法和含有这些化合物的药物，用于治疗中枢神经系统疾病和促进脑血液循环
公开(公告)号：US5641772A
公开(公告)日：1997-06-24
申请号：US421108
申请日：1995-04-13
申请人： Wolfgang Eberlein , Gerhard Mihm , Wolfhard Engel , Klaus Rudolf , Henri Doods , Harald Ziegler , Michael Entzeroth
发明人： Wolfgang Eberlein , Gerhard Mihm , Wolfhard Engel , Klaus Rudolf , Henri Doods , Harald Ziegler , Michael Entzeroth
IPC分类号： A61K31/55 , A61K31/5513 , A61K31/5517 , A61P9/00 , A61P9/06 , A61P25/00 , A61P25/28 , C07D243/12 , C07D243/38 , C07D401/06 , C07D403/06 , C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04 , C07D495/14 , C07D243/10
CPC分类号： C07D401/06 , C07D471/04 , C07D487/04 , C07D495/04
摘要： New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
摘要翻译：（I）其中B表示二价基团之一的新的浓缩二氮杂酮通式I（I）其中B表示二价基团之一，其中X， m，n和R 1至R 7如本文所定义，以及其与无机或有机酸的盐及其制备方法。这些化合物可用于改善或归一化动脉硬化诱导的脑血流紊乱，用于治疗中枢神经系统疾病，特别是阿尔茨海默病和帕金森病，以及用于治疗心动过缓和缓慢心律失常的迷走神经心脏起搏器，以及用于改善记忆性能。

5. 发明授权

US5610155A Condensed diazepinones, processes for preparing them and agents containing these compounds for treating diseases of the central nervous system and for promoting cerebral blood circulation 失效
公开(公告)号：US5610155A
公开(公告)日：1997-03-11
申请号：US457061
申请日：1995-06-01
申请人： Wolfgang Eberlein , Gerhard Mihm , Wolfhard Engel , Klaus Rudolf , Henri Doods , Harald Ziegler , Michael Entzeroth
发明人： Wolfgang Eberlein , Gerhard Mihm , Wolfhard Engel , Klaus Rudolf , Henri Doods , Harald Ziegler , Michael Entzeroth
IPC分类号： C07D401/06 , C07D471/04 , C07D487/04 , C07D495/04 , A61K31/55 , C07D243/10
CPC分类号： C07D401/06 , C07D471/04 , C07D487/04 , C07D495/04
摘要： New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.

6. 发明授权

US06344449B1 Modified aminoacids, pharmaceuticals containing these compounds and method for their production 有权
标题翻译：改性氨基酸，含有这些化合物的药物及其制备方法
公开(公告)号：US06344449B1
公开(公告)日：2002-02-05
申请号：US09254281
申请日：1999-10-12
申请人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Helmut Pieper , Henri Doods , Gerhard Hallermayer , Michael Entzeroth , Wolfgang Wienen
发明人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Helmut Pieper , Henri Doods , Gerhard Hallermayer , Michael Entzeroth , Wolfgang Wienen
IPC分类号： C07D24310
CPC分类号： G01N33/9406 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/549 , A61K38/00 , C07K5/06078 , C07K5/06191 , Y02P20/55
摘要： The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
摘要翻译：本发明涉及通式化合物A，Z，X，n，m，R，R 2，R 3，R 4和R 11的修饰氨基酸如权利要求1至5中所定义，它们的互变异构体，它们的非对映体，其对映异构体，其混合物其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，含有这些化合物的药物组合物，其用途及其制备方法以及其用于制备和纯化抗体和标记化合物的用途 RIA和ELISA测定以及神经递质研究中的诊断或分析辅助。

7. 发明授权

US07498325B2 Modified amino acids, pharmaceuticals containing these compounds and method for their production 有权
公开(公告)号：US07498325B2
公开(公告)日：2009-03-03
申请号：US10835495
申请日：2004-04-29
申请人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Helmut Pieper , Henri Doods , Gerhard Hallermayer , Michael Entzeroth , Wolfgang Wienen
发明人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Helmut Pieper , Henri Doods , Gerhard Hallermayer , Michael Entzeroth , Wolfgang Wienen
IPC分类号： C07D498/02 , C07D285/22 , A61K31/50
CPC分类号： G01N33/58 , A61K31/4745 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/549 , G01N33/9406
摘要： The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.

8. 发明授权

US06040289A Amino acid derivatives, medicaments containing said compounds and methods of producing said compounds 失效
标题翻译：氨基酸衍生物，含有所述化合物的药物和制备所述化合物的方法
公开(公告)号：US06040289A
公开(公告)日：2000-03-21
申请号：US77663
申请日：1998-05-29
申请人： Wolfgang Eberlein , Wolfhard Engel , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim
发明人： Wolfgang Eberlein , Wolfhard Engel , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim
IPC分类号： C07D277/20 , A61K31/00 , A61K31/165 , A61K31/22 , A61K31/223 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/44 , A61P3/00 , A61P3/10 , A61P5/00 , A61P5/14 , A61P9/00 , A61P13/00 , A61P13/12 , A61P25/08 , A61P35/00 , A61P43/00 , C07C279/14 , C07C279/22 , C07C279/24 , C07D209/18 , C07D213/72 , C07D213/75 , C07D213/81 , C07D277/42 , C07D277/48 , A61K38/00 , A01N37/18
CPC分类号： C07D213/75 , C07C279/22 , C07C279/24 , C07D209/18 , C07D213/81 , C07D277/48
摘要： The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
摘要翻译： PCT No.PCT / EP96 / 05214 Sec。 371日期：1998年5月29日 102（e）日期1998年5月29日PCT提交1996年11月26日PCT公布。第WO97 / 19914号公报日期1996年6月5日本发明涉及通式的新氨基酸衍生物，其中R，U，V，Y，n，m和R 1至R 3如权利要求1所定义，其互变异构体，非对映异构体，对映体，其混合物和盐特别是其与无机或有机酸或碱的生理上可接受的盐，其具有有价值的药理学性质，特别是选择性的NPY拮抗性质，含有这些化合物的药物组合物，其用途及其制备方法。

9. 发明授权

US5962530A Amino acid derivatives, medicaments containing said compounds and methods of producing them 失效
标题翻译：氨基酸衍生物，含有所述化合物的药物及其制备方法
公开(公告)号：US5962530A
公开(公告)日：1999-10-05
申请号：US77629
申请日：1998-05-29
申请人： Wolfhard Engel , Wolfgang Eberlein , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim
发明人： Wolfhard Engel , Wolfgang Eberlein , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim
IPC分类号： G01N33/534 , A61K31/00 , A61K31/165 , A61P5/24 , C07C279/18 , C07C279/24 , G01N33/60 , G01N33/68 , A01N47/28 , A01N37/18 , C07C233/31 , C07C275/18
CPC分类号： C07C279/18 , C07C279/24 , G01N33/60 , G01N33/68 , C07C2101/14
摘要： The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
摘要翻译： PCT No.PCT / EP96 / 05217 Sec。 371日期：1998年5月29日 102（e）日期1998年5月29日PCT提交1996年11月26日PCT公布。第WO97 / 19913号公报日期1996年6月5日本发明涉及通式的新氨基酸衍生物，其中R，U，V，Y，n，m和R 1至R 3如权利要求1所定义，其互变异构体，非对映异构体，对映体，其混合物和盐特别是其与无机或有机酸或碱的生理上可接受的盐，其具有有价值的药理学性质，特别是选择性的NPY拮抗性质，含有这些化合物的药物组合物，其用途及其制备方法。

10. 发明授权

US5179090A Condensed diazepinones and medicaments containing these compounds 失效
标题翻译：浓缩二氮杂酮和含有这些化合物的药物
公开(公告)号：US5179090A
公开(公告)日：1993-01-12
申请号：US779203
申请日：1991-10-18
申请人： Klaus Rudolf , Wolfhard Engel , Wolfgang Eberlein , Gunter Trummlitz , Gerhard Mihm , Henri Doods , Norbert Mayer
发明人： Klaus Rudolf , Wolfhard Engel , Wolfgang Eberlein , Gunter Trummlitz , Gerhard Mihm , Henri Doods , Norbert Mayer
IPC分类号： C07D487/18 , C07D519/00
CPC分类号： C07D487/18 , C07D519/00
摘要： Condensed diazepinones of general formula I ##STR1## in which]B represents one of the divalent groups ##STR2## X is a .dbd.CH-- group or a nitrogen atom,R represents a lower alkyl radical, which may optionally be further substituted by a phenyl optionally carrying halogen, methyl or methoxy,R.sup.4 and R.sup.5 represent hydrogen, halogen or lower alkyl,R.sup.6 is hydrogen, chlorine or methyl,R.sup.7 and R.sup.8 denote lower alkyl, R.sup.8 also additionally denotes halogen, andm, n, o and p represent the numbers 0, 1, 2 or 3 with the following limitations: the sum of m+n and the sum of o+p each denote the numbers 1, 2 or 3, the sum of n+o and the sum of m+p each denote the numbers 1, 2, 3, 4 or 5, wherein, however, the sum of m+n+o+p must always be greater than 2, andA.sup.1, A.sup.2, A.sup.3 and A.sup.4 denote hydrogen, or, for the case where m, n, o and p each denote the number 1, A.sup.1 and A.sup.2 together or A.sup.3 and A.sup.4 together represent an ethylene bridge,are suitable for the treatment of cholinergically induced spasms and motility disorders of the gastrointestinal tract and in the region of the evacuating bile ducts, for the symptomatic treatment of cystitis and of spasms from urelithiasis, for the treatment of relative incontinence, for the symptomatic treatment of bronchial asthma and bronchitis, and for the treatment of ischaemic heart diseases. The compounds are characterized by good selectivity.
摘要翻译：（I）其中] + E，crc / B /表示二价基团之一的通式I的缩二氮杂酮类（I）其中一个二价基团（S）（T） V）X是= CH-基或氮原子，R表示低级烷基，其可以任选地被任选地带有卤素，甲基或甲氧基的苯基进一步取代，R4和R5代表氢，卤素或低级烷基，R6 是氢，氯或甲基，R7和R8表示低级烷基，R8还另外表示卤素，m，n，o和p表示数字0,1,2或3，具有以下限制：m + n和 o + p的和表示数字1,2或3，n + o和m + p之和各自表示数字1,2,3,4或5，其中，然而， m + n + o + p必须始终大于2，A1，A2，A3和A4表示氢，或者对于m，n，o和p分别表示数字1，A1和A2一起或A3 和A4一起代表乙烯桥，适合于处理o f胆碱能诱发胃肠道的痉挛和运动障碍以及排空胆管区域，用于膀胱炎和尿毒症痉挛的症状治疗，用于治疗相对失禁，用于支气管哮喘和支气管炎的症状治疗，并用于治疗缺血性心脏病。该化合物的特征在于良好的选择性。

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