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1. 发明授权

US4931436A Condensed diazepinones, processes for preparing them and pharmaceutical compositions containing these compounds 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组合物
公开(公告)号：US4931436A
公开(公告)日：1990-06-05
申请号：US230406
申请日：1988-08-09
申请人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gerhard Mihm , Norbert Mayer , Adriaan De Jonge , Klaus Rudolf
发明人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gerhard Mihm , Norbert Mayer , Adriaan De Jonge , Klaus Rudolf
IPC分类号： C07D471/04 , C07D495/04
CPC分类号： C07D471/04 , C07D495/04
摘要： New condensed diazepinones of general formula I are described ##STR1## wherein B represents one of the divalent groups ##STR2## and X.sup.1, X.sup.2, A, R.sup.1 to R.sup.10 and Z are defined as in the specification.
摘要翻译：描述通式I的新的缩合二氮杂酮其中B表示二价基团之一，其中X 1，X 2，A，R 1至R 10和Z如说明书中所定义。

2. 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。

3. 发明授权

US5011836A Agents for the treatment of acute and chronic obstructive respiratory passage diseases 失效
标题翻译：用于治疗急性和慢性阻塞性呼吸道疾病的药剂
公开(公告)号：US5011836A
公开(公告)日：1991-04-30
申请号：US438827
申请日：1989-11-17
申请人： Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Klaus Rudolf , Henri Doods , Norbert Mayer
发明人： Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Klaus Rudolf , Henri Doods , Norbert Mayer
IPC分类号： C07D223/20 , A61K31/55 , A61P11/00 , C07D401/12
CPC分类号： A61K31/55 , Y10S514/826
摘要： A method for treating abstructive respiratory passage disorders which comprises the use of 5,11-dihydro-11-[[(1-methyl-4-piperidinyl)-amino]carbonyl]-6H-dibenz[b,e]azepin-6-one; 5,11-dihydro-11-[(1-methyl-4-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-one, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-one, alone or in combination.
摘要翻译：一种治疗阻塞性呼吸道传播障碍的方法，其包括使用5,11-二氢-11 - [[（1-甲基-4-哌啶基） - 氨基]羰基] -6H-二苯并[b，e]氮杂- 一; 5,11-二氢-11 - [（1-甲基-4-哌嗪基）乙酰基] -6H-二苯并[b，e]氮杂-6-酮，5,11-二氢-11 - [（4-甲基-1- - 哌嗪基）乙酰基] -6H-二苯并[b，e]氮杂-6-酮，单独或组合使用。

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.

7. 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。

8. 发明授权

US5468766A 1,5,6,7-tetrahydro-4H-indazol-4-ones 失效
标题翻译： 1,5,6,7-四氢-4H-吲唑-4-酮
公开(公告)号：US5468766A
公开(公告)日：1995-11-21
申请号：US128506
申请日：1993-09-29
申请人： Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Klaus Rudolf , Gunther Engelhardt
发明人： Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Klaus Rudolf , Gunther Engelhardt
IPC分类号： A61K31/415 , A61P25/04 , A61P29/00 , C07D231/54 , C07D231/56
CPC分类号： A61K31/415
摘要： Pharmaceutical compositions are described which contain 1,5,6,7-tetrahydro-4H-indazol-4-ones of the formula ##STR1## some of these substances themselves being new. The pharmaceutical compositions may be used as analgesics, antipyretics and antiphlogistics.
摘要翻译：描述了包含式（I）的1,5,6,7-四氢-4H-吲唑-4-酮的药物组合物（I）这些物质中的一些本身是新的。药物组合物可用作止痛剂，解热药和消炎药。

9. 发明授权

US06521609B1 Use of CGRP antagonists and CGRP release inhibitors for combating menopausal hot flushes 有权
标题翻译：使用CGRP拮抗剂和CGRP释放抑制剂来对抗更年期热潮红
公开(公告)号：US06521609B1
公开(公告)日：2003-02-18
申请号：US09614343
申请日：2000-07-12
申请人： Henri Doods , Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel
发明人： Henri Doods , Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel
IPC分类号： A61K31454
CPC分类号： A61K31/445 , A61K31/00 , A61K31/496 , A61K31/513 , A61K31/5415 , A61K31/551
摘要： A method for treating menopausal hot flushes using CGRP antagonists and/or CGRP release inhibitors and the corresponding pharmaceutical compositions containing as active substance one or more CGRP antagonists and/or CGRP release inhibitors, and the preparation thereof.
摘要翻译：一种使用CGRP拮抗剂和/或CGRP释放抑制剂治疗绝经期潮热的方法以及含有一种或多种CGRP拮抗剂和/或CGRP释放抑制剂作为活性物质的相应药物组合物及其制备方法。

10. 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。

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