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31. 发明授权

US4288437A 2-[(Amino)-aryl-methylene]-benzo[b]thiophen-3(2H)-ones 失效
标题翻译： 2 - [（氨基） - 芳基 - 亚甲基] - 苯并[b]噻吩-3（2H） - 酮
公开(公告)号：US4288437A
公开(公告)日：1981-09-08
申请号：US173173
申请日：1980-07-28
申请人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Joachim Kahling
发明人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Joachim Kahling
IPC分类号： A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4433 , A61K31/445 , A61K31/495 , A61K31/535 , A61P25/08 , C07D333/62 , C07D333/64 , C07D409/06
CPC分类号： C07D333/62 , C07D333/64
摘要： Compounds of the formula ##STR1## wherein Ar is phenyl; mono- or di-substituted phenyl, where the substituents are one to two halogens, one to two alkyls of 1 to 3 carbon atoms, or one amino, nitro, cyano or trifluoromethyl; or pyridinyl;R is hydrogen, chlorine, methyl or methoxy;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, methyl-(cycloalkyl of 3 to 8 carbon atoms) or --A--R.sub.4,where A is alkylene of 2 to 3 carbon atoms, and R.sub.4 is hydroxyl, methylamino, dimethylamino, N-methyl-ethylamino, diethylamino, pyrrolidino, piperidino, hexamethyleneimino, morpholino or 4-methyl-1-piperazinyl; orR.sub.1 and R.sub.2, together with each other and the nitrogen atom to which they are attached, form a 4- to 7-membered, saturated or mono-unsaturated, unsubstituted or substituted heterocycle which may contain nitrogen, oxygen, sulfur, sulfinyl or sulfonyl as additional ring members, where the substituents are alkyls of 1 to 3 carbon atoms.The compounds are useful as anticonvulsants.
摘要翻译：其中Ar是苯基的式IMAMA的化合物; 单取代或二取代的苯基，其中取代基是一至两个卤素，一至二个碳原子数为1至2个的烷基，或一个氨基，硝基，氰基或三氟甲基; 或吡啶基; R是氢，氯，甲基或甲氧基; R1是氢或甲基; R2是氢，1至6个碳原子的烷基，2至6个碳原子的烯基，2至6个碳原子的炔基，3至8个碳原子的环烷基，甲基 - 3至8个碳原子的环烷基或-A -R4，其中A为2至3个碳原子的亚烷基，R4为羟基，甲基氨基，二甲基氨基，N-甲基 - 乙基氨基，二乙基氨基，吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代或4-甲基-1-哌嗪基; 或R 1和R 2彼此连接并与它们相连的氮原子形成可含有氮，氧，硫，亚磺酰基或磺酰基的4-至7-元饱和或单不饱和的未被取代或取代的杂环作为另外的环成员，其中取代基是1至3个碳原子的烷基。该化合物可用作抗惊厥药。

32. 发明授权

US3987197A 3-(2'-Fluoro-4-biphenylyl)-butyric acid and salts thereof 失效
标题翻译： 3-（2'-氟-4-二苯基） - 丁酸及其盐
公开(公告)号：US3987197A
公开(公告)日：1976-10-19
申请号：US577170
申请日：1975-05-14
申请人： Wolfhard Engel , Helmut Teufel , Ernst Seeger , Josef Nickl , Gunther Engelhardt
发明人： Wolfhard Engel , Helmut Teufel , Ernst Seeger , Josef Nickl , Gunther Engelhardt
IPC分类号： C07C45/46 , C07C57/58 , C07C57/76 , C07C63/333 , C07C245/14 , C07F9/54
CPC分类号： C07C245/14 , C07C255/00 , C07C45/46 , C07C57/58 , C07C57/76 , C07F9/5407
摘要： 3-(2'-Fluoro-4-biphenylyl)-butyric acid and salts thereof formed with inorganic or organic bases; the compound as well as its salts are useful as antiphlogistics and antirheumatics.

33. 发明授权

US3969419A 3-(2-Halo-4-biphenylyl)-1-butanols and derivatives thereof 失效
标题翻译： 3-（2-卤代-4-联苯基）-1-丁醇及其衍生物
公开(公告)号：US3969419A
公开(公告)日：1976-07-13
申请号：US497716
申请日：1974-08-15
申请人： Wolfhard Engel , Helmut Teufel , Ernst Seeger , Gunther Engelhardt
发明人： Wolfhard Engel , Helmut Teufel , Ernst Seeger , Gunther Engelhardt
IPC分类号： C07C69/007 , C07C27/00 , C07C29/147 , C07C33/46 , C07C43/178 , C07C45/71 , C07C51/41 , C07C67/00 , C07C69/12 , C07C69/22 , C07C69/76 , C07C69/773 , C07D213/55 , C07D213/79 , C07C31/14 , C07C69/14 , C07C69/24 , C07C69/78
CPC分类号： C07D213/79 , C07C43/1786 , C07C45/71
摘要： Compounds of the formula formula ##EQU1## wherein R.sub.1 is chlorine or fluorine, and R.sub.2 is hydrogen, alkanoyl of 1 to 10 carbon atoms, benzoyl, nicotinoyl or isonicotinoyl,Or, when R.sub.2 contains a basic nitrogen atom, a non-toxic, pharmacologically acceptable salt thereof formed with an inorganic or organic acid; the compounds as well as the salts are useful as antiphlogistics.
摘要翻译：化学式为CH 3 | CH-CH 2 -CH 2 -OR 2的化合物，其中R 1是氯或氟，R 2是氢，1-10个碳原子的烷酰基，苯甲酰基，烟酰基或异烟酰基，OR，当R 2含有碱性氮原子时，由无机或有机酸形成的无毒的药学上可接受的盐; 化合物以及盐可用作消炎剂。

34. 发明授权

US3969523A Antiphlogistic pharmaceutical compositions containing a 1-(nicotinoyl or isonicotinoyl)-3-biphenylyl-alkanone-(2) 失效
标题翻译：含有1-（烟酰基或异烟酰基）-3-联苯基 - 烷酮（2）的消炎药物组合物
公开(公告)号：US3969523A
公开(公告)日：1976-07-13
申请号：US607667
申请日：1975-08-25
申请人： Josef Nickl , Helmut Teufel , Wolfhard Engel , Ernst Seeger , Gunther Engelhardt
发明人： Josef Nickl , Helmut Teufel , Wolfhard Engel , Ernst Seeger , Gunther Engelhardt
IPC分类号： C07D307/85 , A61K31/455
CPC分类号： C07D307/85 , C07C45/64 , Y10S514/87
摘要： Pharmaceutical compositions containing a compound of the formula ##SPC1##WhereinR.sub.1 is hydrogen, fluoro or chloro,R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, andR.sub.3 is nicotinoyl or isonicotinoyl, or an optically active antipode thereof; and a method of using the same as antiphlogistics.
摘要翻译：含有下式化合物的药物组合物，其中R 1为氢，氟或氯，R 2为氢或1至3个碳原子的烷基，R 3为烟酰基或异烟酰基或其光学活性对映体; 以及将其用作消炎药的方法。

35. 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。

36. 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.

37. 发明授权

US4668674A (+)-6-chloro-5,10-dihy dro-5-[(1-methyl-4-piperidinyl)-acetyl]-11H-dibenzo[b,][1,4]diazepin-11-o ne, the isolation thereof and its use as a pharmaceutical material 失效
标题翻译：（+） - 6-氯-5,10-二氢-5 - [（1-甲基-4-哌啶基） - 乙酰基] -11H-二苯并[b，e] [1,4]二氮杂-11-酮其分离及其作为药物的用途
公开(公告)号：US4668674A
公开(公告)日：1987-05-26
申请号：US898153
申请日：1986-08-19
申请人： G/u/ nter Trummlitz , Wolfhard Engel , Wolfgang Eberlein , Gerhard Mihm , Antonio Giachetti
发明人： G/u/ nter Trummlitz , Wolfhard Engel , Wolfgang Eberlein , Gerhard Mihm , Antonio Giachetti
IPC分类号： C07D243/10 , A61K31/55 , A61P1/00 , C07D401/06 , C07D243/38
CPC分类号： C07D401/06
摘要： There are described (+)-6-chloro-5,10-dihydro-5-[(1-methyl-4-piperidinyl)-acetyl]-11H-dibenzo [b,e][1,4]diazepin-11-one, the isolation thereof from a mixture of enantiomers and its use as a pharmaceutical material.The compound is characterized by a powerful activity against ulcers of the gastro-intestinal tract.
摘要翻译：描述了（+） - 6-氯-5,10-二氢-5 - [（1-甲基-4-哌啶基） - 乙酰基] -11H-二苯并[b，e] [1,4]二氮杂_ 一种，其与对映异构体的混合物的分离及其作为药物的用途。该化合物的特征在于对胃肠道溃疡具有强大的活性。

38. 发明授权

US4424222A Pyridobenzodiazepinones, pharmaceutical compositions and method of use thereof 失效
标题翻译：吡啶并二氮杂酮，药物组合物及其使用方法
公开(公告)号：US4424222A
公开(公告)日：1984-01-03
申请号：US462183
申请日：1983-01-31
申请人： Wolfhard Engel , Gu/ nther Schmidt , Gu/ nther Trummlitz , Wolfgang Eberlein , Rudolf Hammer , Piero D. Soldato
发明人： Wolfhard Engel , Gu/ nther Schmidt , Gu/ nther Trummlitz , Wolfgang Eberlein , Rudolf Hammer , Piero D. Soldato
IPC分类号： A61K31/00 , A61K31/55 , A61P1/00 , A61P1/04 , A61P25/02 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , Y10S514/926 , Y10S514/927
摘要： New pyridobenzodiazepinones of the formula ##STR1## are described wherein X represents oxygen, --NH-- or --NCH.sub.3 -- and R represents 1-methyl-4-piperidinyl or 4-methyl-1-piperazinyl group optionally substituted by a methyl group, or a 3.alpha.- or 3.beta.-tropanyl group, and the nontoxic pharmaceutically acceptable acid addition salts thereof. The specification also describes processes for preparing these compounds, pharmaceutical compositions containing these compounds and new intermediate products used in preparing them. The compounds of formula I have antiulcerative effects and an inhibitory effect on gastric acid secretion, without the side effects such as dryness of the mouth and mydriasis which occur with other substances having an anticholinergic activity.
摘要翻译：描述了式（I）的新的吡啶并苯并二氮杂酮，其中X表示氧，-NH-或-NCH 3 - ，R代表1-甲基-4-哌啶基或4-甲基-1-哌嗪基，任选被甲基取代，或3α-或3β-丙酰基，以及其无毒的药学上可接受的酸加成盐。本说明书还描述了制备这些化合物的方法，含有这些化合物的药物组合物和用于制备它们的新的中间产物。式I化合物具有抗溃疡作用和对胃酸分泌的抑制作用，而没有与具有抗胆碱能活性的其它物质发生的口腔干燥和散瞳等副作用。

39. 发明申请

US20050032783A1 Use of CGRP antagonists in treatment and prevention of hot flushes in prostate cancer patients 审中-公开
标题翻译：使用CGRP拮抗剂治疗和预防前列腺癌患者的热潮红
公开(公告)号：US20050032783A1
公开(公告)日：2005-02-10
申请号：US10881892
申请日：2004-06-30
申请人： Henri Doods , Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Mats Hammar , Anna-Clara Spetz
发明人： Henri Doods , Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Mats Hammar , Anna-Clara Spetz
IPC分类号： A61K31/00 , A61K31/4045 , A61K31/422 , A61K31/517 , A61K31/5513 , A61K45/06
CPC分类号： A61K45/06 , A61K31/00 , A61K31/4045 , A61K31/422 , A61K31/517 , A61K31/5513 , A61K2300/00
摘要： The invention relates to a method of treatment or prevention of hot flushes in men who underwent castration, e.g. due to androgen ablation treatment in prostate cancer therapy, comprising administration of an effective amount of a CGRP antagonist and/or of a CGRP release inhibitor to the patient, and to the use of said active compounds for the manufacture of a pharmaceutical composition intended to be used in this method.
摘要翻译：本发明涉及一种治疗或预防接受阉割的男性热潮红的方法，例如，由于在前列腺癌治疗中的雄激素消除治疗，包括向患者施用有效量的CGRP拮抗剂和/或CGRP释放抑制剂，以及使用所述活性化合物来制备旨在成为用于此方法。

40. 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。

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