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11. 发明授权

US4626325A Process for the preparation of 4-hydroxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide 失效
标题翻译：制备4-羟基-1,2-苯并异噻唑-3（2H） - 酮-1,1-二氧化物的方法
公开(公告)号：US4626325A
公开(公告)日：1986-12-02
申请号：US841392
申请日：1986-03-19
申请人： Gunter Trummlitz , Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm
发明人： Gunter Trummlitz , Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm
IPC分类号： C07D275/06 , C25B3/02 , C25C3/00
CPC分类号： C07D275/06 , C25B3/02
摘要： The specification describes a process for preparing 4-hydroxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide, a sweetener, from 1,2-benzisothiazol-3(2H)-one-1,1-dioxide by anodic oxidation in the presence of trifluoroacetic acid or trifluoromethanesulfonic acid and, optionally, in the presence of salts which increase the conductivity. The oxidation is effected in an anhydrous medium and the 4-trifluoroacetoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide formed as an intermediate when, for example, trifluoroacetic acid is used is decomposed with water to obtain the desired end product.
摘要翻译：该说明书描述了由1,2-苯并异噻唑-3（2H） - 酮-1,1（2H） - 酮-1,1-二氧化物制备4-羟基-1,2-苯并异噻唑-3（2H） - 酮-1,1-二氧化物通过在三氟乙酸或三氟甲磺酸存在下阳极氧化和任选地在增加导电性的盐的存在下进行阳离子氧化。氧化是在无水介质中进行的，当使用例如三氟乙酸时形成的作为中间体的4-三氟乙酰氧基-1,2-苯并异噻唑-3（2H） - 酮-1,1-二氧化物用水分解获得所需的最终产品。

12. 发明授权

US4550107A Condensed diazepinones, their compositions and methods of use as pharmaceuticals 失效
标题翻译：浓缩二氮杂酮，其组合物和用作药物的方法
公开(公告)号：US4550107A
公开(公告)日：1985-10-29
申请号：US711913
申请日：1985-03-14
申请人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gerhard Mihm , Gunther Schmidt , Rudolf Hammer , Antonio Giachetti
发明人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gerhard Mihm , Gunther Schmidt , Rudolf Hammer , Antonio Giachetti
IPC分类号： A61K31/00 , A61K31/55 , A61P9/06 , A61P25/02 , C07D207/09 , C07D207/16 , C07D207/34 , C07D211/26 , C07D213/38 , C07D223/04 , C07D223/08 , C07D223/12 , C07D243/00 , C07D243/14 , C07D243/38 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D495/14 , C07D521/00
CPC分类号： C07D401/06 , C07C255/00 , C07D207/16 , C07D207/34 , C07D211/26 , C07D223/04 , C07D223/08 , C07D403/06 , C07D413/06 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Disclosed are novel condensed diazepinones of formula I ##STR1## wherein B is a fused ring selected from ##STR2## X is --CH-- or, when B is ortho-phenylene, X can also be nitrogen; A.sub.1 is C.sub.1 -C.sub.2 alkylene; A.sub.2 is C.sub.1 -C.sub.2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R.sub.1 is C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C.sub.3 -C.sub.7 cycloalkyl, optionally hydroxy substituted, or C.sub.3 -C.sub.7 cycloalkylmethyl; or R.sub.1 and R.sub.2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH.sub.3 ; R.sub.3 is hydrogen, chlorine, or methyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 is hydrogen, chlorine or C.sub.1 -C.sub.4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR.sub.1 R.sub.2 --N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.
摘要翻译：公开了式I的新型稠合二氮杂酮，其中B是选自下列的稠环，X是-CH-，或当B是邻 - 亚苯基时，X也可以是氮; A1是C1-C2亚烷基; 当A2位于3-或4-位时相对于饱和杂环氮或单键或亚甲基为2-位，则为C1-C2; R1是C1-C3烷基; R2是任选在其第二至第七碳中的至少一个上被羟基取代的C 1 -C 7烷基，或任选被羟基取代的C 3 -C 7环烷基或C 3 -C 7环烷基甲基; 或者R 1和R 2可以与它们之间的氮一起是可以任选地包括氧或N-CH 3的4-至7-元饱和单环杂环; R3是氢，氯或甲基; R4是氢或C1-C4烷基，R5是氢，氯或C1-C4烷基; Z为单键，氧，亚甲基或1,2-亚乙基; 和NR 1 R 2 -N氧化物和无毒的药学上可接受的加成盐。还公开了吡咯并苯并二氮杂酮中间体，含有缩合二氮嗪酮的药物组合物及其用于治疗心血管疾病，特别是心动过缓和缓慢性心律失常的方法。

13. 发明授权

US5001122A Use of diazepinones for treating disorders of the microcirculation 失效
标题翻译：二氮嗪酮用于治疗微循环障碍的用途
公开(公告)号：US5001122A
公开(公告)日：1991-03-19
申请号：US353262
申请日：1989-05-17
申请人： Wolfgang Eberlein , Volker Trach , Wolfhard Engel , Gerhard Mihm , Norbert Mayer , Henri Doods , Richard Reichl
发明人： Wolfgang Eberlein , Volker Trach , Wolfhard Engel , Gerhard Mihm , Norbert Mayer , Henri Doods , Richard Reichl
IPC分类号： C07D243/38 , A61K31/00 , A61K31/55 , A61P9/00 , A61P9/08 , C07D471/04 , C07D487/04 , C07D495/04
CPC分类号： A61K31/55 , Y10S514/921
摘要： A method for treating shock in a patient, which comprises administering to the patient a therapeutically effective amount of a diazepinone of the general formula: ##STR1## wherein A represents a 5,11-dihydro-6H-pyrido[2,3-b] [1,4] benzodiazepin-6-one group bound in the 11-position; a 5,10-dihydro-11H-dibenzo [b,e] [1,4] diazepin-11-one group bound in the 5-position; a 5,11-dihydro-10H-pyrido [3-2b] [1-4] benzodiazepin-10-one group bound in the 5-position; a 4,9-dihydro-10H-thieno [3,4-b] [1,5] benzodiazpin-10-one group bound in the 4-position, unsubstituted or substituted at the 1- or 3-position or both in the 1- and 3-position by an alkyl group having from 1 to 4 carbon atoms, or in the 3-positionby chlorine, fluorine or bromine; a 6-11-dihydro-5H-pyrido [2,3-b] [1,5] benzodiazepin-5-one group bound in the 11-position; or a 1-methyl-1,4,9,10-tetrahydropyrrolo-[3,2-b] [1,5] benzodiazepin-10-one group bound in the 4-position, unsubstituted or substituted at the 3-position by methyl or methyl or chlorine;R.sub.1 represents a hydrogen atom or an alkyl group having from 1 to 3 carbon atoms;R.sub.2 represents an alkyl group having from 1 to 3 carbon atoms; andn and m each represent an integer from 1 to 3.
摘要翻译：一种治疗患者休克的方法，其包括向患者施用治疗有效量的通式如下的二氮杂酮：其中A代表5,11-二氢-6H-吡啶并[2,3-b] 结合在11位的[1,4]苯并二氮杂- 5位结合的5,10-二氢-11H-二苯并[b，e] [1,4]二氮杂-11-酮基; 5位结合的5,11-二氢-10H-吡啶并[3-2b] [1-4]苯并二氮杂-10-酮基; 在4-位上结合的未取代或取代的4,9-二氢-10H-噻吩并[3,4-b] [1,5]苯并二氮杂基-10-酮基或在通过具有1至4个碳原子的烷基或3-，3-位上的氯，氟或溴取代1-和3-位; 在11位结合的6-11-二氢-5H-吡啶并[2,3-b] [1,5]苯并二氮杂-5-基; 或在4-位上结合的1-甲基-1,4,9,10-四氢吡咯并[3,2-b] [1,5]苯并二氮杂-10-酮基，其未被取代或在3位被甲基或甲基或氯; R1表示氢原子或具有1至3个碳原子的烷基; R2表示具有1至3个碳原子的烷基; n和m各自表示1〜3的整数。

14. 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。

15. 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.

17. 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。

18. 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。

19. 发明授权

US4404230A 4-Hydroxy-1,2-Benzisothiazol-3(2H)-one-1,1-dioxides and salts thereof 失效
标题翻译： 4-羟基-1,2-苯并异噻唑-3（2H） - 酮-1,1-二氧化物及其盐
公开(公告)号：US4404230A
公开(公告)日：1983-09-13
申请号：US254546
申请日：1981-04-15
申请人： Gunter Trummlitz , Wolfgang Eberlein , Wolfhard Engel , Gunther Schmidt
发明人： Gunter Trummlitz , Wolfgang Eberlein , Wolfhard Engel , Gunther Schmidt
IPC分类号： A23L27/20 , A23L27/30 , C07C205/58 , C07D275/04 , C07D275/06 , A23L1/236
CPC分类号： C07D275/06 , A23L27/2056 , A23L27/30 , C07C205/58 , C07C255/00 , C07C309/00
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxyl, and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as sweetening agents.
摘要翻译：其中R1是氢或羟基的式“IMAGE”的化合物，以及与无机或有机碱形成的无毒的药学上可接受的盐。化合物及其盐可用作甜味剂。

20. 发明授权

US4328235A Suppressing pain with benzothiazol-2(3H)-ones 失效
标题翻译：用苯并噻唑-2（3H）酮抑制疼痛
公开(公告)号：US4328235A
公开(公告)日：1982-05-04
申请号：US163965
申请日：1980-06-30
申请人： Gunter Trummlitz , Wolfhard Engel , Gunther Schmidt , Wolfgang Eberlein , Ernst Seeger , Gunther Engelhardt , Rainer Zimmermann
发明人： Gunter Trummlitz , Wolfhard Engel , Gunther Schmidt , Wolfgang Eberlein , Ernst Seeger , Gunther Engelhardt , Rainer Zimmermann
IPC分类号： A61K31/425 , A61K31/428 , A61P25/04 , A61P29/00 , C07D277/68
CPC分类号： C07D277/68 , A61K31/425
摘要： There are described pharmaceutical compositions containing as active substances benzothiazol-2(3H)-ones of the general formula ##STR1## wherein R represents a hydrogen atom or a methyl, methoxy, or ethoxy group. The pharmaceutical compositions serve as analgesics and antipyretics and possess little or no methemoglobin-forming activity.
摘要翻译：描述了含有作为活性物质的通式为“IMAGE”的苯并噻唑-2（3H） - 酮的药物组合物，其中R表示氢原子或甲基，甲氧基或乙氧基。药物组合物用作止痛剂和解热药，并且几乎没有或没有高铁血红蛋白形成活性。

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