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1. 发明授权

US5002943A 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：US5002943A
公开(公告)日：1991-03-26
申请号：US366828
申请日：1989-06-15
申请人： Gerhard Mihm , Wolfgang Eberlein , Wolfhard Engel , Gunter Trummlitz , Norbert Mayer , Adrian de Jonge , Henri Doods
发明人： Gerhard Mihm , Wolfgang Eberlein , Wolfhard Engel , Gunter Trummlitz , Norbert Mayer , Adrian de Jonge , Henri Doods
IPC分类号： A61K31/00 , A61K31/55 , A61K31/551 , A61P1/00 , A61P9/04 , A61P9/06 , A61P11/00 , A61P13/02 , A61P15/00 , C07D243/14 , C07D403/12 , C07D471/04 , C07D471/14 , C07D495/04
CPC分类号： C07D403/12 , C07D471/04 , C07D471/14 , C07D495/04
摘要： Novel condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, A.sup.1, A.sup.2 and R.sup.1 -R.sup.10 are as defined herein. The condensed diazepinones are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia and they have spasmolytic effects on peripheral organs, particularly the colon, bladder and bronchi.
摘要翻译：新的通式I的缩合二氮杂酮其中B表示二价基团之一，其中X，A1，A2和R1-R10如本文所定义。浓缩的二氮嗪酮适合作为迷走神经起搏器用于治疗心动过缓和缓慢性心律失常，并且对周围器官特别是结肠，膀胱和支气管具有解痉作用。

2. 发明授权

US5175158A Condensed diazepinones, processes for preparing them and pharmaceutical compositions containing these compounds 失效
标题翻译：浓缩的双酚A，其制备方法及含有这些化合物的药物组合物
公开(公告)号：US5175158A
公开(公告)日：1992-12-29
申请号：US261950
申请日：1988-10-24
申请人： Wolfgang Eberlein , Wolfhard Engel , Gunter Trummlitz , Gerhard Mihm , Norbert Mayer , Henri Doods
发明人： Wolfgang Eberlein , Wolfhard Engel , Gunter Trummlitz , Gerhard Mihm , Norbert Mayer , Henri Doods
IPC分类号： A61K31/00 , A61P9/06 , A61P25/02 , C07D401/06 , C07D401/14 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04 , C07D495/14
CPC分类号： C07D471/04 , C07D487/04 , C07D495/04
摘要： New diazepinones of formula I ##STR1## wherein the substituents are defined herein, which compounds exhibit favorable effects on heart rate and in view of the absence of inhibitory effects on gastric acid secretion and salivation and the absence of mydriatic effects, are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia in human and veterinary medicine.
摘要翻译：式I的新二氮杂酮（I）其中取代基在本文中定义，这些化合物对心率表现出有利的影响，并且鉴于对胃酸分泌和唾液分泌和不存在散瞳效应的抑制作用不存在是合适的作为迷走神经心脏起搏器，用于治疗人类和兽医学中的心动过缓和慢性心律失常。

3. 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。

4. 发明授权

US4971966A Substituted pyrido(2,3-B) (1,4) benzodiazepin-6-ones, and medicaments containing these compounds 失效
标题翻译：取代的吡啶并（2,3-B）（1,4）苯并二氮杂-6，以及含有这些化合物的药物
公开(公告)号：US4971966A
公开(公告)日：1990-11-20
申请号：US80716
申请日：1987-07-31
申请人： Wolfhard Engel , Wolfgang Eberlein , Gunter Trummlitz , Gerhard Mihm , Norbert Mayer , Adriaan de Jonge
发明人： Wolfhard Engel , Wolfgang Eberlein , Gunter Trummlitz , Gerhard Mihm , Norbert Mayer , Adriaan de Jonge
IPC分类号： A61K31/55 , A61P9/06 , C07D471/04
CPC分类号： C07D471/04
摘要： New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.
摘要翻译：描述了适用于治疗人类和兽医学中的心动过缓和缓慢性心律失常的迷走神经起搏器的新取代的吡啶并[2,3-b] [1,4]苯并二氮杂--6-酮。

5. 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。

6. 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。

7. 发明授权

US4873236A 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：US4873236A
公开(公告)日：1989-10-10
申请号：US136212
申请日：1987-12-18
申请人： Wolfhard Engel , Wolfgang Eberlein , Gerhard Mihm , Gunter Trummlitz , Norbert Mayer , Adriaan De Jonge
发明人： Wolfhard Engel , Wolfgang Eberlein , Gerhard Mihm , Gunter Trummlitz , Norbert Mayer , Adriaan De Jonge
IPC分类号： C07D519/00 , A61K31/55 , A61P9/06 , A61P25/02 , C07D223/20 , C07D243/38 , C07D401/12 , C07D403/12 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D495/04
CPC分类号： C07D401/12 , C07D243/38 , C07D403/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： There are described new condensed diazepinones of general formula ##STR1## wherein .circle.B represents one of the divalent groups ##STR2## and D represents the groups ##STR3## and X.sup.1, X.sup.2 represents a .dbd.CH-- group or, if .circle.B assumes the meaning of the divalent group S, U or W, they may also represent an N atom, A.sup.1 and A.sup.2 in general represent lower alkylene groups, Z represents a C--C bond or the groups, --O--, --S--, --CH.sub.2 --, or --(CH.sub.2).sub.2 --; R represents hydrogen or methyl, R.sup.1 and R.sup.2 generally represent alkyl groups which, together with the nitrogen atom between them, may also form a saturated monocylic, heterocyclic group, R.sub.3 represents alkyl, chlorine or hydrogen, R.sub.4 represents hydrogen or methyl, R.sup.5 and R.sup.6 represent hydrogen, halogen or alkyl, R.sub.7 represents hydrogen, chlorine or methyl, R.sup.8 represents hydrogen or lower alkyl, R.sup.9 represents hydrogen, halogen, lower alkyl and R.sup.10 represents hydrogen or methyl and R.sup.12 represents branched or unbranched alkyl. The compounds of general formula I and the acid addition salts thereof may be resolved into their isomers. The compounds of formula I and their salts may be used as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia.
摘要翻译：描述了通式为“IMAGE”（I）的新的缩合二氮杂酮，其中＆cir＆B表示二价基团之一 + TR ，D表示基团 + TR 和X1 ，X2表示a = CH-基团，或者如果＆Cir＆B表示二价基团S，U或W的含义，它们也可以表示N原子，A1和A2一般表示低级亚烷基，Z表示CC键或基团，-O - ， - S - ， - CH 2 - 或 - （CH 2）2 - ; R表示氢或甲基，R 1和R 2通常表示烷基，它们与氮原子一起也可以形成饱和单环，杂环基，R 3表示烷基，氯或氢，R 4表示氢或甲基，R 5和R 6 代表氢，卤素或烷基，R7代表氢，氯或甲基，R8代表氢或低级烷基，R9代表氢，卤素，低级烷基，R10代表氢或甲基，R12代表支链或非支链烷基。通式I的化合物及其酸加成盐可以分解成它们的异构体。式I化合物及其盐可用作迷走神经起搏器用于治疗心动过缓和缓慢性心律失常。

8. 发明授权

US4724236A 5,11-dihydro-6H-pyrido(2,3-B)(1,4)benzodiazepin-6-ones substituted in the 11-position, processes for preparing them and pharmaceutical compositions containing these compounds 失效
标题翻译：在11位被取代的5,11-二氢-6H-吡啶并（2,3-B）（1,4）苯并二氮杂-6-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：US4724236A
公开(公告)日：1988-02-09
申请号：US944146
申请日：1986-12-19
申请人： Wolfgang Eberlein , Gunter Trummlitz , Wolfhard Engel , Gerhard Mihm , Rudolf Hammer , Norbert Mayer , Antonio Giachetti , Adriaan de Jonge
发明人： Wolfgang Eberlein , Gunter Trummlitz , Wolfhard Engel , Gerhard Mihm , Rudolf Hammer , Norbert Mayer , Antonio Giachetti , Adriaan de Jonge
IPC分类号： A61K31/55 , C07D471/04 , C07D403/14
CPC分类号： C07D471/04
摘要： Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom andA represents the groups --NR.sup.1 R.sup.2,wherein R.sup.1 and R.sup.2 represent alkyl, cycloalkyl or phenylalkyl groups, n represents the number 0, 1 or 2, R.sup.3 represents a hydrogen atom, a hydroxy or alkyl group or a group --(CH.sub.2).sub.n --N--R.sup.5 R.sup.6 (R.sup.5 and R.sup.6 being lower alkyl groups) and R.sup.4 is an alkyl or phenylalkyl group; two processes for preparing these compounds and the salts thereof are also described.The compounds have favourable effects on heart rate and can be used as vagal pacemakers for treating bradycardia and bradyarrhythmia in human and veterinary medicine. Some of these compounds also have very good antithrombotic effects.
摘要翻译：描述通式I的化合物，其中X表示基团= CHR，= NR或氧原子，A表示基团-NR1R2，其中R1和R2表示烷基，环烷基或苯基烷基，n表示数字0,1或2，R3表示氢原子，羟基或烷基或基团 - （CH2）nN-R5R6（R5和R6是低级烷基），R4表示烷基或苯基烷基; 还描述了制备这些化合物及其盐的两种方法。这些化合物对心率有好的影响，可用作迷走神经心脏起搏器，用于治疗人和兽医学中的心动过缓和缓慢性心律失常。这些化合物中的一些也具有非常好的抗血栓形成作用。

9. 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。

10. 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。

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