公开(公告)号：US20050161965A1

公开(公告)日：2005-07-28

申请号：US10946138

申请日：2004-09-21

申请人： Wolfgang Eberlein

发明人： Wolfgang Eberlein

IPC分类号： B21D39/00 ,  B21J15/00 ,  B23K11/00 ,  B23K11/02 ,  B23K11/06 ,  B23K11/11 ,  B23P11/00 ,  B62D27/02 ,  F16B5/04 ,  F16B19/08

CPC分类号： B23K11/11 ,  B21J15/025 ,  B23K11/002 ,  B23K11/0066 ,  B23K11/02 ,  B23K11/06 ,  B23K2101/006 ,  B62D27/02 ,  F16B5/04 ,  F16B19/086 ,  Y10T29/49943 ,  Y10T29/49954 ,  Y10T29/49968 ,  Y10T29/5377

摘要： Method for connecting two or more metal sheets or profile parts, especially of an automobile body segment as well as said automobile body segment. A method is described for joining two or more metal sheets and/or profile parts of which typically one is a high strength steel with the following steps. a) mechanically joining in a force-locking or frictional manner the metal sheets or profile parts at one or more connecting sites and subsequently b) thermally joining the connecting sites by means of pressure welding. With the method according to the invention in particular in the motor vehicle sector automobile body segments can be produced which display qualitatively very high quality point weld joints.

摘要翻译： 用于连接两个或更多个金属板或轮廓部分，特别是汽车车身段以及所述汽车车身段的方法。 描述了用于连接两个或更多个金属片和/或轮廓部分的方法，其中通常一个是高强度钢，具有以下步骤。 a）在一个或多个连接部位以金属片或轮廓部件的力锁定或摩擦方式机械接合，随后b）通过压力焊接热连接连接部位。 利用根据本发明的方法，特别是在机动车辆部件中，可以生产出显示质量上非常高质量的点焊接头的汽车车身部分。

公开(公告)号：US06855710B2

公开(公告)日：2005-02-15

申请号：US10666643

申请日：2003-09-19

申请人： Rainer Walter ,  Wolfgang Grell ,  Armin Heckel ,  Frank Himmelsbach ,  Wolfgang Eberlein ,  Gerald Roth ,  Jacobus C.A. van Meel ,  Norbert Redemann ,  Walter Spevak ,  Ulrike Tontsch-Grunt ,  Thomas von Rueden

发明人： Rainer Walter ,  Wolfgang Grell ,  Armin Heckel ,  Frank Himmelsbach ,  Wolfgang Eberlein ,  Gerald Roth ,  Jacobus C.A. van Meel ,  Norbert Redemann ,  Walter Spevak ,  Ulrike Tontsch-Grunt ,  Thomas von Rueden

IPC分类号： C07D401/12 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D209/34 ,  C07D209/36 ,  C07D209/48 ,  C07D401/14 ,  C07D403/12

CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D403/12

摘要： The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.

摘要翻译： 本发明涉及新一代的取代的二氢吲哚酮，其通式为R，R 1至R 5如权利要求1所定义，其异构体及其盐具有有价值的性质。上述通式I的化合物，其中R 1表示氢原子， 3-烷基或前药基团具有有价值的药理学性质，特别是对各种激酶，对病毒细胞周期蛋白和受体酪氨酸激酶的抑制作用，以及上述通式I的其它化合物，其中R1不表示氢原子， C1-3烷基或前药基团是用于制备上述化合物的有价值的中间产物。

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。

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.

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。

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。

公开(公告)号：US4379788A

公开(公告)日：1983-04-12

申请号：US327348

申请日：1981-12-04

申请人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Christian Lillie

发明人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Christian Lillie

IPC分类号： C07D239/88 ,  A61K31/513 ,  A61P9/00 ,  C07D213/82 ,  C07D239/91 ,  C07D265/22 ,  C07D471/04 ,  C07D498/04 ,  A61K31/505

CPC分类号： C07D213/82 ,  C07D239/91 ,  C07D265/22 ,  C07D471/04

摘要： Compounds of the formula ##STR1## wherein A and B, together with each other and the respective carbon atoms to which they are attached, form a phenyl or pyridine ring;R.sub.1 is hydrogen, halogen, amino, nitro, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;R.sub.2 is hydrogen or alkoxy of 1 to 3 carbon atoms;D is alkylene of 3 to 4 carbon atoms or hydroxy(alkylene of 3 to 4 carbon atoms);R.sub.3 and R.sub.5, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is hydrogen or alkoxy of 1 to 3 carbon atoms; andR.sub.6 is straight or branched alkyl of 1 to 6 carbon atoms or --E--R.sub.7 ;where E is straight alkylene of 2 to 4 carbon atoms or hydroxy-substituted straight alkylene of 2 to 4 carbon atoms, andR.sub.7 is ##STR2## where R.sub.8 and R.sub.9 are each hydrogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof formed with inorganic or organic acids; the compounds as well as their salts are useful as hypotensives, antiarrhythmics and .beta.-receptor-blockers.

摘要翻译： 其中A和B与它们相连的相互连接的碳原子一起形成苯基或吡啶环; R 1是氢，卤素，氨基，硝基，1至3个碳原子的烷基或1至3个碳原子的烷氧基; R2是氢或1〜3个碳原子的烷氧基; D是3至4个碳原子的亚烷基或羟基（3至4个碳原子的亚烷基）; R 3和R 5可以相同或不同，分别为氢或1-3个碳原子的烷基; R4是氢或1〜3个碳原子的烷氧基; R6是1-6个碳原子的直链或支链烷基或-E-R7; 其中E是2至4个碳原子的直链亚烷基或2至4个碳原子的羟基取代的直链亚烷基，并且R 7是R 8和R 9各自为氢，1至3个碳原子的烷基或1至 3个碳原子; 和与无机或有机酸形成的无毒的，药学上可接受的酸加成盐; 化合物及其盐可用作低血糖，抗心律失常药和β-受体阻滞剂。

公开(公告)号：US4361563A

公开(公告)日：1982-11-30

申请号：US259537

申请日：1981-05-01

申请人： Volkhard Austel ,  Joachim Heider ,  Wolfgang Eberlein ,  Willi Diederen ,  Walter Haarmann

发明人： Volkhard Austel ,  Joachim Heider ,  Wolfgang Eberlein ,  Willi Diederen ,  Walter Haarmann

IPC分类号： A61K31/50 ,  C07D235/18 ,  C07D237/04 ,  C07D403/04

CPC分类号： C07D237/04 ,  A61K31/50 ,  C07D235/18 ,  Y10S514/822

摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; trifluoromethyl; alkyl of 1 to 11 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; hydroxyl; alkoxy of 1 to 6 carbon atoms; mercapto; (alkyl of 1 to 6 carbon atoms)-mercapto; phenyl-(alkyl of 1 to 3 carbon atoms); phenyl; or mono-, di- or tri-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, alkyl of 1 to 4 carbon atoms, (alkyl of 1 to 6 carbon atoms)-sulfinyl, hydroxyl, alkoxy of 1 to 6 carbon atoms, mercapto or (alkyl of 1 to 6 carbon atoms)-mercapto;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms or phenyl-(alkyl of 1 to 3 carbon atoms); andR.sub.3 is alkyl of 1 to 6 carbon atoms; optically active antipodes thereof; and non-toxic, pharmaceutically acceptable acid addition salts of said compounds or of said optically active antiposed. The compounds are useful as cardiotonics and antithrombotics.

摘要翻译： 其中R 1是氢的式IMAMA的化合物; 三氟甲基 1至11个碳原子的烷基; 3至7个碳原子的环烷基; 羟; 1至6个碳原子的烷氧基; 巯基 （1-6个碳原子的烷基） - 巯基; 苯基 - （1至3个碳原子的烷基）; 苯基; 或单取代，二取代或三取代的苯基，其中可以相同或不同的取代基各自为卤素，具有1至4个碳原子的烷基，（1至6个碳原子的烷基） - 亚磺酰基 ，羟基，1至6个碳原子的烷氧基，巯基或（1至6个碳原子的烷基） - 巯基; R2是氢，1至6个碳原子的烷基，3至6个碳原子的环烷基或苯基 - （1至3个碳原子的烷基）; 且R 3为1至6个碳原子的烷基; 光学活性对映体; 和所述化合物或所述光学活性药物的无毒的药学上可接受的酸加成盐。 这些化合物可用作强心剂和抗血栓药物。

公开(公告)号：US4154837A

公开(公告)日：1979-05-15

申请号：US867308

申请日：1978-01-06

申请人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Jurgen Dammgen ,  Walter Kobinger ,  Christian Lillie

发明人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Jurgen Dammgen ,  Walter Kobinger ,  Christian Lillie

IPC分类号： A61K31/444 ,  A61K31/47 ,  A61K31/472 ,  A61P9/00 ,  A61P9/12 ,  C07D217/24 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D217/24

摘要： Compounds of the formula ##STR1## wherein A is benzo, mono-, di- or tri-substituted benzo, the substituents being selected from the group consisting of lower alkoxy, amino and nitro, or pyrido;R.sub.1 is hydrogen or lower alkyl;R.sub.2 is alkyl of 1 to 6 carbon atoms or --X--R.sub.6, where X is straight alkylene of 1 to 4 carbon atoms or hydroxy-substituted straight alkylene of 1 to 4 carbon atoms; andR.sub.6 is amino; carbalkoxy of 2 to 6 carbon atoms; phenyl; mono-, di- or tri-substituted phenyl, the substituents being selected from the group consisting of lower alkyl and lower alkoxy; phenoxy; or mono-, di- or tri-substituted phenoxy, the substituents being selected from the group consisting of lower alkyl and lower alkoxy;R.sub.3 is hydrogen or hydroxyl;R.sub.4 is hydrogen, lower alkyl or lower alkoxy;R.sub.5 is hydrogen or lower alkyl; andN is 0, 1 or 2;And non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as antiarrhythmics, .beta.-adrenergic-receptor blockers and anti-anginous agents.

摘要翻译： 其中A是苯并，一或二取代或三取代的苯并，其取代基选自低级烷氧基，氨基和硝基，或吡啶并。 R1是氢或低级烷基; R2是1至6个碳原子的烷基或-X-R6，其中X是1至4个碳原子的直链亚烷基或1至4个碳原子的羟基取代的直链亚烷基; R6为氨基; 2至6个碳原子的烷氧基; 苯基; 单取代，二取代或三取代的苯基，所述取代基选自低级烷基和低级烷氧基; 苯氧基 或单 - ，二 - 或三 - 取代的苯氧基，所述取代基选自低级烷基和低级烷氧基; R3是氢或羟基; R4是氢，低级烷基或低级烷氧基; R5是氢或低级烷基; 和N IS 0，1或2; 和非毒性，药理学上可接受的酸添加量。 化合物和盐可用作抗心律失常药，β-肾上腺素能受体阻断剂和抗麻痹剂。

公开(公告)号：US3948898A

公开(公告)日：1976-04-06

申请号：US503072

申请日：1974-09-04

申请人： Eberhard Kutter ,  Volkard Austel ,  Wolfgang Eberlein ,  Joachim Heider

发明人： Eberhard Kutter ,  Volkard Austel ,  Wolfgang Eberlein ,  Joachim Heider

IPC分类号： C07D217/04 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61P9/06 ,  A61P9/12 ,  A61P25/20 ,  C07D217/24 ,  C07D401/06 ,  C07D401/12 ,  C07D217/16

CPC分类号： C07D217/24 ,  Y10S514/821

摘要： Compounds of the formula ##SPC1##Wherein R.sub.1 is hydrogen, halogen, methoxy or methylthioR.sub.2 is hydrogen or methoxy,n is 2 or 3, andA is ##SPC2##Or ##SPC3##Where R.sub.3 is hydrogen or methyl,R.sub.4 is pyridyl, methy-pyridyl, phenyl, chlorophenyl, trifluoromethyl-phenyl, tolyl, xylyl, ethyl-phenyl, diethyl-phenyl, methoxy-phenyl or dimethoxy-phenyl, andR.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen or methoxy,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as hypotensives, sedatives, antiarrhythmics and bradycardiacs.

摘要翻译： 式WHEREIN R 1是氢，卤素，甲氧基或甲硫基R 2的化合物是氢或甲氧基，N IS 2 OR 3，A是或R 3是氢或甲基，R 4是吡啶基，甲基 - 吡啶基，苯基，氯苯基，三氟甲基 苯基，甲苯基，二甲苯基，乙基 - 苯基，二乙基 - 苯基，甲氧基 - 苯基或二甲氧基 - 苯基，以及可以相同或不同的R5和R6各自为氢或甲氧基。非 - 药理学上可接受的酸添加剂; 该化合物作为盐类有效地用作高血压药物，消炎药，抗精神病药和溴氰菊酯。