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1. 发明授权

US4038407A Benzisothiazoline-1,1-dioxide derivatives, compositions and methods 失效
标题翻译：苯并噻唑啉-1,1-二氧化物衍生物，组合物和方法
公开(公告)号：US4038407A
公开(公告)日：1977-07-26
申请号：US660841
申请日：1976-02-24
申请人： Wolfgang Eberlein , Eberhard Kutter , Joachim Heider , Volkhard Austel , Rudolf Kadatz , Willi Diederen , Walter Kobinger , Christian Lillie , Jurgen Dammgen
发明人： Wolfgang Eberlein , Eberhard Kutter , Joachim Heider , Volkhard Austel , Rudolf Kadatz , Willi Diederen , Walter Kobinger , Christian Lillie , Jurgen Dammgen
IPC分类号： A61K31/435 , C07D209/46 , C07D209/48 , C07D275/04 , C07D275/06 , C07D491/04 , A61K31/425 , C07D91/12
CPC分类号： C07D209/48 , C07C309/00 , C07D209/46 , C07D275/06
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or phenyl,R.sub.2 is hydrogen, chlorine or methoxy,R.sub.3 is hydrogen or methoxy,R.sub.2 and R.sub.3, together with each other, are methylenedioxy or ethylenedioxy,R.sub.4 and R.sub.5 are each hydrogen or lower alkyl,R.sub.6 is hydrogen or lower alkoxy,R.sub.7 is lower alkoxy,R.sub.6 and R.sub.7, together with each other, are methylenedioxy or ethylenedioxy,X is carbonyl or sulfonyl, andn is 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful for slowing the heart rate.

2. 发明授权

US4031219A Bis-homophthalimides and salts thereof 失效
标题翻译：双 - 高邻苯二甲酰亚胺及其盐
公开(公告)号：US4031219A
公开(公告)日：1977-06-21
申请号：US704844
申请日：1976-07-13
申请人： Eberhard Kutter , Volkhard Austel , Wolfgang Eberlein , Joachim Heider , Walter Kobinger , Christian Lillie , Rudolf Kadatz
发明人： Eberhard Kutter , Volkhard Austel , Wolfgang Eberlein , Joachim Heider , Walter Kobinger , Christian Lillie , Rudolf Kadatz
IPC分类号： A61K31/47 , A61K31/472 , A61P9/06 , C07D217/24 , C07D221/22
CPC分类号： C07D217/24 , Y10S514/821
摘要： Compounds of the formula ##STR1## wherein A and B, which may be identical to or different from each other, are each straight alkylene of 2 to 4 carbon atoms which may have a methyl or phenyl substituent attached thereto,R.sub.1, r.sub.2, r.sub.3 and R.sub.4, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, hydroxyl, amino, nitro, acetylamino, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or (alkyl of 1 to 3 carbon atoms)thio,R.sub.5, r.sub.6, r.sub.7 and R.sub.8, which may be identical to or different from each other, are each hydrogen, alkyl of 1 to 4 carbon atoms, phenyl-(alkyl of 1 to 4 carbon atoms) or methoxyphenyl-(alkyl of 1 to 4 carbon atoms), orR.sub.5 and R.sub.6, together with each other, are straight alkylene of 2 to 5 carbon atoms, orR.sub.7 and R.sub.8, together with each other, are straight alkylene of 2 to 5 carbon atoms, andR.sub.9 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl-(alkyl of 1 to 6 carbon atoms),And non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as the salts are useful as antiarrhythmics.
摘要翻译：其中A和B可以彼此相同或不同的化合物是可以具有连接到其上的甲基或苯基取代基的2至4个碳原子的直链亚烷基，R 1，R 2，R 3和 R 4可以相同或不同，分别为氢，氟，氯，溴，羟基，氨基，硝基，乙酰氨基，1〜3个碳原子的烷基，1〜3个碳原子的烷氧基或（ 1至3个碳原子）硫代，R 5，R 6，R 7和R 8可彼此相同或不同，分别为氢，1至4个碳原子的烷基，苯基 - （1至4个碳原子的烷基）或甲氧基苯基 - （1至4个碳原子的烷基）或R 5和R 6彼此一起是2至5个碳原子的直链亚烷基，或者R 7和R 8彼此一起是2至5个直链亚烷基碳原子，并且R 9为氢，1至6个碳原子的烷基或苯基 - （1至6个碳原子的烷基），和非毒性，药学上可接受的酸附加费用化合物作为反应物可用作生物反应器。

3. 发明授权

US4087541A 2-(Aralkylaminoalkyl)phthalimidines 失效
标题翻译： 2-（芳烷基氨基烷基）苯二甲酰亚胺
公开(公告)号：US4087541A
公开(公告)日：1978-05-02
申请号：US793734
申请日：1977-05-04
申请人： Wolfgang Eberlein , Eberhard Kutter , Joachim Heider , Volkhard Austel , Rudolf Kadatz , Willi Diederen , Walter Kobinger , Christian Lillie , Jurgen Dammgen
发明人： Wolfgang Eberlein , Eberhard Kutter , Joachim Heider , Volkhard Austel , Rudolf Kadatz , Willi Diederen , Walter Kobinger , Christian Lillie , Jurgen Dammgen
IPC分类号： C07D209/46 , C07D209/48 , C07D275/06 , C07D491/056 , A61K31/40 , C07D405/12 , C07D491/04
CPC分类号： C07D209/48 , C07C309/00 , C07D209/46 , C07D275/06
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or phenyl,R.sub.2 is hydrogen, chlorine or methoxy,R.sub.3 is hydrogen or methoxy,R.sub.2 and R.sub.3, together with each other, are methylenedioxy or ethylenedioxy,R.sub.4 and R.sub.5 are each hydrogen or lower alkyl,R.sub.6 is hydrogen or lower alkoxy.R.sub.7 is lower alkoxy,R.sub.6 and R.sub.7, together with each other, are methylenedioxy or ethylenedioxy, andn is 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful for slowing the heart rate.
摘要翻译：其中R 1是氢，低级烷基或苯基，R 2是氢，氯或甲氧基，R 3是氢或甲氧基，R 2和R 3彼此是亚甲二氧基或亚乙二氧基，R 4和R 5各自是氢或低级烷基，R6是氢或低级烷氧基。

4. 发明授权

US4176184A Imidazoisoquinoline-diones and salts thereof 失效
标题翻译：咪唑并异喹啉二酮及其盐
公开(公告)号：US4176184A
公开(公告)日：1979-11-27
申请号：US925461
申请日：1978-07-17
申请人： Volkhard Austel , Eberhard Kutter , Joachim Heider , Wolfgang Eberlein , Walter Kobinger , Christian Lillie , Willi Diederen , Walter Haarmann
发明人： Volkhard Austel , Eberhard Kutter , Joachim Heider , Wolfgang Eberlein , Walter Kobinger , Christian Lillie , Willi Diederen , Walter Haarmann
IPC分类号： A61K31/47 , A61K31/4745 , A61K31/495 , A61K31/535 , A61P7/02 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/20 , C07D217/24 , C07D471/04
CPC分类号： C07D471/04 , C07D217/24 , Y10S514/821
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl; phenyl-lower alkyl; cycloalkyl of 3 to 6 carbon atoms; phenyl; mono- or di-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, hydroxyl, methoxy, methylmercapto, methylsulfinyl, methylsulfonyl or benzyloxy; andA is hydrogen or ##STR2## where R.sub.2 is hydrogen or lower alkyl;R.sub.3 is lower alkyl or dimethoxyphenyl-lower alkyl; orR.sub.2 and R.sub.3, together with each other and the nitrogen atom to which they are attached, are piperidino, morpholino or N'-lower alkyl-piperazino; andn is 2 or 3;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives, antithrombotics and antiarrhythmics.
摘要翻译：其中R 1是低级烷基的式IMAMA的化合物; 苯基 - 低级烷基; 3至6个碳原子的环烷基; 苯基; 羟基，甲氧基，甲基巯基，甲基亚磺酰基，甲基磺酰基或苄氧基的取代基可以相同或不同。和A是氢或者其中R 2是氢或低级烷基; R3是低级烷基或二甲氧基苯基 - 低级烷基; 或R 2和R 3彼此连接并且与它们相连的氮原子是哌啶子基，吗啉代或N'-低级烷基 - 哌嗪子基; n为2或3; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作强心剂，低血糖剂，抗血栓药物和抗心律失常药物。

5. 发明授权

US4026891A 5- Or 6-pyridazinyl-benzimidazoles and salts thereof 失效
标题翻译： 5-或6-哒嗪基 - 苯并咪唑及其盐
公开(公告)号：US4026891A
公开(公告)日：1977-05-31
申请号：US583641
申请日：1975-06-04
申请人： Volkhard Austel , Eberhard Kutter , Joachim Heider , Wolfgang Eberlein , Rudolf Kadatz , Willi Diederen
发明人： Volkhard Austel , Eberhard Kutter , Joachim Heider , Wolfgang Eberlein , Rudolf Kadatz , Willi Diederen
IPC分类号： C07D403/04 , A61K20060101 , A61K31/415 , A61K31/495 , A61K31/50 , A61K31/535 , A61P7/02 , A61P9/04 , A61P9/12 , C07D20060101 , C07D235/04 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/14 , C07D235/18 , C07D235/24 , C07D235/28 , C07D237/00 , C07D237/02 , C07D237/04 , C07D237/08 , C07D237/12 , C07D237/14 , C07D237/20 , C07D247/00 , C07D295/12 , C07D403/02 , C07D403/10 , C07D403/14 , C07D413/14
CPC分类号： Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, trifluoromethyl, alkyl of 1 to 5 carbon atoms, mercapto, lower alkyl-mercapto, phenyl, fluoro-phenyl, tolyl, hydroxy-phenyl, methylmercapto-phenyl, methylsulfinyl-phenyl, methylsulfonyl-phenyl, dimethylamino-phenyl, or mono-, di- or tri-methoxy-substituted phenyl;A is hydrogen or, together with B, a double bond,B is hydrogen, alkyl of 1 to 3 carbon atoms or, together with A, a double bond;C is, together with R.sub.2, a double bond, or, together with R.sub.3, oxygen;R.sub.2 is hydrogen, alkyl of 1 to 3 carbon atoms or, together with C, a double bond; andR.sub.3 is chlorine, methylamino, morpholino, 4-methylpiperazino or, when R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, together with C, oxygen;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as hypotensives, antithrombotics and cardiotonics.
摘要翻译：其中R 1为氢，三氟甲基，1至5个碳原子的烷基，巯基，低级烷基 - 巯基，苯基，氟 - 苯基，甲苯基，羟基 - 苯基，甲基巯基 - 苯基，甲基亚磺酰基 - 苯基，甲基磺酰基苯基，二甲基氨基 - 苯基或单 - ，二 - 或三 - 甲氧基取代的苯基; A为氢或与B一起为双键，B为氢，1〜3个碳原子的烷基，或与A一起为双键; C与R2一起为双键，或与R3一起为氧; R 2是氢，1至3个碳原子的烷基，或与C一起形成双键; 并且R 3是氯，甲基氨基，吗啉代，4-甲基哌嗪基，或者当R 2是氢或有1至3个碳原子的烷基与C，氧时; 和非毒性，药理学上可接受的酸添加量; 该化合物作为有效的低分子量有机抗体，抗生素和心脏病。

6. 发明授权

US4179508A Sulfur-containing derivatives of 4,4-dimethyl-2H,4H-isoquinoline-1,3-dione, and anticonvulsant and antihyperlipidemic compositions thereof 失效
标题翻译： 4,4-二甲基-2H，4H-异喹啉-1,3-二酮的含硫衍生物及其抗惊厥和抗高脂血症组合物
公开(公告)号：US4179508A
公开(公告)日：1979-12-18
申请号：US925877
申请日：1978-07-18
申请人： Volkhard Austel , Eberhard Kutter , Wolfgang Eberlein , Joachim Heider , Joachim Kahling
发明人： Volkhard Austel , Eberhard Kutter , Wolfgang Eberlein , Joachim Heider , Joachim Kahling
IPC分类号： A61K31/47 , A61K31/472 , A61P3/06 , A61P25/08 , C07D217/24
CPC分类号： C07D217/24
摘要： Compounds of the formula ##STR1## wherein A is lower alkylene,R is lower alkyl, andn is 0, 1 or 2;the compounds are useful as anti-hyperlipidemics and anti-convulsants.
摘要翻译：其中A为低级亚烷基，R为低级烷基，n为0,1或2的式IMA化合物; 该化合物可用作抗高脂血症和抗惊厥药。

7. 发明授权

US4299834A 8-Phenyl-purines and pharmaceutical compositions containing same 失效
标题翻译： 8-苯基嘌呤和含有它们的药物组合物
公开(公告)号：US4299834A
公开(公告)日：1981-11-10
申请号：US166709
申请日：1980-07-08
申请人： Volkhard Austel , Eberhard Kutter , Joachim Heider , Willi Diederen
发明人： Volkhard Austel , Eberhard Kutter , Joachim Heider , Willi Diederen
IPC分类号： A61K31/52 , A61P9/04 , C07D239/48 , C07D473/00
CPC分类号： C07D239/48 , C07D473/00
摘要： This invention is directed to 8-phenyl-purines of general formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom; an alkoxy group optionally substituted by alkylmercapto, alkylsulfinyl or alkylsulfonyl group; or an alkylmercapto, alkylsulfinyl or alkylsulfonyl group, whereby each alkyl moiety may contain from 1 to 3 carbon atoms, andR.sub.2 is an alkoxy group with from 1 to 3 carbon atoms, and their physiologically compatible acid addition salts. The compounds exhibit valuable pharmacological properties, particularly positive inotropic activity.
摘要翻译：本发明涉及通式为“IMAGE”的8-苯基嘌呤，其中R 1是氢或卤素原子; 任选被烷基巯基，烷基亚磺酰基或烷基磺酰基取代的烷氧基; 或烷基巯基，烷基亚磺酰基或烷基磺酰基，其中每个烷基部分可以含有1至3个碳原子，并且R 2是具有1至3个碳原子的烷氧基，以及它们的生理上相容的酸加成盐。该化合物显示出有价值的药理学性质，特别是正性肌力活性。

8. 发明授权

US3948898A 1,3-Dioxo-2-aminoalkyl-4,4-dimethyl-isoquinolines and salts thereof 失效
标题翻译： 1,3-二氧代-2-氨基烷基-4,4-二甲基 - 异喹啉及其盐
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。

9. 发明授权

US4021558A 1,3-Dioxo-2-[(methoxyphenethyl-amino)-alkyl]-4,4-dimethyl-isoquinolines and salts thereof useful as hypotensive agents 失效
标题翻译： 1,3-二氧代-2- {8-（甲氧基苯乙基 - 氨基） - 烷基{9-4,4-二甲基 - 异喹啉及其盐作为降压剂
公开(公告)号：US4021558A
公开(公告)日：1977-05-03
申请号：US651568
申请日：1976-01-22
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： C07D217/24 , A61K31/47
CPC分类号： C07D217/24 , Y10S514/821
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, methoxy or methylthio, R.sub.2 is hydrogen or methoxy,n is 2 or 3,R.sub.3 is hydrogen or methyl, andR.sub.4 and R.sub.5, 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：其中R 1是氢，卤素，甲氧基或甲硫基，R 2是氢或甲氧基，N IS 2 OR 3，R 3是氢或甲基，R 4和R 5可以相同或相同，彼此不同，分别为氢或甲氧基，以及无毒的，药学上可接受的酸加成盐; 化合物和盐可用作低血糖，镇静剂，抗心律失常药物和心动过缓。

10. 发明授权

US3985891A 2-Phenyl-imidazo (4,5-b)pyridines and salts thereof 失效
标题翻译： 2-苯基 - 咪唑并（4,5-b）吡啶及其盐
公开(公告)号：US3985891A
公开(公告)日：1976-10-12
申请号：US606886
申请日：1975-08-22
申请人： Eberhard Kutter , Volkhard Austel , Willi Diederen
发明人： Eberhard Kutter , Volkhard Austel , Willi Diederen
IPC分类号： A61K31/395 , C07D213/74
摘要： Compounds of the isomeric formulas ##SPC1##WhereinR.sub.1 is alkoxy of 1 to 4 carbon atoms, allyloxy, benzyloxy, methoxy-ethoxy, methylthio, methylsulfinyl, methylsulfonyl or methylsulfinylethoxy,R.sub.2 is hydrogen, hydroxyl, methyl, methoxy, ethoxy, fluorine, chlorine, (alkyl of 1 to 4 carbon atoms)-thio, (alkyl of 1 to 4 carbon atoms)-sulfinyl, (alkyl of 1 to 4 carbon atoms)-sulfonyl, dimethylamino or Z-A-O-whereA is alkylene of 2 to 3 carbon atoms, andZ is chlorine, hydroxyl, methylthio, ethylthio, methylsulfinyl; ethylsulfinyl, methylsulfonyl, ethylsulfonyl, methylamino, dimethylamino, diethylamino, phenethylamino, N-methyl-phenethylamino or N-methyl-dimethoxyphenethylamino,R.sub.3 is hydrogen or methoxy,Or any two of R.sub.1, R.sub.2 and R.sub.3 together are methylenedioxy, andR.sub.5 is hydrogen, chlorine or methyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as cardiotonics, anticoagulants and for altering the blood pressure.
摘要翻译：异构体式的化合物，其中R1是具有1至4个碳原子的烷氧基，烯丙氧基，苄氧基，甲氧基 - 乙氧基，甲硫基，甲基亚磺酰基，甲基磺酰基或甲基亚硫酰基乙氧基，R2是氢，羟基，甲基，甲氧基，乙氧基，氟，氯，（烷基具有1至4个碳原子的） - 硫代，（具有1至4个碳原子的烷基） - 亚磺酰基，（1至4个碳原子的烷基） - 磺酰基，二甲基氨基或ZAO-，其中A是2至3个碳原子的亚烷基， Z是氯，羟基，甲硫基，乙硫基，甲基亚磺酰基; 乙基亚磺酰基，甲基磺酰基，乙基磺酰基，甲基氨基，二甲基氨基，二乙基氨基，苯乙基氨基，N-甲基 - 苯乙基氨基或N-甲基 - 二甲氧基苯乙基氨基，R3是氢或甲氧基，或任何两个R1，R2和R3一起是亚甲二氧基，R5是氢，氯或甲基，和非毒性，药理学上可接受的酸添加量; 化合物作为细胞因子有利于心脏病，抗凝血剂和改善血压。

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