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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

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。

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

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。

6. 发明授权

US4361563A Pyridazinone-substituted benzimidazoles and salts 失效
标题翻译：哒嗪酮取代的苯并咪唑和盐
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。

7. 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。

8. 发明授权

US4722929A Novel 2-phenyl-imidazoles and pharmaceutical compositions containing same 失效
标题翻译：新的2-苯基 - 咪唑和含有它们的药物组合物
公开(公告)号：US4722929A
公开(公告)日：1988-02-02
申请号：US684052
申请日：1984-12-20
申请人： Volkhard Austel , Joachim Heider , Norbert Hauel , Manfred Reiffen , Josef Nickl , Jacobus C. A. van Meel , Willi Diederen
发明人： Volkhard Austel , Joachim Heider , Norbert Hauel , Manfred Reiffen , Josef Nickl , Jacobus C. A. van Meel , Willi Diederen
IPC分类号： A61K31/435 , A61K31/50 , A61K31/53 , A61P9/00 , A61P9/04 , A61P9/12 , C07D213/75 , C07D239/54 , C07D239/545 , C07D471/04 , C07D473/00 , C07D473/04 , C07D473/06 , C07D473/28 , C07D473/30 , C07D473/40 , C07D487/04
CPC分类号： C07D213/75 , C07D239/545 , C07D471/04 , C07D473/00 , C07D473/04 , C07D473/06 , C07D473/40 , C07D487/04
摘要： The invention relates to novel 2-phenyl-imidazoles of the formula ##STR1## and the tautomers and acid addition salts thereof, particularly the pharmacologically acceptable acid addition salts, which exhibit valuable pharmacological properties, particularly an effect on the contractility of the heart muscle. The compounds of Formula I may be prepared by methods conventionally used for similar compounds.
摘要翻译：本发明涉及新颖的式（I）的2-苯基 - 咪唑及其互变异构体及其酸加成盐，特别是药理学上可接受的酸加成盐，其具有有价值的药理学性质，特别是对心脏肌肉式I的化合物可以通过常规用于类似化合物的方法制备。

9. 发明授权

US4670438A Imidazo[4,5-c]pyridazine-3-ones, imidazo[4,5-d]pyridazine-4-ones, imidazo[4,]pyrazin-5-ones, purin-2-ones, purin-6-ones, and purin-2,6-diones useful as hypotensive or cardiotonic agents 失效
标题翻译：咪唑并[4,5-c]哒嗪-3-酮，咪唑并[4,5-d]哒嗪-4-酮，咪唑并[4,5-b]吡嗪-5-酮，嘌呤-2-酮， 6-酮和嘌呤-2,6-二酮可用作降血压或强心剂
公开(公告)号：US4670438A
公开(公告)日：1987-06-02
申请号：US623718
申请日：1984-06-22
申请人： Volkhard Austel , Joachim Heider , Norbert Hauel , Manfred Reiffen , Jacobus C. A. van Meel , Willi Diederen
发明人： Volkhard Austel , Joachim Heider , Norbert Hauel , Manfred Reiffen , Jacobus C. A. van Meel , Willi Diederen
IPC分类号： A61K31/44 , A61K31/50 , A61K31/52 , A61K31/522 , A61K31/53 , A61P9/04 , A61P9/12 , C07D471/04 , C07D473/02 , C07D473/04 , C07D473/08 , C07D473/28 , C07D473/30 , C07D473/40 , C07D487/04 , A61K31/495
CPC分类号： C07D471/04 , C07D473/02 , C07D473/08 , C07D473/28 , C07D473/30 , C07D473/40 , C07D487/04
摘要： Compounds of the formula ##STR1## wherein A, B, C and D are --N.dbd., HN.dbd., R.sub.3 N.dbd., O.dbd.C.dbd., HC.tbd., HO--C.tbd. or R.sub.3 SO.sub.2 --O--C.tbd.; andR.sub.1 and R.sub.2 are substituents of various types.The compounds are useful as hypotensives and cardiotonics.
摘要翻译：其中A，B，C和D为-N + 50，HN =，R3N =，O = C =，HC 3BOND，HO-C 3BOND或R3SO2-O-C3OND的式IMA化合物; 并且R 1和R 2是各种类型的取代基。这些化合物可用作低渗剂和强心剂。

10. 发明授权

US4716169A Imidazo[1,2a]pyridines and their use as cardiotonic agents 失效
标题翻译：咪唑并[1,2a]吡啶并用作强心剂
公开(公告)号：US4716169A
公开(公告)日：1987-12-29
申请号：US810008
申请日：1985-12-17
申请人： Joachim Heider , Norbert Hauel , Volkhard Austel , Klaus Noll , Andreas Bomhard , Jacques van Meel , Willi Diederen
发明人： Joachim Heider , Norbert Hauel , Volkhard Austel , Klaus Noll , Andreas Bomhard , Jacques van Meel , Willi Diederen
IPC分类号： A61K31/435 , A61K31/495 , A61P7/02 , A61P9/04 , C07D471/04 , C07D487/04 , A61K31/41
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to new imidazo derivatives of the formula ##STR1## wherein "A-D and R.sup.1 -R.sup.3 are as defined in the specification". The new compounds have valuable pharmacological properties, particularly antithrombotic and cardiovascular properties such as a cardiotonic activity and/or an effect on blood pressure, and can be prepared using methods known per se.
摘要翻译：本发明涉及式（I）的新的咪唑衍生物，其中“A-D和R 1 -R 3如说明书中所定义”。新化合物具有有价值的药理学性质，特别是抗血栓形成和心血管性质，例如强心剂活性和/或对血压的作用，并且可以使用本身已知的方法制备。

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