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1. 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。

2. 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.

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

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。

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

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

US4134980A Phenylalkylamino-alkyl derivatives of quinazolinone and phthalazinone 失效
标题翻译：喹唑啉酮和酞嗪酮的苯基烷基氨基 - 烷基衍生物
公开(公告)号：US4134980A
公开(公告)日：1979-01-16
申请号：US827142
申请日：1977-08-24
申请人： Wolfgang Eberlein , Volkhard Austel , Joachim Heider , Jurgen Dammgen , Rudolf Kadatz , Christian Lillie , Walter Kobinger
发明人： Wolfgang Eberlein , Volkhard Austel , Joachim Heider , Jurgen Dammgen , Rudolf Kadatz , Christian Lillie , Walter Kobinger
IPC分类号： C07D239/91 , A61K31/50 , A61K31/502 , A61K31/505 , A61K31/517 , A61P9/06 , A61P9/12 , B01J23/00 , C07D237/00 , C07D237/32 , C07D239/88 , C07D239/90 , C07D317/00 , C07D319/00 , C07D405/12 , C07D491/04 , C07D491/056 , C07D239/72
CPC分类号： C07D491/04 , C07D237/32 , C07D239/90
摘要： Compounds of the formula ##STR1## wherein A is ##STR2## where R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is alkoxy of 1 to 3 carbon atoms;R.sub.3 is alkoxy of 1 to 3 carbon atoms or, together with R.sub.2, methylenedioxy or ethylenedioxy;R.sub.4 is hydrogen, alkyl of 1 to 3 carbon atoms or benzyl;R.sub.5 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.6 is hydrogen or alkoxy of 1 to 3 carbon atoms;R.sub.7 is alkoxy of 1 to 3 carbon atoms or, together with R.sub.6, methylenedioxy or ethylenedioxy; andN is 2 or 3;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as heart rate reducers and mild antihypertensives.This invention relates to novel N-(phenylalkylaminoalkyl)-substituted quinazolinones and phthalazinones and nontoxic acid addition salts thereof, as well as to various methods of preparing these compounds.More particularly, the present invention relates to a novel class of N-substituted quinazolinones and phthalazinones represented by the formula ##STR3## wherein A is ##STR4## where R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is alkoxy of 1 to 3 carbon atoms;R.sub.3 is alkoxy of 1 to 3 carbon atoms or, together with R.sub.2, methylenedioxy or ethylenedioxy;R.sub.4 is hydrogen, alkyl of 1 to 3 carbon atoms or benzyl;R.sub.5 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.6 is hydrogen or alkoxy of 1 to 3 carbon atoms;R.sub.7 is alkoxy of 1 to 3 carbon atoms or, together with R.sub.6, methylenedioxy or ethylenedioxy; andN is 2 or 3;Or a non-toxic, pharmacologically acceptable acid addition salt thereof.A preferred sub-genus thereunder is constituted by compounds of the formula I whereR.sub.1 and R.sub.5 are each hydrogen, methyl, ethyl, n-propyl or isopropyl;R.sub.4 is hydrogen, methyl, ethyl, n-propyl, isopropyl or benzyl;R.sub.2, r.sub.3 and R.sub.7 are each methoxy, ethoxy, n-propoxy or isopropoxy;R.sub.6 is hydrogen, methoxy, ethoxy, n-propoxy or isopropoxy;R.sub.2 and R.sub.3, together with each other, are methylenedioxy or ethylenedioxy;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.A further, especially preferred sub-genus thereunder is constituted by compounds of the formula I whereR.sub.2 and R.sub.3 are methoxy in the 6- and 7-position, respectively, or, together with each other, methylenedioxy or ethylenedioxy;R.sub.4 is hydrogen or methyl;R.sub.5 is hydrogen;R.sub.6 is hydrogen or methoxy in the 3-position;R.sub.7 is methoxy in the 4-position or, together with R.sub.6, methylenedioxy or ethylenedioxy; andn is 2 or 3;and non-toxic, pharmacologically acceptable acid addition salts thereof.The compounds embraced by formula I may be prepared by the following methods:Method ABy reacting a compound of the formula ##STR5## wherein R.sub.2, R.sub.3, A and n have the same meanings as in formula I, andZ is a leaving-group, such as chlorine, bromine, iodine, alkylsulfonyloxy or arylsulfonyloxy,with a phenylalkylamine of the formula ##STR6## wherein R.sub.4, R.sub.5, R.sub.6 and R.sub.7 have the same meanings as in formula I.The reaction is carried out in an inert solvent, such as ether, tetrahydrofuran, methylformamide, dimethylformamide, dimethylsulfoxide, chlorobenzene or benzene, and depending upon the reactivity of substituent Z, at a temperature between -50 and +250.degree. C, but preferably at the boiling point of the particular solvent which is used. The presence of an acid-binding agent, such as an alkali metal alcoholate, an alkali metal hydroxide, an alkali metal carbonate, especially potassium carbonate, or a tertiary organic base, particularly triethylamine or pyridine, or of a reaction accelerator, such as potassium iodide, is of advantage.Method BBy reacting a compound of the formula ##STR7## wherein A, R.sub.2 and R.sub.3 have the same meanings as in formula I, with a phenylalkylamine of the formula ##STR8## wherein R.sub.4, R.sub.5, R.sub.6 and n have the same meanings as in formula I, andZ has the same meanings as in formula II.The reaction is carried out in an inert solvent, such as acetone, dimethylformamide, dimethylsulfoxide or chlorobenzene, and, depending upon the reactivity of substituent Z, at a temperature between 0 and 150.degree. C, but preferably at the boiling point of the particular solvent which is used. The presence of an acid-binding agent, such as an alkali metal alcoholate, an alkali metal hydroxide, an alkali metal carbonate, especially potassium carbonate, an alkali metal amide or a tertiary organic base, particularly triethylamine or pyridine, or of a reaction accelerator, such as potassium iodide, is of advantage.Method CBy reacting an aldehyde of the formula ##STR9## wherein R.sub.2, R.sub.3, A and n have the same meanings as in formula I, or an acetal thereof, with an amine of the formula III in the presence of catalytically activated hydrogen.The reductive amination is carried out with hydrogen in the presence of a hydrogenation catalyst, such as palladized charcoal, at a hydrogen pressure of 5 atmospheres, in a solvent, such as methanol, ethanol or dioxane, and at a temperature between 0 and 100.degree. C, but preferably between 20 and 80.degree. C.Method DBy reacting an amine of the formula ##STR10## wherein R.sub.2, R.sub.3, R.sub.4, A and n have the same meanings as in formula I, with a phenylalkyl compound of the formula ##STR11## wherein R.sub.5, R.sub.6 and R.sub.7 have the same meanings as in formula I, andZ has the same meanings as in formula II.The reaction is carried out in an inert solvent, such as acetone, methylene chloride, dimethylformamide, dimethylsulfoxide or chlorobenzene, and, depending upon the reactivity of substituent Z, at a temperature between 0 and 150.degree. C, but preferably at the boiling point of the particular solvent which is used. The presence of an acid-binding agent, such as an alkali metal alcoholate, an alkali metal hydroxide, an alkali metal carbonate, especially potassium carbonate, or a tertiary organic base, particularly triethylamine or pyridine, or of a reaction accelerator, such as potassium iodide, is of advantage.Method EFor the preparation of a quinazolinone derivative of the formula I, by reacting a benzoxazin-4-one of the formula ##STR12## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as in formula I, with an alkylenediamine of the formula wherein R.sub.4, R.sub.5, R.sub.6 and R.sub.7 have the same meanings as in formula I.The reaction is advantageously carried out in a solvent, such as benzene, dioxane, a lower alkanoic acid such as glacial acetic acid, or dimethylformamide, and optionally in the presence of an acid catalyst at a temperature between 50 and 150.degree. C, but preferably at the boiling point of the particular solvent which is used. The preferred solvent is glacial acetic acid. The reaction may, however, also be performed without a solvent.If the end product of methods A through E is a compound of the formula I wherein R.sub.4 is benzyl, the same may be de-benzylated to yield the corresponding compound wherein R.sub.4 is hydrogen. The de-benzylation is preferably effected by means of catalytic hydrogenation, for example with hydrogen in the presence of a catalyst such as palladized charcoal, in a solvent such as ethanol or ethylacetate, at a temperature between 25 and 75.degree. C and at a hydrogen pressure of 1 to 7 atmospheres.On the other hand, if the end product of methods A through E is a compound of the formula I wherein R.sub.4 is hydrogen; the same may be alkylated at the bridge nitrogen atom to form the corresponding compound where R.sub.4 is alkyl. The alkylation is carried out with a conventional alkylating agent, for example with an alkyl halide such as methyl iodide, ethyl iodide or isopropyl bromide, or with a dialkylsulfate such a dimethylsulfate, in a solvent such as acetone, dimethylformamide or dioxane, optionally in the presence of an inorganic or tertiary organic base, at a temperature between 0 and 50.degree. C. A methylation may also be effected by reaction with a mixture of formaldehyde and formic acid, preferably at the boiling point of said mixture.The compounds embraced by formula I are organic bases and therefore form acid addition salts with inorganic or organic acids. Examples of non-toxic, pharmacologically acceptable acid addition salts are those formed with hydrochloric acid, phosphoric acid, hydrobromic acid, sulfuric acid, lactic acid, tartaric acid, maleic acid, 8-chlorotheophylline or the like.The starting compounds of the formulas II through X are either described in the literature or may be prepared by known methods, as described in the examples below.
摘要翻译：其中A是其中R 1是氢或1至3个碳原子的烷基的式“IMAGE”的化合物; R 2是1至3个碳原子的烷氧基; R3为1〜3个碳原子的烷氧基，或与R2一起亚甲二氧基或亚乙二氧基; R4是氢，1至3个碳原子的烷基或苄基; R5是氢或1〜3个碳原子的烷基; R6是氢或1〜3个碳原子的烷氧基; R 7为1〜3个碳原子的烷氧基，或与R6一起亚甲二氧基或亚乙二氧基; 和N IS 2 OR 3; 和非毒性，药理学上可接受的酸添加量; 化合物作为其有效的有效的H

8. 发明授权

US4154837A (Aminoalkoxy-aryl)-substituted isoquinolinones and naphthydrinones and salts thereof, and hypotensive compositions and methods employing them 失效
标题翻译：（氨基烷氧基 - 芳基） - 取代的异喹啉酮和萘啶酮及其盐，以及使用它们的低血压组合物和方法
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。

9. 发明授权

US4490369A Benzazepine derivatives, their pharmaceutical compositions and method of use 失效
标题翻译：苯扎西平衍生物，其药物组合物和使用方法
公开(公告)号：US4490369A
公开(公告)日：1984-12-25
申请号：US547940
申请日：1983-11-02
申请人： Manfred Reiffen , Joachim Heider , Norbert Hauel , Volkhard Austel , Wolfgang Eberlein , Walter Kobinger , Christian Lillie , Klaus Noll , Helmut Pieper , Gerd Kruger , Johannes Keck
发明人： Manfred Reiffen , Joachim Heider , Norbert Hauel , Volkhard Austel , Wolfgang Eberlein , Walter Kobinger , Christian Lillie , Klaus Noll , Helmut Pieper , Gerd Kruger , Johannes Keck
IPC分类号： C07C59/64 , C07D205/04 , C07D223/16 , C07D243/02 , C07D243/04 , C07D491/04 , A61K31/55 , C07D521/00
CPC分类号： C07D223/16 , C07C59/64 , C07D205/04 , C07D243/02 , C07D243/04 , C07D491/04
摘要： Compounds of the formula ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO--, --CH.sub.2 --CO-- or ##STR2## where R.sub.7 is alkyl of 1 to 3 carbon atoms, andB is methylene, carbonyl or thiocarbonyl, orA is --CO--CO--, --N.dbd.CH--, ##STR3## where R.sub.8 is hydrogen or alkyl of 1 to 3 carbon atoms substituted by a phenyl, methoxyphenyl or dimethoxyphenyl, andB is methylene;E is n-alkylene of 2 to 4 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;G is n-alkylene of 1 to 5 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, wherein one methylene group of an n-alkylene of 2 to 5 carbon atoms can be replaced by a carbonyl group, with the proviso that B represents a methylene or carbonyl group, or methylene-n-hydroxy-alkylene of 1 to 4 carbon atoms, where the methylene group is attached to the nitrogen atom; andR.sub.1 to R.sub.5 are simple substituents of various types;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要翻译：其中A是-CH 2 -CH 2 - ， - CH = CH - ， - NH-CO-， - CH 2 -CO-或者其中R 7是1至3个碳原子的烷基，和B 是亚甲基，羰基或硫代羰基，或A是-CO-CO-，-N = CH-，其中R 8是氢或被苯基，甲氧基苯基或二甲氧基苯基取代的1至3个碳原子的烷基，和 B是亚甲基; E是任选被1至3个碳原子的烷基取代的2至4个碳原子的正亚烷基，2-羟基 - 正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯; G是任选被1至3个碳原子的烷基取代的1至5个碳原子的正亚烷基，其中2至5个碳原子的正亚烷基的一个亚甲基可被羰基取代，条件是 B表示亚甲基或羰基，或亚甲基与氮原子连接的1至4个碳原子的亚甲基 - 正 - 羟基 - 亚烷基; 而R1至R5是各种简单的取代基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作心动过缓。

10. 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。

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