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1. 发明授权

US4871735A Naphthyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：萘衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US4871735A
公开(公告)日：1989-10-03
申请号：US96097
申请日：1987-09-11
申请人： Joachim Heider , Manfred Psiorz , Andreas Bomhard , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Jurgen Dammgen
发明人： Joachim Heider , Manfred Psiorz , Andreas Bomhard , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Jurgen Dammgen
IPC分类号： C07D209/48 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/55 , A61P9/00 , A61P9/12 , C07D209/44 , C07D209/46 , C07D217/04 , C07D217/22 , C07D217/24 , C07D223/16 , C07D491/04 , C07D491/056
CPC分类号： C07D223/16 , C07D209/44 , C07D209/46 , C07D217/04 , C07D217/24 , C07D491/04
摘要： The present invention relates to new naphthyl derivatives of general formula ##STR1## wherein N represents the number 1 or 2,A represents a --CH.sub.2 --, --CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## while the atom marked with an x is linked to the phenyl nucleus, E represents a straight chained alkylene group optionally substituted by an alkyl group,G represents a straight chained alkylene group optionally substituted by an alkyl group,L represents a bond or an oxygen atom, if G represents a straight chained alkylene group with 2 to 5 carbon atoms optionally substituted by an alkyl group,R.sub.1 and R.sub.2, which may be identical or different, represent alkyl or alkoxy groups or R.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, or an alkyl or an allyl group,R.sub.4, R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen atoms, alkyl or alkoxy groups, the enantiomers and the acid addition salts thereof, which have valuable pharmacological properties, particularly a heart rate lowering activity.The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的萘基衍生物，其中N表示数1或2，A表示-CH 2 - ， - CO - ， - CH 2 CH 2 - ， - CH = CH-，而标记有x的原子与苯基连接，E表示任选被烷基取代的直链亚烷基，G表示任选被烷基取代的直链亚烷基，L表示键或氧原子如果G表示任选被烷基取代的具有2至5个碳原子的直链亚烷基，则可以相同或不同的R 1和R 2表示烷基或烷氧基，或者R 1和R 2一起表示亚烷基二氧基，R 3表示氢原子或烷基或烯丙基，可以相同或不同的R 4，R 5和R 6表示氢原子，烷基或烷氧基，其对映体和酸加成盐，具有有价值的药理学性质，特别是一个心率下降活动。新化合物可以使用本身已知的方法制备。

2. 发明授权

US4616011A Novel indole derivatives and pharmaceutical compositions containing same 失效
标题翻译：新型吲哚衍生物和含有它们的药物组合物
公开(公告)号：US4616011A
公开(公告)日：1986-10-07
申请号：US675084
申请日：1984-11-26
申请人： Manfred Reiffen , Joachim Heider , Volkhard Austel , Norbert Hauel , Walter Kobinger , Christian Lillie
发明人： Manfred Reiffen , Joachim Heider , Volkhard Austel , Norbert Hauel , Walter Kobinger , Christian Lillie
IPC分类号： A61K31/55 , A61P9/06 , A61P9/08 , A61P9/10 , A61P25/02 , C07C59/64 , C07D209/14 , C07D209/16 , C07D209/18 , C07D223/16 , C07D403/12 , C07D405/14
CPC分类号： C07D223/16 , C07C59/64 , C07D209/16 , C07D209/18 , C07D403/12
摘要： This invention relates to novel indole derivatives of the formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## group and B represents a methylene, carbonyl, or thiocarbonyl group or A represents a --CO--CO-- or ##STR3## group and B represents a methylene group, E represents an alkylene group or a 2-hydroxy-n-propylene, 2-hydroxy-n-butylene, or 3-hydroxy-n-butylene group,G represents an alkylene group,R.sub.1 represents a hydrogen, chlorine, or bromine atom or a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine, or bromine atom or a hydroxyl, alkoxy, phenylalkoxy, or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen, chlorine, or bromine atom or an alkyl group,R.sub.4 represents a hydrogen atom or an alkyl or phenylalkyl group,R.sub.5 represents a hydrogen, fluorine, chlorine, or bromine atom or an alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.6 represents a hydrogen atom or an alkoxy group, andR.sub.7 represents a hydrogen atom or an alkenyl, alkyl or phenylalkyl group,and the acid additional salts thereof. These compounds, which may be obtained by use of known methods, have valuable pharmacological properties, particularly a heart rate-lowering activity.
摘要翻译：本发明涉及式（I）的新的吲哚衍生物，其中A代表-CH2-CH2-，-CH = CH-，IMA组，B代表亚甲基，羰基或硫代羰基，或A代表 -CO-CO-或基，B表示亚甲基，E表示亚烷基或2-羟基正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯基，G表示亚烷基，R 1表示氢，氯或溴原子或三氟甲基，硝基，氨基，烷基氨基，二烷基氨基，烷基，羟基，烷氧基或苯基烷氧基，R 2表示氢，氯或溴原子或羟基，烷氧基，苯基烷氧基或烷基，或者R 1和R 2一起表示亚烷基二氧基，R 3表示氢，氯或溴原子或烷基，R 4表示氢原子或烷基或苯基烷基，R 5表示氢，氟，氯或溴原子或烷基，羟基，烷氧基或苯基烷氧基，R6代表氢原子或烷氧基，R7表示氢原子或烯基，烷基或苯基烷基，及其酸加成盐。可以通过使用已知方法获得的这些化合物具有有价值的药理学性质，特别是心率降低活性。

3. 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

4. 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.

5. 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。

6. 发明授权

US07996127B2 Display system for a trailer vehicle 有权
标题翻译：拖车车辆的显示系统
公开(公告)号：US07996127B2
公开(公告)日：2011-08-09
申请号：US12308631
申请日：2007-05-02
申请人： Joachim Heider , Bernd Heise , Axel Stender , Norbert Witte
发明人： Joachim Heider , Bernd Heise , Axel Stender , Norbert Witte
IPC分类号： G01C22/02
CPC分类号： G01C22/02
摘要： A display system is provided for a trailer equipped with an electronic braking system (EBS) and/or an anti-lock braking system (ABS). A separate display device having a display is provided for indicating at least the mileage on the trailer vehicle. In order to reduce the amount of wiring required, a speed signal of at least one of the wheels of the trailer is looped through the EBS/ABS and is routed directly to the display device.
摘要翻译：为配备有电子制动系统（EBS）和/或防抱死制动系统（ABS）的拖车提供显示系统。提供具有显示器的单独的显示装置，用于至少指示拖车上的行驶里程。为了减少所需的接线量，拖车的至少一个车轮的速度信号通过EBS / ABS循环并被直接路由到显示设备。

7. 发明授权

US4912115A Heteroaromatic amine derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：杂芳族胺衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US4912115A
公开(公告)日：1990-03-27
申请号：US125626
申请日：1987-11-25
申请人： Andreas Bomhard , Joachim Heider , Manfred Psiorz , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Willi Diederen
发明人： Andreas Bomhard , Joachim Heider , Manfred Psiorz , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Willi Diederen
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/472 , A61P9/00 , A61P9/08 , A61P9/10 , C07D209/44 , C07D209/46 , C07D209/48 , C07D217/04 , C07D217/08 , C07D217/14 , C07D217/22 , C07D217/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/056
CPC分类号： C07D209/48 , C07D209/44 , C07D209/46 , C07D217/14 , C07D217/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04
摘要： The present invention relates to new heteroaromatic amine derivatives of general formula ##STR1## wherein the substituents are defined hereinbelow, which have valuable pharmacological properties, particularly a heart rate lowering activity and a positive inotropic activity.
摘要翻译：本发明涉及通式为（I）的新的杂芳族胺衍生物，其中取代基定义如下，其具有有价值的药理学性质，特别是心率降低活性和正性肌力活性。

8. 发明授权

US4831027A Imidazo-benzoxazinones, the preparation thereof and pharmaceutical compositions containing these compounds 失效
标题翻译：咪唑并苯并恶嗪酮，其制备方法和含有这些化合物的药物组合物
公开(公告)号：US4831027A
公开(公告)日：1989-05-16
申请号：US105144
申请日：1987-10-05
申请人： Berthold Narr , Norbert Hauel , Klaus Noll , Joachim Heider , Manfred Psiorz , Andreas Bomhard , Jacques van Meel , Willi Diederen
发明人： Berthold Narr , Norbert Hauel , Klaus Noll , Joachim Heider , Manfred Psiorz , Andreas Bomhard , Jacques van Meel , Willi Diederen
IPC分类号： A61K31/535 , A61P7/02 , C07D498/04
CPC分类号： C07D498/04
摘要： The invention relates to new imidazo-benzoxazinones of formula ##STR1## wherein the substituents are defined herein below, which compounds are useful in the treatment of cardiovascular disorders.
摘要翻译：本发明涉及式（I）的新的咪唑并 - 苯并嗪酮，其中取代基如下文所定义，该化合物可用于治疗心血管疾病。

9. 发明授权

US4766130A 2-phenyl-imidazopyridin-ones and also useful as cardiotonics and anti-hypertensives 失效
标题翻译： 2-苯基 - 咪唑并吡啶酮，也可用作强心剂和抗高血压药
公开(公告)号：US4766130A
公开(公告)日：1988-08-23
申请号：US7530
申请日：1987-01-28
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 , A61K31/435
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 =，HN =，R 3 N =，O = C =，HC 3 SO，HO-C 3 SO 3或R 3 SO 2 -O-C 3 DON的式并且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

US4699909A Benzotriazolyl-4,5-dihydro-3(2H)-pyridazinones 失效
标题翻译：苯并三唑基-4,5-二氢-3（2H） - 哒嗪酮
公开(公告)号：US4699909A
公开(公告)日：1987-10-13
申请号：US889814
申请日：1986-07-24
申请人： Norbert Hauel , Volkhard Austel , Joachim Heider , Manfred Reiffen , Willi Diederen , Walter Haarman
发明人： Norbert Hauel , Volkhard Austel , Joachim Heider , Manfred Reiffen , Willi Diederen , Walter Haarman
IPC分类号： C07D237/04 , C07D249/18 , C07D401/14 , C07D403/04 , C07D403/02 , A61K31/50
CPC分类号： C07D401/14 , C07D237/04 , C07D249/18 , C07D403/04
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methypyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; andR.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives and antithrombotics.
摘要翻译：其中R 1是氢的式IMAMA的化合物; 1至7个碳原子的烷基; 3至7个碳原子的环烷基; 取代基为吡啶基，甲基吡啶基，苯基，单 - ，二 - 或三取代苯基的单取代烷基，其中苯环上的取代基可以相同或不同，选自由一个氨基，一个二甲基氨基，一至两个羟基，一至三个甲氧基和一至三个卤素组成的组; 2至4个碳原子的ω-单取代的烷基，其中取代基是羟基或二（1至3个碳原子的烷基）氨基; 苯基; 单卤代苯基; 未取代的或单取代的1至6个碳原子的直链或支链烷酰基，其中取代基是苯基，甲氧基苯基或3-7个碳原子的环烷基; 或未取代或单取代的苯基磺酰基，其中取代基是甲基或甲氧基; 并且R 2是氢或1至3个碳原子的烷基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作强心剂，低血糖剂和抗血栓药物。

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