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1. 发明授权

US5175157A Cyclic amine derivatives, pharmaceutical compositions containing these compounds and methods for preparing them 失效
标题翻译：环胺衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5175157A
公开(公告)日：1992-12-29
申请号：US725855
申请日：1991-07-03
申请人： Manfred Psiorz , Joachim Heider , Andreas Bomhard , Manfred Reiffen , Norbert Hauel , Klaus Noll , Berthold Narr , Christian Lillie , Walter Kobinger , Jurgen Dammgen
发明人： Manfred Psiorz , Joachim Heider , Andreas Bomhard , Manfred Reiffen , Norbert Hauel , Klaus Noll , Berthold Narr , Christian Lillie , Walter Kobinger , Jurgen Dammgen
IPC分类号： C07D223/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D491/04
CPC分类号： C07D223/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D491/04
摘要： Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.
摘要翻译：公开了式I（I）的新的环胺衍生物，其中取代基在说明书中定义。这些化合物可用于治疗窦性心动过速。

2. 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。

3. 发明授权

US5116986A Heteroaromatic amine derivatives 失效
标题翻译：异构胺衍生物
公开(公告)号：US5116986A
公开(公告)日：1992-05-26
申请号：US696677
申请日：1991-05-07
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.

4. 发明授权

US4737495A (2H)-3-benzazepin-2-ones, their pharmaceutical compositions and their pharmaceutical uses 失效
公开(公告)号：US4737495A
公开(公告)日：1988-04-12
申请号：US868986
申请日：1986-05-30
申请人： Andreas Bomhard , Manfred Psiorz , Joachim Heider , Norbert Hauel , Klaus Noll , Berthold Narr , Walter Kobinger , Christian Lillie
发明人： Andreas Bomhard , Manfred Psiorz , Joachim Heider , Norbert Hauel , Klaus Noll , Berthold Narr , Walter Kobinger , Christian Lillie
IPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D521/00 , A61K31/445 , A61K31/47 , A61K31/55 , C07D233/16
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04
摘要： The invention relates to new heteroaromatic amine derivatives of formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--or ##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, in which the carbon atom marked 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,R.sub.1 represents a hydrogen, fluorine, chlorine or bromine atom, a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylmercapto, hydroxy, alkoxy or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, an alkenyl group, an alkyl or phenylalkyl group, andHet represents a 5- or 6-membered heteroaromtic ring bonded via a carbon or nitrogen atom, which contains an oxygen, sulphur or nitrogen atom, two nitrogen atoms or a nitrogen atom and an oxygen or sulphur atom, and onto which additionally a phenyl ring can be condensed, in which case the bond can also be via the phenyl nucleus, or an imidazo[1,2-a]pyridyl group wherein the carbon structure of the above-mentioned groups can be substituted by a methylenedioxy or ethylenedioxy group or can be mono- or disubstituted by a halogen atom or an alkyl, hydroxy, alkoxy, phenylalkoxy, phenyl, dimethoxyphenyl, nitro, amino, acetylamino, carbamoylamino, N-alkyl-carbamoylamino, hydroxymethyl, mercapto, alkylmercapto, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, alkylsulphonylamino, alkoxycarbonylmethoxy, carboxymethoxy or alkoxymethyl group, and at the same time any imino group present in the above-mentioned heteroaromatic groups can be substituted by an alkyl, phenylalkyl or phenyl group, the N-oxides and the acid addition salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly the effect of lowering heart rate and oxygen requirement of the heart. They can be used to treat sinus tachycardia or ischaemic heart disease.

5. 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。

6. 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。

7. 发明授权

US4604389A Benzazepine derivatives 失效
标题翻译：苯扎西平衍生物
公开(公告)号：US4604389A
公开(公告)日：1986-08-05
申请号：US732204
申请日：1985-05-08
申请人： Manfred Reiffen , Klaus Noll , Joachim Heider , Volkhard Austel , Norbert Hauel , Walter Kobinger , Christian Lillie
发明人： Manfred Reiffen , Klaus Noll , Joachim Heider , Volkhard Austel , Norbert Hauel , Walter Kobinger , Christian Lillie
IPC分类号： A61K31/55 , A61P9/06 , C07C59/64 , C07D223/16 , C07D233/16 , C07D243/04 , C07D405/12 , C07D491/04 , C07D491/056 , C07D521/00
CPC分类号： C07D223/16 , C07C59/64 , C07D243/04 , C07D405/12 , C07D491/04
摘要： This invention relates to benzazepine derivatives of formula I ##STR1## wherein A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sub.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, acylamino, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy or, together with R.sub.1, can be C.sub.1 -C.sub.3 alkylenedioxy;R.sub.3 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.3 alkoxy;R.sub.4 is hydrogen, benzyl, C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.5 alkenyl;R.sub.5 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy or, together with R.sub.5, can be a C.sub.1 -C.sub.2 alkylenedioxy;X is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is oxygen, sulphur, sulphinyl or sulphonyl;Y is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is methylene or carbonyl;m and n are each independently 2, 3 or 4; and nontoxic, pharmaceutically acceptable addition salts thereof. These compounds have valuable pharmacological properties, particularly the effect of lowering heart rate and reducing the O.sub.2 requirement of the heart.
摘要翻译：本发明涉及式I的苯并氮杂衍生物，其中A是-CH 2 CH 2 - 或-CH = CH-; R1是氢，氯，溴，C1-C3烷基，氨基，C1-C3烷基氨基，C1-C3二烷基氨基，酰氨基，羟基，C1-C3烷氧基或苯基C1-C3烷氧基; R2是氢，氯，溴，羟基，C1-C3烷基，C1-C3烷氧基或苯基C1-C3烷氧基，或与R1一起可以是C1-C3亚烷基二氧基; R3是氢，氯，溴或C1-C3烷氧基; R4是氢，苄基，C1-C3烷基或C3-C5烯基; R5是氢，卤素，C1-C3烷基或C1-C3烷氧基; R 6是氢，C 1 -C 3烷基或C 1 -C 3烷氧基，或与R 5一起可以是C 1 -C 2亚烷基二氧基; X是任选被苄基或C 1 -C 3烷基取代的亚氨基，或是氧，硫，亚磺酰基或磺酰基; Y是任选被苄基或C 1 -C 3烷基取代的亚氨基，或亚甲基或羰基; m和n各自独立地为2,3或4; 和无毒的药学上可接受的加成盐。这些化合物具有有价值的药理学特性，特别是降低心率并降低心脏O2需求的作用。

8. 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。

9. 发明授权

US4584293A Aminotetralin derivatives 失效
标题翻译：氨基四氢萘衍生物
公开(公告)号：US4584293A
公开(公告)日：1986-04-22
申请号：US732199
申请日：1985-05-08
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 , C07C45/00 , C07C45/51 , C07C49/755 , C07C57/58 , C07C59/64 , C07C205/56 , C07D223/16 , C07D243/04 , C07D491/056 , C07D521/00
CPC分类号： C07D223/16 , C07C205/56 , C07C45/00 , C07C45/513 , C07C49/755 , C07C57/58 , C07C59/64 , C07D231/12 , C07D233/56 , C07D243/04 , C07D249/08
摘要： This invention related to new aminotetralin derivatives of formula I ##STR1## wherein ##STR2## B is methylene or, when A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO-- or --CH.sub.2 --CO--, B can also be carbonyl or thiocarbonyl;E is a C.sub.2 -C.sub.4 straight-chain alkylene, optionally substituted by a C.sub.1 -C.sub.3 alkyl, or is 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;R.sub.1 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, nitro, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylthio, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkoxy phenyl C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkyl or, together with R.sub.1, can be a C.sub.1 -C.sub.2 alkylenedioxy;R.sub.3 and R.sub.4 are each independently selected from hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, nitro, amino, C.sub.1 -C.sub.3 alkylamino, or C.sub.1 -C.sub.3 dialkylamino, or together can be methylenedioxy; andR.sub.5 is hydrogen, C.sub.3 -C.sub.5 alkenyl, C.sub.1 -C.sub.3 alkyl, or phenyl C.sub.1 -C.sub.3 alkyl, and nontoxic, pharmaceutically acceptable addition salts thereof which have valuable pharmacological properties, particularly a long-lasting heart rate lowering effect and the effect of reducing the O.sub.2 requirement of the heart.
摘要翻译：本发明涉及新的式I的氨基蝶呤衍生物，其中B是亚甲基，或当A是-CH 2 -CH 2 - 时，-CH = CH-，-NH-CO-或-CH 2 -CO-，B也可以是羰基或硫代羰基; E是任选被C 1 -C 3烷基取代的C 2 -C 4直链亚烷基，或是2-羟基 - 正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯; R1是氢，氟，氯，溴，三氟甲基，硝基，氨基，C1-C3烷基氨基，C1-C3二烷基氨基，C1-C3烷基，C1-C3烷硫基，羟基，C1-C3烷氧基或苯基C1-C3烷氧基; R2是氢，氯，溴，羟基，C1-C3烷氧基苯基C1-C3烷氧基或C1-C3烷基，或与R1一起可以是C1-C2亚烷基二氧基; R 3和R 4各自独立地选自氢，氟，氯，溴，C 1 -C 3烷基，羟基，C 1 -C 3烷氧基，硝基，氨基，C 1 -C 3烷基氨基或C 1 -C 3二烷基氨基，或一起可以是亚甲二氧基; 并且R 5是氢，C 3 -C 5烯基，C 1 -C 3烷基或苯基C 1 -C 3烷基，以及其无毒的药学上可接受的加成盐，其具有有价值的药理学性质，特别是持久的心率降低效果和降低心脏的O2要求。

10. 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。

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