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1. 发明授权

US5068325A 4,5,7,8-tetrahydro-6H-thiazolo[5,4-d]azepines, their preparation and their use as pharmaceutical compositions 失效
标题翻译： 4,5,7,8-四氢-6H-噻唑（5,4-D）亚胺，其制备及其作为药物组合物的用途
公开(公告)号：US5068325A
公开(公告)日：1991-11-26
申请号：US368753
申请日：1989-06-20
申请人： Wolfgang Grell , Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Ludwig Pichler , Walter Kobinger , Michael Entzeroth , Joachim Mierau , Gunter Schingnitz
发明人： Wolfgang Grell , Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Ludwig Pichler , Walter Kobinger , Michael Entzeroth , Joachim Mierau , Gunter Schingnitz
IPC分类号： A61K31/55 , A61P9/00 , A61P25/00 , C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to new 4,5,7,8-tetrahydro-6H-thiazolo[5,4-d]azepines of general formula II ##STR1## wherein the substituents are defined herein below, which compounds have valuable pharmacological properties, namely selective effects on the dopaminergic system which are achieved by stimulating (predominantly D2) dopamine receptors.
摘要翻译：本发明涉及通式II（II）的新的4,5,7,8-四氢-6H-噻唑并[5,4-d]吖庚因，其中取代基如下文所定义，该化合物具有有价值的药理学性质，即通过刺激（主要是D2）多巴胺受体而实现的对多巴胺能系统的选择性作用。

2. 发明授权

US4843086A Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
标题翻译：四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途
公开(公告)号：US4843086A
公开(公告)日：1989-06-27
申请号：US124197
申请日：1987-11-23
申请人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D277/82
摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms.R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核可各自被1或2个卤素原子取代。 R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而苯基核可以被氟取代，氯或溴原子，R4表示氢原子，烷基，烷基或烯基或R3和R4以及它们之间的氮原子表示吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，对映体和酸加成的盐。上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。新化合物可以使用本身已知的方法制备。

3. 发明授权

US4886812A Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
标题翻译：四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途
公开(公告)号：US4886812A
公开(公告)日：1989-12-12
申请号：US256671
申请日：1988-10-12
申请人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D277/82
摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nucleic may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核酸可各自被1或2个卤素原子取代，R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基基团可以被氟，氯或溴原子取代，R4表示氢原子，烷基，烷基或烯基，或者R3和R4与它们之间的氮原子一起代表吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，其对映异构体及其酸加成盐。上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。新化合物可以使用本身已知的方法制备。

4. 发明授权

US4731374A Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
标题翻译：四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途
公开(公告)号：US4731374A
公开(公告)日：1988-03-15
申请号：US810947
申请日：1985-12-19
申请人： Gerhart Griss, deceased , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D277/82
摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核可各自被1或2个卤素原子取代，R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基基团可以被氟里酰，氯或溴原子取代，R4表示氢原子，烷基，烷基或烯基，或者R3和R4与它们之间的氮原子一起代表吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，其对映异构体及其酸加成盐。上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。新化合物可以使用本身已知的方法制备。

5. 发明授权

US4486433A Fused-ring amino-pyrazines as bradycardiacs 失效
标题翻译：融合环氨基吡嗪作为心动过缓
公开(公告)号：US4486433A
公开(公告)日：1984-12-04
申请号：US501437
申请日：1983-06-06
申请人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
发明人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
IPC分类号： A61K31/495 , A61K31/55 , A61P9/02 , A61P9/06 , A61P9/12 , A61P25/02 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;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和B可以相同或不同，各自表示亚甲基，（1至3个碳原子的烷基） - 亚甲基，亚乙基或（1至3个碳原子的烷基） - 亚乙基; R 1是氢，1至6个碳原子的烷基，3至7个碳原子的环烷基，3至6个碳原子的烯基，苯基 - （1至3个碳原子的烷基），卤代苯基 - （1至3个碳原子的烷基），1〜3个碳原子的烷酰基，1〜3个碳原子的苯基 - （烷酰基），1〜3个碳原子的卤代苯基 - （烷酰基），2〜4个碳原子的烷氧基羰基，8〜10个碳原子的芳烷氧羰基，苯基; R2和R3中的一个是氨基，另一个是氢，氯，溴，1至3个碳原子的烷基，1至3个碳原子的烷氧基，2至4个碳原子的烷氧基羰基，苯基或卤代苯基; 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。

6. 发明授权

US4409220A Fused-ring amino-pyrazines as bradycardiac agents 失效
标题翻译：稠环氨基吡嗪作为心动过缓剂
公开(公告)号：US4409220A
公开(公告)日：1983-10-11
申请号：US297024
申请日：1981-08-27
申请人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
发明人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
IPC分类号： A61K31/495 , A61K31/55 , A61P9/02 , A61P9/06 , A61P9/12 , A61P25/02 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;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和B可以相同或不同，各自表示亚甲基，（1至3个碳原子的烷基） - 亚甲基，亚乙基或（1至3个碳原子的烷基） - 亚乙基; R 1是氢，1至6个碳原子的烷基，3至7个碳原子的环烷基，3至6个碳原子的烯基，苯基 - （1至3个碳原子的烷基），卤代苯基 - （1至3个碳原子的烷基），1〜3个碳原子的烷酰基，1〜3个碳原子的苯基 - （烷酰基），1〜3个碳原子的卤代苯基 - （烷酰基），2〜4个碳原子的烷氧基羰基，8〜10个碳原子的芳烷氧羰基，苯基; R2和R3中的一个是氨基，另一个是氢，氯，溴，1至3个碳原子的烷基，1至3个碳原子的烷氧基，2至4个碳原子的烷氧基羰基，苯基或卤代苯基; 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

US4575504A Thienothiazole derivatives 失效
标题翻译：噻吩噻唑衍生物
公开(公告)号：US4575504A
公开(公告)日：1986-03-11
申请号：US649898
申请日：1984-09-12
申请人： Robert Sauter , Gerhart Griss, deceased , Wolfgang Grell , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler
发明人： Robert Sauter , Gerhart Griss, deceased , Wolfgang Grell , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler
IPC分类号： A61K31/435 , A61K31/55 , A61P9/06 , C07D495/04 , C07D513/14 , A61K31/44
CPC分类号： C07D495/04 , C07D513/14
摘要： Compounds of the formula ##STR1## wherein A is ##STR2## and R is hydrogen, alkyl of 1 to 5 carbon atoms, alkanoyl of 1 to 5 carbon atoms, alkenyl of 3 to 5 carbon atoms, (alkoxy of 1 to 4 carbon atoms)carbonyl, or aralkyl of 7 to 11 carbon atoms optionally halo-substituted,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为X，R为氢，1至5个碳原子的烷基，1至5个碳原子的烷酰基，3至5个碳原子的烯基，（1至4个碳原子的烷氧基））羰基或任选被卤素取代的7至11个碳原子的芳烷基，以及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。

8. 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。

9. 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。

10. 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。

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