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111. 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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