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16 条记录 (耗时 0.021 秒)

    Tetracyclic quinazoline derivatives, effective as antiarrythmic agents
    1.
    发明授权
    Tetracyclic quinazoline derivatives, effective as antiarrythmic agents 失效
    作为抗菌药物有效的四环喹诺酮衍生物

    公开(公告)号：US5214047A

    公开(公告)日：1993-05-25

    申请号：US243469

    申请日：1988-09-12

    申请人： Bernd Ostersehlt ,  Rainer Schlecker ,  Beatrice Rendenbach ,  Gerda von Philipsborn ,  Albrecht Franke, deceased

    发明人： Bernd Ostersehlt ,  Rainer Schlecker ,  Beatrice Rendenbach ,  Gerda von Philipsborn ,  Albrecht Franke, deceased

    IPC分类号： A61K31/505 ,  A61P9/06 ,  C07D471/14 ,  C07D487/14

    CPC分类号： C07D471/14 ,  C07D487/14

    摘要： A tetracyclic quinazoline derivative of the formula I: ##STR1## wherein A is C.sub.2-3 -alkylene or C.sub.2-3 -alkylene which is substituted by one or two C.sub.1-4 -alkyl radicals or A is cyclohexylene; X is phenyl, naphthyl or phenyl or naphthyl which is substituted by halogen, nitro, amino, C.sub.1-4 -alkylamino, sulfonylamino, C.sub.1-4 -acylamino, hydroxyl, C.sub.1-4 -alkoxy, --O--(CH.sub.2).sub.2-4 --NR.sup.1 R.sup.2, C.sub.1-4 -alkyl or C.sub.1-4 -alkylsulfonyl, wherein R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 -alkyl; or X is thienyl or thienyl which is substituted by chlorine, fluorine, methyl, ethyl, methoxy, ethoxy, nitro or hydroxyl; and R is hydrogen, halogen, nitro, amino, C.sub.1-4 -alkylamino, sulfonylamino, C.sub.1-4 -acylamino, hydroxyl, C.sub.1-4 -alkoxy, --O--(CH.sub.2).sub.2-4 --NR.sup.3 R.sup.4, C.sub.1-4 -alkyl or C.sub.1-4 -alkylsulfonyl, wherein R.sup.3 and R.sup.4 are each hydrogen or C.sub.1-4 -alkyl, and the pharmaceutically acceptable salts thereof. The compounds and compositions of the present invention are effective as antiarrhythmic agents.

    摘要翻译： 式I的四环喹唑啉衍生物：其中A是被一个或两个C 1-4 - 烷基取代的C 2-3亚烷基或C 2-3亚烷基，或者A是亚环己基; X是被卤素，硝基，氨基，C 1-4 - 烷基氨基，磺酰基氨基，C 1-4 - 酰氨基，羟基，C 1-4 - 烷氧基，-O-（CH 2）2-4取代的苯基，萘基或苯基或萘基 -NR 1 R 2，C 1-4 - 烷基或C 1-4 - 烷基磺酰基，其中R 1和R 2各自为氢或C 1-4 - 烷基; 或X是被氯，氟，甲基，乙基，甲氧基，乙氧基，硝基或羟基取代的噻吩基或噻吩基; 并且R是氢，卤素，硝基，氨基，C 1-4 - 烷基氨基，磺酰基氨基，C 1-4 - 酰氨基，羟基，C 1-4 - 烷氧基，-O-（CH 2）2-4 -NR 3 R 4，C 1-4 - 烷基 或C 1-4 - 烷基磺酰基，其中R 3和R 4各自为氢或C 1-4 - 烷基，及其药学上可接受的盐。 本发明的化合物和组合物作为抗心律失常药有效。

    p-Hydroxy phenone derivatives and the use thereof
    3.
    发明授权
    p-Hydroxy phenone derivatives and the use thereof 失效
    P-羟基苯酮衍生物及其用途

    公开(公告)号：US5118682A

    公开(公告)日：1992-06-02

    申请号：US378966

    申请日：1989-07-12

    申请人： Wilfried Lubisch ,  Manfred Raschack ,  Gerda von Philipsborn

    发明人： Wilfried Lubisch ,  Manfred Raschack ,  Gerda von Philipsborn

    IPC分类号： A61K31/135 ,  A61K31/40 ,  A61K31/445 ,  A61P9/06 ,  C07C217/22 ,  C07D295/08 ,  C07D295/092

    CPC分类号： C07D295/088 ,  C07C217/22

    摘要： p-Hydroxy phenone derivatives of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are identical or different and are methyl, chlorine, bromine and hydrogen, but R.sup.1, R.sup.2 and R.sup.3 are not all H,R.sup.4 and R.sup.5 are identical or different and are H, C.sub.1 -C.sub.4 -alkyl, or OR.sup.6, but R.sup.4 and R.sup.5 are not both H,X is a --CH.dbd.CH--, --CH.sub.2 CH.sub.2 or --CH.sub.2 -- bridge,Y is a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.4 bridge, andZ is NR.sup.6 R.sup.7, where R.sup.6 and R.sup.7 are, independently of one another, hydrogen or C.sub.1-4 -alkyl, or Z is a 5- or 6-membered ring with a nitrogen atom in the 1 position and, where appropriate, additionally a second N atom or an O or S atom, the second N atom being substituted by R.sup.7, as well as the physiologically tolerated salts thereof,are used to prepare drugs antiarrhythmic of Vaughan-Williams class III.

    摘要翻译： 通式I的对羟基苯酮衍生物其中R 1，R 2和R 3相同或不同，为甲基，氯，溴和氢，但R 1，R 2和R 3不全为H，R 4和R 5相同 或不同的是H，C 1 -C 4烷基或OR 6，但R 4和R 5不同时为H，X为-CH = CH-，-CH 2 CH 2或-CH 2 - 桥，Y为直链或支链， 饱和或不饱和的C 1 -C 4桥，Z为NR 6 R 7，其中R 6和R 7彼此独立地为氢或C 1-4 - 烷基，或Z为在1位上具有氮原子的5-或6-元环 位置，并且在适当的情况下另外还有第二个N原子或O或S原子，被R7取代的第二个N原子及其生理上耐受的盐用于制备Vaughan-Williams III类抗心律不齐药物。

    Substituted anilides
    5.
    发明授权
    Substituted anilides 失效
    取代的酰苯胺

    公开(公告)号：US5260330A

    公开(公告)日：1993-11-09

    申请号：US790869

    申请日：1991-11-12

    申请人： Wilfried Lubisch ,  Gerda von Philipsborn ,  Sabine Schult ,  Michael Kirchengast

    发明人： Wilfried Lubisch ,  Gerda von Philipsborn ,  Sabine Schult ,  Michael Kirchengast

    IPC分类号： A61K31/165 ,  A61K31/00 ,  A61K31/167 ,  A61K31/40 ,  A61K31/445 ,  A61K31/4453 ,  A61P9/00 ,  A61P9/06 ,  C07C233/29 ,  C07C235/38 ,  C07D295/08 ,  C07D295/092 ,  C07D202/05

    CPC分类号： C07D295/088 ,  C07C233/29

    摘要： Substituted anilides of the formula I ##STR1## (where R.sup.1 is C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, cyano, nitro, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl;X is methylene, ethylene, vinylene;R.sup.2 and R.sup.3 are each C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl or together are tetra- or pentamethylene;R.sup.4 is C.sub.1 -C.sub.4 -alkyl, methoxy;n is 2, 3 or 4),and the physiologically tolerated acid addition salts thereof, the pharmaceutical use thereof, drugs produced therefrom and the use thereof for treating cardiac arrhythmias and/or for lowering the heart rate, are described.

    摘要翻译： 取代的式I的酰苯胺（其中R 1是C 1 -C 4 - 烷基，C 1 -C 4卤代烷基，C 1 -C 4 - 烷氧基，卤素，氰基，硝基，C 2 -C 4 - 烯基，C 2 -C 4 - 炔基; X是亚甲基，亚乙基，亚乙烯基; R 2和R 3各自是C 1 -C 4烷基，C 3 -C 6环烷基或一起是四或五亚甲基; R 4是C 1 -C 4 - 烷基，甲氧基; n是2,3或4） 及其生理上耐受的酸加成盐，其药学用途，由其制备的药物及其用于治疗心律失常和/或用于降低心率的用途。

    Bispidine derivatives as class III antiarrhythmic agents
    8.
    发明授权
    Bispidine derivatives as class III antiarrhythmic agents 失效
    双膦衍生物作为III类抗心律失常药

    公开(公告)号：US4959373A

    公开(公告)日：1990-09-25

    申请号：US247645

    申请日：1988-09-22

    申请人： Wilfried Lubisch ,  Fritz Binnig ,  Gerda von Philipsborn

    发明人： Wilfried Lubisch ,  Fritz Binnig ,  Gerda von Philipsborn

    IPC分类号： A61K31/44 ,  A61P9/06 ,  C07D471/08

    CPC分类号： C07D471/08

    摘要： Bispidine derivatives of the formula I ##STR1## where R, R.sup.1 and R.sup.3 are identical or different and are each H, C.sub.1 -C.sub.4 -alkyl, halogen or C.sub.1 -C.sub.4 -alkoxy, when Y is ##STR2## R.sup.2 is C.sub.1 -C.sub.4 -alkyl, halogen, --CN, C.sub.1 -C.sub.4 -alkoxy, --NHSO.sub.2 CH.sub.3, --CF.sub.3, NH-acetyl or --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are each C.sub.1 -C.sub.4 -alkyl, when Y is ##STR3## R.sup.2 is C.sub.1 -C.sub.4 -alkyl, halogen, --CN.sub.1 C.sub.1 -C.sub.4 -alkoxy, --NHSO.sub.2 CH.sub.3, --CF.sub.3, NH-acetyl or --NR.sup.9 R.sup.10 where R.sup.9 is C.sub.1 -C.sub.4 -alkyl and R.sup.10 is H or C.sub.1 -C.sub.4 -alkyl, and when X is not CH.sub.2 R.sub.2 may also be NO.sub.2 or NH.sub.2, X is --CH.sub.2 --, --C(O)-- or --C(R.sup.6)OR.sup.7 -- (where R.sup.6 is H or C.sub.1 -C.sub.4 -alkyl and R.sup.7 is H, C.sub.1 -C.sub.4 -alkyl or ##STR4## where R.sup.8 is H, C.sub.1 -C.sub.4 -alkyl, halogen or C.sub.1 -C.sub.4 -alkoxy), Y is --C(O) or --CONH-- and Z is C.sub.1 -C.sub.4 -alkylene which may be olefinically unsaturated and/or branched, and their physiologically tolerated salts, and drugs containing these compounds as active compounds are described.

    摘要翻译： 其中R，R 1和R 3相同或不同，并且各自为H，C 1 -C 4 - 烷基，卤素或C 1 -C 4 - 烷氧基时，当Y为C 1 -C 4 - 烷基，卤素，-CN，C 1 -C 4 - 烷氧基，-NHSO 2 CH 3，-CF 3，NH-乙酰基或-NR 4 R 5，其中R 4和R 5各自为C 1 -C 4 - 烷基，当Y为C 1 -C 4 - 烷基，卤素，-CN1C1-C4-烷氧基，-NHSO2CH3，-CF3，NH-乙酰基或-NR9R10，其中R9为C1-C4-烷基，R10为H或C1-C4-烷基，当X不为CH2R2时 也可以是NO 2或NH 2，X是-CH 2 - ， - C（O） - 或-C（R 6）OR 7 - （其中R 6是H或C 1 -C 4烷基，且R 7是H，C 1 -C 4烷基或