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    Sulfonates of hydroxycoumarins
    4.
    发明授权
    Sulfonates of hydroxycoumarins 失效
    羟基香豆素磺酸盐

    公开(公告)号：US4618622A

    公开(公告)日：1986-10-21

    申请号：US552787

    申请日：1983-11-17

    申请人： Rainer Schlecker ,  Peter Schmidt ,  Peter C. Thieme ,  Dieter Lenke ,  Hans-Jurgen Teschendorf ,  Martin Traut ,  Claus D. Mueller ,  Hans P. Hofmann ,  Horst Kreiskott

    发明人： Rainer Schlecker ,  Peter Schmidt ,  Peter C. Thieme ,  Dieter Lenke ,  Hans-Jurgen Teschendorf ,  Martin Traut ,  Claus D. Mueller ,  Hans P. Hofmann ,  Horst Kreiskott

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/365 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P37/08 ,  A61P43/00 ,  C07D311/08 ,  C07D311/16 ,  C07D311/80 ,  A61K31/37

    CPC分类号： C07D311/80 ,  C07D311/16

    摘要： Sulfonates of hydroxycoumarins of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and are each hydrogen, halogen or alkyl of 1 to 5 carbon atoms which can be substituted by --NR.sup.4 R.sup.5, --OR.sup.4 or --OC(O)R.sup.4, where R.sup.4 and R.sup.5 are identical or different and are each hydrogen or alkyl of 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 are each a carboxylic acid group --OC(O)R.sup.4 or a carboxamido radical, with the proviso that R.sup.1 is not methyl when R.sup.2 is hydrogen, or R.sup.1 and R.sup.2 together form a --(CH.sub.2).sub.n -- chain where n is 3-5, and R.sup.3 is a straight-chain or branched alkyl radical of 1 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms, each of which can be substituted by halogen, --OR.sup.4, --NR.sup.4 R.sup.5, --CN or phenyl, or R.sup.3 is a straight-chain or branched alkenyl radical of 3 to 8 carbon atoms, an amino group -- NR.sup.4 R.sup.5, or phenyl or naphthyl, each of which is unsubstituted or monosubstituted or polysubstituted by --OR.sup.4, --NR.sup.4 R.sup.5, --NO.sub.2, halogen, --SR.sup.4, --S(O)R.sup.4, --OS(O)R.sup.4, --SCF.sub.3, --OS(O)CF.sub.3, --CN, --C(O)R.sup.4, --OC(O)R.sup.4, --NHC(O)R.sup.4, --CF.sub.3, C.sub.1 -C.sub.4 -alkyl or a combination of these substituents, a process for their preparation, drugs containing these compounds, and compounds of the formula I, in which R.sup.1 is methyl and R.sup.2 is hydrogen, for use as drugs.

    摘要翻译： 式I的羟基香豆素的磺酸盐其中R 1和R 2相同或不同，各自为氢，卤素或可被-NR 4 R 5，-OR 4或-OC（O）取代的1至5个碳原子的烷基 ）R 4，其中R 4和R 5相同或不同并且各自为氢或1至4个碳原子的烷基，或者R 1和R 2各自为羧酸基-OC（O）R 4或甲酰胺基，条件是R 1 当R 2为氢时，R 1和R 2一起形成 - （CH 2）n - 链，其中n为3-5，R 3为1至8个碳原子的直链或支链烷基或3个环烷基 至8个碳原子，每个可以被卤素，-OR4，-NR4R5，-CN或苯基取代，或R3是3-8个碳原子的直链或支链烯基，氨基-NR4R5或 苯基或萘基，它们各自被-OR4，-NR4R5，-NO2，卤素，-SR4，-S（O）R4，-OS（O）R4，-SCF3，-OS（O）未取代或单取代或多取代， CF 3，-CN，-C（O）R 4，-OC（O）R 4， -NHC（O）R 4，-CF 3，C 1 -C 4烷基或这些取代基的组合，其制备方法，含有这些化合物的药物和式I化合物，其中R 1是甲基，R 2是氢， 用作药物。

    9-amino-2-phenylbicyclo[3.3.1]nonanes and 9-amino-2-phenylbicyclo[3.3.1]non-2-enes and drugs containing them
    5.
    发明授权
    9-amino-2-phenylbicyclo[3.3.1]nonanes and 9-amino-2-phenylbicyclo[3.3.1]non-2-enes and drugs containing them 失效
    9-氨基-2-苯基二醇（3.3.1）非氨基和9-氨基-2-苯基二醇（3.3.1）含有它们的非2-烯和药物

    公开(公告)号：US5153228A

    公开(公告)日：1992-10-06

    申请号：US713276

    申请日：1991-06-11

    申请人： Rainer Schlecker ,  Hans P. Hofmann ,  Laszlo Szabo

    发明人： Rainer Schlecker ,  Hans P. Hofmann ,  Laszlo Szabo

    IPC分类号： A61K31/135 ,  A61K31/445 ,  A61P25/00 ,  C07C211/41 ,  C07C215/64 ,  C07C217/54 ,  C07C217/74 ,  C07C317/32 ,  C07C323/31 ,  C07D211/14

    CPC分类号： C07C217/54 ,  C07C211/41 ,  C07D211/14 ,  C07C2102/46

    摘要： 9-Amino-2-phenylbicyclo-[3.3.1]nonanes and 9-amino-2-phenylbicyclo[3.3.1]non-2-enes of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and each is hydrogen, halogen, alkyl, alkoxy, dialkylamino, trifluoromethyl, hydroxyl, alkylthio, alkylsulfonyl or nitro, R.sup.3 and R.sup.4 are identical or different and each is hydrogen, alkyl or 1 to 5 or alkenyl or alkynyl of 2 to 5 carbon atoms, or benzyl, it also being possible for R.sup.3 and R.sup.4 together to form a saturated chain which contains from three to seven carbon atoms and can be substituted by phenyl, and where is a single or double bond, are used for producing drugs which act, in particular, on the central nervous system.

    摘要翻译： 具有式I的9-氨基-2-苯基双环[3.3.1]壬烷和9-氨基-2-苯基双环[3.3.1]壬-2-烯，其中R 1和R 2相同或不同， 烷基，卤素，烷基，烷氧基，二烷基氨基，三氟甲基，羟基，烷硫基，烷基磺酰基或硝基，R 3和R 4相同或不同，各自为氢，烷基或1至5个或2至5个碳原子的烯基或炔基， 苄基，也可以将R3和R4一起形成含有3至7个碳原子并可被苯基取代的饱和链，并且其中是单键或双键，用于生产特别是作用的药物 ，在中枢神经系统。

    Tetracyclic quinazoline derivatives, effective as antiarrythmic agents
    8.
    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。