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11 条记录 (耗时 0.031 秒)

    Diaminocyclobutene-3,4-diones
    5.
    发明授权
    Diaminocyclobutene-3,4-diones 失效
    二氨基环丁烯-3,4-二酮

    公开(公告)号：US5512585A

    公开(公告)日：1996-04-30

    申请号：US459598

    申请日：1995-06-02

    申请人： Madelene M. Antane ,  John A. Butera ,  Bradford H. Hirth ,  Schuyler A. Antane

    发明人： Madelene M. Antane ,  John A. Butera ,  Bradford H. Hirth ,  Schuyler A. Antane

    IPC分类号： C07C233/41 ,  C07C255/60 ,  C07C271/28 ,  C07C311/08 ,  C07D213/75 ,  C07D217/02 ,  A61K31/44 ,  C07D213/36

    CPC分类号： C07D213/75 ,  C07C233/41 ,  C07C255/60 ,  C07C271/28 ,  C07C311/08 ,  C07D217/02 ,  C07C2101/04 ,  C07C2101/14 ,  C07C2102/42

    摘要： The compound of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independent from each other, hydrogen, C.sub.1-10 straight chain alkyl, C.sub.1-10 branched alkyl, or C.sub.3-10 cyclic or bicyclic alkyl;R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl of 2 to 7 carbon atoms, alkenoyl of 3 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms;A is selected from the group consisting of: ##STR2## wherein: R.sub.4 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkoxy, C.sub.1-6 perfluoroalkoxy, amino, C.sub.1-6 alkylamino, C.sub.2-12 dialkylamino, C.sub.1-6 alkylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, nitro, cyano or carboxyl;or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

    摘要翻译： 下式的化合物：其中：R 1和R 2彼此独立地为氢，C 1-10直链烷基，C 1-10支链烷基或C 3-10环状或双环烷基; R3是选自甲酰基，2至7个碳原子的烷酰基，3至7个碳原子的烯酰基，1至7个碳原子的烷基磺酰基，7至12个碳原子的芳酰基，9至20个芳基烯酰基 6至12个碳原子的芳基磺酰基，8至12个碳原子的芳基烷酰基或7至12个碳原子的芳烷基磺酰基; A选自：其中：R4是氢，C1-6烷基，C1-6全氟烷基，C1-6烷氧基，C1-6全氟烷氧基，氨基，C1-6烷基氨基，C2-12二烷基氨基， 含有2-7个碳原子的C 1-6烷基磺酰氨基，烷基羧酰胺基，硝基，氰基或羧基; 或其药学上可接受的盐是平滑肌松弛剂。

    Substituted N-arylmethylamino derivatives of cyclobutene-3,4-diones
    6.
    发明授权
    Substituted N-arylmethylamino derivatives of cyclobutene-3,4-diones 失效
    取代的环丁烯-3,4-二酮的N-芳基甲基氨基衍生物

    公开(公告)号：US5763474A

    公开(公告)日：1998-06-09

    申请号：US889164

    申请日：1997-07-07

    申请人： David R. Herbst ,  Madelene M. Antane ,  Geraldine R. McFarlane ,  Eric G. Gundersen ,  Bradford H. Hirth ,  Dominick A. Quagliato ,  Russell F. Graceffa ,  John A. Butera

    发明人： David R. Herbst ,  Madelene M. Antane ,  Geraldine R. McFarlane ,  Eric G. Gundersen ,  Bradford H. Hirth ,  Dominick A. Quagliato ,  Russell F. Graceffa ,  John A. Butera

    IPC分类号： C07C225/20 ,  C07C233/41 ,  C07C255/58 ,  C07C271/24 ,  A61K31/135 ,  A61K31/165 ,  C07C235/82

    CPC分类号： C07C225/20 ,  C07C233/41 ,  C07C255/58 ,  C07C271/24 ,  C07C2101/04 ,  C07C2101/08

    摘要： The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 and R.sub.5 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, fluoroalkyl, alkoxy, perfluoroalkoxy, fluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen, with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen; or a pharmaceutically acceptable salt thereof, relaxes smooth muscles.

    摘要翻译： 下式的化合物：其中R 1是直链烷基，支链烷基环烷基，羟基烷基，氟烷基或多氟烷基; R2和R3独立地为氢或选自甲酰基，烷酰基，烯酰基，烷氧基羰基，烷基磺酰基，芳酰基，芳基烯酰基，芳基磺酰基，芳基烷酰基或芳基烷基磺酰基的酰基取代基。 A是下式的取代苯基：其中R 4和R 5独立地是氰基，硝基，氨基，烷基，全氟烷基，氟烷基，烷氧基，全氟烷氧基，氟烷氧基，氨基，烷基氨基，二烷基氨基，氨基磺酰基，烷基亚磺酰氨基， 芳基亚磺酰氨基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，烷基酰胺基，芳基羧酰氨基，烷基磺酰基，全氟烷基磺酰基，芳基磺酰基，氯，溴，氟，碘，1-咪唑基，羧基或氢，条件是R4和R5不能都是氢; 或其药学上可接受的盐，使平滑肌松弛。

    Substituted N-arylmethylamino derivatives of cyclobutene-3, 4-diones
    8.
    发明授权
    Substituted N-arylmethylamino derivatives of cyclobutene-3, 4-diones 失效
    取代的环丁基-3,4-二酮的N-芳基甲基氨基衍生物

    公开(公告)号：US5780505A

    公开(公告)日：1998-07-14

    申请号：US889166

    申请日：1997-07-07

    申请人： Madelene M. Antane ,  David R. Herbst ,  Geraldine R. McFarlane ,  Eric G. Gundersen ,  Bradford H. Hirth ,  Dominick A. Quagliato ,  Russell F. Graceffa ,  John A. Butera

    发明人： Madelene M. Antane ,  David R. Herbst ,  Geraldine R. McFarlane ,  Eric G. Gundersen ,  Bradford H. Hirth ,  Dominick A. Quagliato ,  Russell F. Graceffa ,  John A. Butera

    IPC分类号： C07C225/20 ,  C07C233/41 ,  C07C255/58 ,  C07C271/24 ,  A61K31/275

    CPC分类号： C07C255/58 ,  C07C225/20 ,  C07C233/41 ,  C07C271/24 ,  C07C2101/04 ,  C07C2101/08

    摘要： The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.6 is methyl, fluoro, chloro, or methoxy; or a pharmaceutically acceptable salt thereof, relax smooth muscles.

    摘要翻译： 下式的化合物：其中R 1是直链烷基，支链烷基，环烷基，羟基烷基，氟烷基或多氟烷基; R 7和R 8独立地是氢或选自甲酰基，烷酰基，烯酰基，烷氧基羰基，烷基磺酰基，芳酰基，芳基烯酰基，芳基磺酰基，芳基烷酰基或芳基烷基磺酰基的酰基取代基。 A是具有下式的两个或三个取代基的苯基：其中取代的位置是R2，R3-，R2，R4-，R2，R5-，R2，R6-，R3，R4-， R 3，R 5和R 2，R 4，R 6和R 2是甲基，乙基，氟，氯，甲氧基或三氟甲基; R3是甲基，乙基，氟，氯，甲氧基或三氟甲基; R4是甲基，氟，溴，甲氧基或氰基; R5是甲基，氟，氯，甲氧基，氰基或三氟甲基; R6是甲基，氟，氯或甲氧基; 或其药学上可接受的盐，使平滑肌松弛。