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    Cinnamide derivatives as KCNQ potassium channel modulators
    7.
    发明授权
    Cinnamide derivatives as KCNQ potassium channel modulators 有权
    桂酰胺衍生物作为KCNQ钾通道调节剂

    公开(公告)号：US06831080B2

    公开(公告)日：2004-12-14

    申请号：US10160582

    申请日：2002-05-31

    申请人： Yong-Jin Wu ,  Li-Quang Sun ,  Jie Chen ,  Huan He ,  Alexandre L'Heureux ,  Pierre Dextraze ,  Jean-Paul Daris ,  Gene G. Kinney ,  Steven I. Dworetzky ,  Piyasena Hewawasam

    发明人： Yong-Jin Wu ,  Li-Quang Sun ,  Jie Chen ,  Huan He ,  Alexandre L'Heureux ,  Pierre Dextraze ,  Jean-Paul Daris ,  Gene G. Kinney ,  Steven I. Dworetzky ,  Piyasena Hewawasam

    IPC分类号： C07C23720

    CPC分类号： C07D213/40 ,  C07C233/11 ,  C07C235/34 ,  C07D209/08 ,  C07D213/56 ,  C07D215/04 ,  C07D215/12 ,  C07D217/06 ,  C07D239/26 ,  C07D241/12 ,  C07D265/30 ,  C07D265/36 ,  C07D295/135 ,  C07D307/79 ,  C07D311/58 ,  C07D317/58 ,  C07D317/60 ,  C07D319/18 ,  C07D333/24 ,  C07D407/12 ,  C07D491/08

    摘要： There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken together are —CH═CH—CH═CH— or —X(CH2)mY— in which X and Y are each independently selected from the group consisting of CH2, (CH2)nN(R9)— and O, wherein m is 1 or 2; n is 0 or 1; and R6, R7, and R8 are each independently selected from hydrogen, chloro and fluoro; and R9 is selected from the group consisting of hydrogen, C1-4 alkyl, hydroxyethyl, C1-4 alkoxyethyl, cyclopropylmethyl, —CO2(C1-4alkyl), and —CH2CH2NR10R11 in which R10 and R11 are each independently hydrogen or C1-4 alkyl, which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.

    摘要翻译： 提供式I的新颖的肉桂酰胺衍生物：其中R是C 1-4烷基或三氟甲基; R 1选自吡啶基，喹啉基，噻吩基，呋喃基，1,4-苯并二恶烷基，1,3-苯并二恶唑基，苯并二氢吡喃基，茚满基，联苯基，苯基和取代的苯基，其中所述取代的苯基被一个 或两个各自独立地选自卤素，C 1-4烷基，C 1-4烷氧基，三氟甲基，三氟甲氧基和硝基的取代基; R 2和R 3各自独立地选自氢，C 1-4烷基和卤素; R 4选自二（C 1-4烷基）氨基，三氟甲氧基和任选取代的吗啉-4-基，吡啶基，嘧啶基，哌嗪基和吡嗪基，其中一个或两个取代基独立地选自所述取代基 由C1-4烷基，氨基甲基，羟甲基，氯或氟组成的基团; R 5是氢，氯或氟; 或R 4和R 5一起为-CH = CH-CH = CH-或-X（CH 2）mY-，其中X和Y各自独立地选自CH 2，（CH 2）n N （R 9） - 和O，其中m为1或2; n为0或1; 和R 6，R 7和R 8各自独立地选自氢，氯和氟; 并且R 9选自氢，C 1-4烷基，羟乙基，C 1-4烷氧基乙基，环丙基甲基，-CO 2（C 1-4烷基）和-CH 2 CH 2 NR 10 R 11， 10>和R 11各自独立地是氢或C 1-4烷基，其是KCNQ钾通道的开放剂，并且可用于治疗对开放KCNQ钾通道有响应的病症。

    Antibiotic C-3 dithioacetal-substituted carbapenem compounds, compositions, and methods of use thereof
    9.
    发明授权
    Antibiotic C-3 dithioacetal-substituted carbapenem compounds, compositions, and methods of use thereof 失效
    抗生素C-3取代替代碳水化合物，组合物及其使用方法

    公开(公告)号：US5116833A

    公开(公告)日：1992-05-26

    申请号：US600359

    申请日：1990-10-19

    申请人： Martel Alain ,  Carol Bachand ,  Jean-Paul Daris

    发明人： Martel Alain ,  Carol Bachand ,  Jean-Paul Daris

    IPC分类号： A61K31/40 ,  A61K31/397 ,  A61P31/04 ,  C07D477/00 ,  C07D477/20

    CPC分类号： C07D477/20

    摘要： A dithioacetal carbapenem of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl;n is 0, 1 or 2;R.sup.3 is hydrogen or C.sub.1-6 alkyl;R.sup.2 isC.sub.1-6 alkyl,phenyl optionally substituted with cyano, --CO.sub.2 NH.sub.2, --CH.sub.2 OH, --CH.sub.2 NH.sub.2, --CONHNH.sub.2 or with up to 5 halogen atoms, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy groups,phenylmethyl optionally substituted with up to 5 halogen atoms, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy groups on the phenyl ring, ora radical represented by the formula--(CH.sub.2).sub.p --X in which p is 0 or 1; X is five-membered aromatic heterocyclic ring containing up to 1 sulfur, 1 oxygen or 4 nitrogen atoms, optionally substituted with a C.sub.1-6 alkyl group, or six-membered aromatic heterocylic ring containing up to 4 nitrogen atoms, optionally substituted with a C.sub.1-6 alkyl group.or a non-toxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.