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    Pharmaceutically active compounds
    2.
    发明公开
    Pharmaceutically active compounds 失效
    Pharmazutische aktive Verbindungen。

    公开(公告)号：EP0274867A2

    公开(公告)日：1988-07-20

    申请号：EP87310807.0

    申请日：1987-12-09

    申请人： SCHERING CORPORATION

    发明人： Girijavallabhan, Viyyoor Moopil ,  Pinto, Patrick Anthony ,  Ganguly, Ashit Kumar ,  Versace, Richard William

    IPC分类号： C07D233/60 ,  A61K31/415 ,  C07D277/36 ,  C07D257/04 ,  C07D213/70 ,  C07D257/06 ,  C07D213/30 ,  C07D239/54 ,  C07D233/70 ,  C07D233/94 ,  C07D235/06

    CPC分类号： C07D213/30 ,  C07D213/69 ,  C07D213/70 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/90 ,  C07D233/94 ,  C07D235/06 ,  C07D235/26 ,  C07D235/28 ,  C07D239/54 ,  C07D249/08 ,  C07D257/04 ,  C07D257/06 ,  C07D277/36 ,  C07D295/088 ,  C07D307/20 ,  C07D405/06 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D487/04 ,  C07D493/04

    摘要： The disclosed invention is compounds represented by the formula
    and pharmaceutically acceptable acid addition, basic addition and quarternary amine salts thereof and pharmaceutically acceptable solvates thereof, wherein
    each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile. nitro, phenyslsulfonyl, loweralkylsulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining members of the ring being at least one carbon, and optionally sulfur or oxygen, wherein the substituents are one or more of carboxyl, hydroxymethyl, lower alkyl, loweralkylcarbonyl or aryl lower alkyl;

    X and Y are each independently a bond, -0-,
    each Q is independently a divalent substituted or unsubstituted, straigh or branched chain lower alkanediyl, lower alkanediyl-cycloalkaneidyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofurandiyl, tetrahydrofurandiyl, tetrahydropyrandiyl, or, loweralkanediyl-tetrahydrofurandiyl-loweralkanediyl, wherein the substituents are one or more of hydroxy, epoxy, fluorine, chlorine, azide, or amino; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring containing from 4 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom and the remaining ring atoms being at least one carbon and optionally sulfur or oxygen, wherein the substituents are one or more of hydroxy, oxo amino, carbamoyl, carboxyl, nitrile, nitro, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxyloweralkyl; with the proviso that W cannot be substituted or unsubstituted isoxazolyl, and
    W' is divalent W.

    The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.

    摘要翻译： 所公开的发明是由式表示的化合物及其药学上可接受的酸加成，碱加成和季胺盐及其药学上可接受的溶剂化物，其中每个Z独立地为丁基，苯基，萘基或金刚烷基; 取代的苯基，其中取代基是卤素，低级烷氧基，苯氧基，腈，硝基，苯基磺酰基，低级烷基磺酰基，恶唑-2-基，低级烷酰基，苯甲酰基，低级烷氧基羰基，低级烷基，低级烷硫基，苯基，苯基氨基硫代羰基， 或低级烷基氨基硫代羰基; 含有至少一个氮的4或6元未取代或取代的杂环，其余的成员为至少一个碳，以及任选的硫或氧，其中取代基是羧基，羟甲基，低级烷基，低级烷基羰基或 芳基低级烷基; X和Y各自独立地为键，-O-，各Q独立地为二价取代或未取代的，直链或支链的低级烷二基，低级烷二基 - 环烷烃基 - 低级烷二基，低级烯二基，低级炔二基，亚苯基，二氢呋喃二基 ，四氢呋喃基，四氢吡喃基或低级烷二基 - 四氢呋喃二基 - 低级烷二基，其中取代基是羟基，环氧基，氟，氯，叠氮化物或氨基中的一个或多个; W是单价取代或未取代的芳基或含有4至10个环原子的杂环单或稠环，其至少一个杂原子是氮原子，剩余的环原子是至少一个碳和任选的硫或氧 其中取代基是羟基，氧代氨基，氨基甲酰基，羧基，腈，硝基，低级烷氧基羰基，卤素，氨基磺酰基，低级烷基，低级烷硫基，低级烷氧基，羟基低级烷基，低级烷氧羰基低级烷基，氨基低级烷基，羧基低级烷基，胍基 ，硫脲基，低级烷基磺酰基氨基，氨基羰基低级烷基，烯丙氧基羰基甲基或氨基甲酰氧基低级烷基; 条件是W不能是取代或未取代的异恶唑基，W'是二价的W.该化合物具有抗病毒活性，抗炎活性，是PAF抑制剂。

    Pharmaceutically active compounds
    10.
    发明公开
    Pharmaceutically active compounds 失效
    药物活性化合物

    公开(公告)号：EP0274867A3

    公开(公告)日：1990-11-14

    申请号：EP87310807.0

    申请日：1987-12-09

    申请人： SCHERING CORPORATION

    发明人： Girijavallabhan, Viyyoor Moopil ,  Pinto, Patrick Anthony ,  Ganguly, Ashit Kumar ,  Versace, Richard William

    IPC分类号： C07D233/60 ,  A61K31/415 ,  C07D277/36 ,  C07D257/04 ,  C07D213/70 ,  C07D257/06 ,  C07D213/30 ,  C07D239/54 ,  C07D233/70 ,  C07D233/94 ,  C07D235/06

    CPC分类号： C07D213/30 ,  C07D213/69 ,  C07D213/70 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/90 ,  C07D233/94 ,  C07D235/06 ,  C07D235/26 ,  C07D235/28 ,  C07D239/54 ,  C07D249/08 ,  C07D257/04 ,  C07D257/06 ,  C07D277/36 ,  C07D295/088 ,  C07D307/20 ,  C07D405/06 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D487/04 ,  C07D493/04

    摘要： The disclosed invention is compounds represented by the formula
    and pharmaceutically acceptable acid addition, basic addition and quarternary amine salts thereof and pharmaceutically acceptable solvates thereof, wherein
    each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile. nitro, phenyslsulfonyl, loweralkylsulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining members of the ring being at least one carbon, and optionally sulfur or oxygen, wherein the substituents are one or more of carboxyl, hydroxymethyl, lower alkyl, loweralkylcarbonyl or aryl lower alkyl;
    X and Y are each independently a bond, -0-,
    each Q is independently a divalent substituted or unsubstituted, straigh or branched chain lower alkanediyl, lower alkanediyl-cycloalkaneidyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofurandiyl, tetrahydrofurandiyl, tetrahydropyrandiyl, or, loweralkanediyl-tetrahydrofurandiyl-loweralkanediyl, wherein the substituents are one or more of hydroxy, epoxy, fluorine, chlorine, azide, or amino; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring containing from 4 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom and the remaining ring atoms being at least one carbon and optionally sulfur or oxygen, wherein the substituents are one or more of hydroxy, oxo amino, carbamoyl, carboxyl, nitrile, nitro, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxyloweralkyl; with the proviso that W cannot be substituted or unsubstituted isoxazolyl, and W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.