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    Imidazolidine derivatives as immunosuppressives
    3.
    发明授权
    Imidazolidine derivatives as immunosuppressives 失效
    咪唑烷衍生物作为免疫抑制剂

    公开(公告)号：US4996219A

    公开(公告)日：1991-02-26

    申请号：US448129

    申请日：1989-12-13

    申请人： Christos Tsaklakidis ,  Elmar Bosies ,  Michael Schultz ,  Rainer Haag ,  Dieter Herrmann ,  Wulf Pahlke

    发明人： Christos Tsaklakidis ,  Elmar Bosies ,  Michael Schultz ,  Rainer Haag ,  Dieter Herrmann ,  Wulf Pahlke

    IPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/4427 ,  A61P37/06 ,  C07D233/96 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D233/96 ,  C07D405/06 ,  C07D409/06

    摘要： The present invention provides compounds of the general formulae: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or C.sub.1 -C.sub.5 -alkyl radicals, C.sub.3 -C.sub.5 -alkenyl radicals or phenyl radicals or, together with the carbon atom to which they are attached, form a saturated or unsaturated C.sub.3 -C.sub.7 ring, R.sub.3 and R.sub.4, which can be the same or different, are hydrogen atoms, straight-chained or branched C.sub.1 -C.sub.10 -alkyl radicals, straight-chained or branched C.sub.3 -C.sub.7 -alkenyl radicals, C.sub.3 -C.sub.7 -cycloalkyl radicals, C.sub.3 -C.sub.7 -cycloalkenyl radicals, phenyl, arylalkyl or hetarylalkyl radicals, R.sub.5 is a hydrogen atom or a lower alkyl radical and X is an oxygen or sulphur atom or an imino group.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions with immunosuppressive action containing them.

    摘要翻译： 本发明提供以下通式的化合物：其中R 1和R 2可相同或不同，为氢原子或C 1 -C 5 - 烷基，C 3 -C 5 - 烯基或苯基，或与 它们连接的碳原子形成饱和或不饱和的C 3 -C 7环，可以相同或不同的R 3和R 4是氢原子，直链或支链C 1 -C 10 - 烷基，直链 或支链C 3 -C 7 - 烯基，C 3 -C 7环烷基，C 3 -C 7 - 环烯基，苯基，芳烷基或杂芳基烷基，R 5是氢原子或低级烷基，X是氧或硫原子或 亚氨基组。 本发明还提供了制备这些化合物的方法，以及含有它们的具有免疫抑制作用的药物组合物。

    Phospholipid compound
    5.
    发明授权
    Phospholipid compound 失效

    公开(公告)号：US4492659A

    公开(公告)日：1985-01-08

    申请号：US395954

    申请日：1982-07-07

    申请人： Elmar Bosies ,  Rudi Gall ,  Gunter Weimann ,  Uwe Bicker ,  Wulf Pahlke

    发明人： Elmar Bosies ,  Rudi Gall ,  Gunter Weimann ,  Uwe Bicker ,  Wulf Pahlke

    IPC分类号： A61K31/66 ,  A61P35/00 ,  C07F9/09 ,  C07F9/10 ,  C07F9/02

    CPC分类号： C07F9/10 ,  C07F9/091

    摘要： The present invention provides phospholipids of the general formula: ##STR1## wherein X is a valency bond, an oxygen or sulphur atom or a sulfonyl, sulfinyl, phenylene, cycloaklylene, carbonylamino, aminocarbonyl, ureido or carbonyl group, R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, carbalkoxy or phenyl, R.sub.2 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulphinyl, alkanesulphonyl, carbalkoxy or phenyl, Y is an oxygen atom or a --O--CO--O--, --O--CO--NH-- or --O--CS--NH-- group, R.sub.3 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, which can also be part of a cycloalkane ring system and is optionally substituted one or more times by hydroxyl, halogen, alkylthio, alkanesulphinyl, alkanesulfonyl, nitrile, alkoxycarbonyl, carboxamido optionally substituted by alkyl radicals, cycoalkyl, optionally substituted phenyl or alkoxy, which in turn is optionally substituted by phenyl, hydroxyl, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, optionally acylated amino, alkoxycarbonyl, nitrile or carboxamido optionally substituted by alkyl radicals, Z is an oxygen or sulfur atom, R.sub.4 is a straight-chained or branched alkylene radical containing 2 to 5 carbon atoms and R.sub.5 is a hydrogen atom or a lower alkyl radical, with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together represent an unsubstituted, straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon chain containing up to 18 carbon atoms, Y, R.sub.4 and R.sub.5 have the above-given meanings and Z is an oxygen atom, R.sub.3 cannot be a propylene or 2-methylpropylene chain optionally substituted by hydroxyl, alkoxy or benzyloxy and with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together signify an alkyl radical containing up to 18 carbon atoms and substituted by halogen or phenyl, Y and Z are oxygen atoms and R.sub.4 and R.sub.5 have the above-given meanings, R.sub.3 cannot be a propylene or 2-hydroxypropylene chain; and the pharmacologically acceptable salts thereof.The invention also provides pharmaceutical compositions containing such compounds, having cancerostatic action without inducing thrombocyte aggregation.