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    Alkylated rapamycin derivatives
    4.
    发明授权
    Alkylated rapamycin derivatives 失效

    公开(公告)号：US5922730A

    公开(公告)日：1999-07-13

    申请号：US103445

    申请日：1998-06-24

    申请人： David Cheng Hu ,  Alexander Aleksey Greenfield ,  Thomas Joseph Caggiano ,  Craig Eugene Caufield

    发明人： David Cheng Hu ,  Alexander Aleksey Greenfield ,  Thomas Joseph Caggiano ,  Craig Eugene Caufield

    IPC分类号： C07D498/18 ,  A61K31/445 ,  A61K31/435 ,  C07D471/04

    CPC分类号： C07D498/18

    摘要： This invention relates to compounds which possess immunosuppressive and/or anti tumor and/or antinflammatory activity in vivo and/or inhibit thymocyte proliferation in vitro. These compounds are therefore useful in the treaiment of transplantation rejection, autoimmune diseases such as lupus, rheumatoid ardiritis, diabetes mellitus, multiple sclerosis and in the treatment of Candida albicans infections and also in treatment of diseases of inflammation. These compounds are represented by the formula below ##STR1## wherein W and Y are OR.sup.1 and X and Z together form a bond or W and X are OR.sup.2 and Y and Z together form a bond, wherein:R.sup.1 is selected from --(CH.sub.2).sub.n --Ar with a proviso that Ar is not phenyl,--(CH.sub.2 CH.sub.2 O).sub.n CH.sub.3 with a proviso that n is greater than one,--CH.sub.2 CH.sub.2 CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3,--(CH.sub.2).sub.n --CH.sub.2 CH(OR.sup.3)CH.sub.2 OR.sup.4 where R.sup.3 and R.sup.4 are H, C.sub.1 -C.sub.10 alkyl, or R.sup.3 and R.sup.4 together are ethylene, methylene or dimethylmethylene;--CH.sub.2 (CH.sub.2).sub.n --OR.sup.3 with a proviso that R.sup.3 is not H, C.sub.1 -C.sub.10 alkyl, or C(O)C.sub.1 -C.sub.10 alkyl;and --CH.sub.2 (CH.sub.2).sub.n --X where X is F, Cl, Br or I;R.sup.2 is selected from H, C.sub.1 -C.sub.10 alkyl, Ar(CH.sub.2).sub.n --, C.sub.3 -C.sub.10 alkenyl, --(CH.sub.2 (CH.sub.2 O).sub.n CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3, --CH.sub.2 (CH.sub.2).sub.n --OR.sup.3, --CH.sub.2 (CH.sub.2).sub.n --Xwhere X is F, Cl, Br or I;and --(CH.sub.2).sub.n --CH.sub.2 CH(OR.sup.5)CH.sub.2 OR.sup.6 where R.sup.5 and R.sup.6 are selected independently from H, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.n --Ar, --CONH(CH.sub.2).sub.n --Ar or COC(CH.sub.3).sub.2 --(CH.sub.2).sub.n --Ar, --COR.sup.7 and --CO.sub.2 R.sup.7, where R.sup.7 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or Ar; or R.sup.5 and R.sup.6 together are methylene, ethylene, or dimethylmethylene;R.sup.3 and R.sup.4 indepently are H, methyl, --(CH.sub.2).sub.n CH.sub.3, --(CH.sub.2).sub.n Ar, --(CH.sub.2).sub.n CH.dbd.CH.sub.2, --C(O)R.sup.7, --CO.sub.2 R.sup.7, --CONH(CH.sub.2).sub.n Ar or --C(O)C(CH.sub.3).sub.2 --(CH.sub.2).sub.n Ar;Ar is selected independently from phenyl, pyridinyl, quinolinyl, indolyl, furanyl, 1, 2, 3-triazolyl and tetrazolyl;n=1-10 independently; andm=1-5 independently,or a pharmaceutically acceptable acid addition salt where one can be formed.