会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 10. 发明授权
    • Alkylated rapamycin derivatives
    • US5922730A
    • 1999-07-13
    • US103445
    • 1998-06-24
    • David Cheng HuAlexander Aleksey GreenfieldThomas Joseph CaggianoCraig Eugene Caufield
    • David Cheng HuAlexander Aleksey GreenfieldThomas Joseph CaggianoCraig Eugene Caufield
    • C07D498/18A61K31/445A61K31/435C07D471/04
    • C07D498/18
    • 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.