发明名称 RAPAMYCIN HYDROXYESTERS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
摘要 A compound of structure (I) <CHEM> wherein R<1> and R<2> are each, independently, hydrogen or -CO(CR<3>R<4>)b(CR<5>R<6>)dCR<7>R<8>R<9> ; R<3> and R<4> are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or -F; R<5> and R<6> are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR<3>R<4>)fOR<10>, -CF3, -F, or -CO2R<11>, or R<5> and R<6> may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR<3>R<4>)fOR<10>; R<7> is hydrogen, alkyl, alkenyl, alkynyl, -(CR<3>R<4>)fOR<10>, -CF3, -F, or -CO2R<11>; R<8> and R<9> are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR<3>R<4>)fOR<10>, -CF3, -F, or -CO2R<11>, or R<8> and R<9> may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR<3>R<4>)fOR<10>; R<10> is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R<11> is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X is 5-(2,2-dialkyl)Ä1,3Üdioxanyl, 5-(2,2-dicycloalkyl)Ä1,3Üdioxanyl, 4-(2,2-dialkyl)Ä1,3Ü-dioxanyl, 4-(2,2-dicycloalkyl)Ä1,3Üdioxanyl, 4-(2,2-dialkyl)Ä1,3Üdioxalanyl, or 4-(2,2-dicycloalkyl)Ä1,3Üdioxalanyl; b = 0-6; d = 0-6; and f = 0-6 with the proviso that R<1> and R<2> are both not hydrogen and further provided that either R<1> or R<2> contains at least one -(CR<3>R<4>)fOR<10>, X, or -(CR<3>R<4>)fOR<10> substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
申请公布号 HUT77410(A) 申请公布日期 1998.04.28
申请号 HU19960002893 申请日期 1995.04.14
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 LEONE,CHRISTINA LOUISE;SCHIEHSER,GUY ALAN;SKOTNICKI,JERAULD STANLEY
分类号 C07D487/18;A61K31/435;A61K31/436;A61P9/00;A61P9/10;A61P11/00;A61P19/02;A61P29/00;A61P31/00;A61P31/04;A61P31/10;A61P35/00;A61P37/06;C07D498/18 主分类号 C07D487/18
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