发明名称 RAPAMYCIN HYDROXYESTERS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
摘要 A compound of structure (I) wherein R1 and R2 are each, independently, hydrogen or -CO(CR3R4)b(CR5R6)dCR7R8R9; R3 and R4 are each, independently, hydrogen, alkyl, alkenyle, alkynyl, trifluoromethyl, or -F; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, - F, or -CO2R11, or R5 and R6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR3R4)fOR10; R7 is hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, -F, or -CO2R11; R8 and R9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, - (CR3R4)fOR10, -CF3, -F, or -CO2R11, or R8 and R9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with - (CR3R4)fOR10; R10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri- (alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri- (alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5- (2-spiro-cycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2-spiro- cycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]-dioxalanyl, or 4-(2-spiro- cycloalkyl)[1,3]dioxalanyl; b = 0-6; d = 0-6; and f = 0-6 with the proviso that R1 and R2 are both not hydrogen and further provided that either R1 or R2 contains at least one -(CR3R4)fOR10, X, or -(CR3R4)fOR10 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 CA2187024(C) 申请公布日期 2004.08.10
申请号 CA19952187024 申请日期 1995.04.14
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 SKOTNICKI, JERAULD S.;LEONE, CHRISTINA L.;SCHIEHSER, GUY A.
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;(IPC1-7):C07H19/01;C07H23/00;A61K31/70 主分类号 C07D487/18
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