发明名称 RAPAMYCIN HYDROXYESTERS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
摘要 <p>A compound of structure (I) wherein R?1 and R2¿ are each, independently, hydrogen or -CO(CR3R4)b(CR5R6)dCR?7R8R9; R3 and R4¿ are each, independently, hydrogen, alkyl, alkenyle, alkynyl, trifluoromethyl, or -F; R?5 and R6¿ are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, -F, or -CO2R?11, 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 -CO2R?11; R8 and R9¿ are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, -F, or -CO2R?11, 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 R?1 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.</p>
申请公布号 WO1995028406(A1) 申请公布日期 1995.10.26
申请号 US1995004603 申请日期 1995.04.14
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