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42-HYDROXYESTER DE RAPAMICYNE, PROCEDE D'OBTENTION ET PREPARATIONS PHARMACEUTIQUES LE CONTENANT
专利权人:
Wyeth LLC
发明人:
申请号:
EP95915671.2
公开号:
EP0763039B3
申请日:
1995.04.14
申请国别(地区):
EP
年份:
2017
代理人:
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 antitum
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