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Rapamycin hydroxyesters
专利权人:
Wyeth LLC
发明人:
Jerauld S. Skotnicki,Christina L. Leone,Guy A. Schiehser
申请号:
US13931400
公开号:
USRE044768E1
申请日:
2013.06.28
申请国别(地区):
US
年份:
2014
代理人:
摘要:
A compound of the structurewherein R1 and R2 are each, independently, hydrogen or —CO(CR3R4)b(CR5R6)dCR7R8R9;R3 and R4 are each, independently, hydrogen, alkyl, alkenyl, 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-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;b=0-6;d=0-6; andf=0-6with 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.
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