发明名称 Rapamycin oximes
摘要 A compound of the structure <IMAGE> wherein R1 is <IMAGE> <IMAGE> R2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar; R3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or -CO2R8; R4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or -CO2R8; R5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, or -CO2R8; R6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar; R7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar; R8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, or Ar; Y is O or S; X is =N-O-(CH2)f-Z or =N-O-Ar; Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, -NR5R6, aryloxy, or Ar; Ar is aryl which may be optionally mono-, di-, or tri-substituted; a=0-4; b=0-1; c=0-4; d=0-6; e=0-6; and f=0-6; or a pharmaceutically acceptable salt thereof, with the proviso that when f is 0, Z is hydrogen and further provided that when R3 or R5 is -CO2R8, R8 is not hydrogen which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
申请公布号 US5446048(A) 申请公布日期 1995.08.29
申请号 US19940309816 申请日期 1994.09.21
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 FAILLI, AMEDEO A.;STEFFAN, ROBERT J.;CAUFIELD, CRAIG E.;HU, DAVID C.;GRINFELD, ALEXANDER A.
分类号 C07D498/18;(IPC1-7):A61K31/44 主分类号 C07D498/18
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