发明名称 Carbamates of rapamycin
摘要 A compound of the structure <IMAGE> II wherein R and R1 are each, independently, hydrogen, <IMAGE> <IMAGE> R2 and R3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -CO2R5, -COR5, -CN, -NO2, -SO2R5, -SO3R5, -OR5, -SR5, or Ar; R4 is hydrogen, alkyl, alkenyl, alkynyl, -CF3, -NR5R6, -CO2R5, -COR5, CONR5, CONR5R6, -NO2, halogen, -OR5, -SR5, -CN, -SO2R5, -SO3R5, -SO2NR5R6, or Ar; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; <IMAGE> are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR8 in the heterocyclic ring, and may be optionally substituted by R7; R7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, -CF3, -NR5R6, -CO2R5, -COR5, CONR5R6, -NO2, halogen, -OR5, -SR5, -CN, -SO2R5, -SO3R5, -SO2NR5R6, or Ar; R8 is hydrogen, alkyl, alkenyl, alkynyl, -CF3, -NR5R6, -CO2R5, -COR5, CONR5R6, -OR5, -SR5, -CN, -SO2R5, -SO3R5, -SO2NR5R6, or Ar; Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R1 are both not hydrogen, or a pharmaceutically acceptable salt thereof. which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
申请公布号 US5516780(A) 申请公布日期 1996.05.14
申请号 US19950391400 申请日期 1995.02.27
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 SKOTNICKI, JERAULD S.;PALMER, YVETTE L.;KAO, WENLING;ABOU-GHARBIA, MAGID A.
分类号 A61K31/395;A61K31/44;A61K31/675;C07D491/06;C07D498/04;C07D498/16;(IPC1-7):A61K31/395 主分类号 A61K31/395
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