发明名称 Carbamates of rapamycin
摘要 A compound of the structure <IMAGE> wherein R1 and R2 are each, independently, hydrogen, -CONH-[(CR3R4)m(-A-(CR5R6)n)p]q-B; <IMAGE> R3, R4, R5, R6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, -OR7, -SR7, halogen, -CN, -NO2, -CF3, -COR7, -CO2R7, -CONHR7, -SO2R7, -OSO3R7, -NR7R8, -NHCOR7, -NHSO2R7, or Ar; R7 and R8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl; R9 and R10 are each, independently, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, -CF3, -COR7, -CO2R7, -CONHR7, -SO2R7, or Ar; A is -CH2-, -NR7-, -O-, -S-, -SO-, -SO2-, -PR7-, -CO-, -NHCO-, -NHSO-, or -P(O)(R7)-; Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri- substituted; <IMAGE> is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R1 and R2 are not both hydrogen; m=0-6; n=0-6; p=0-1; q=0-1; or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
申请公布号 US5302584(A) 申请公布日期 1994.04.12
申请号 US19930054655 申请日期 1993.04.23
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 KAO, WENLING;ABOU-GHARBIA, MAGID A.;VOGEL, ROBERT L.
分类号 A61K31/435;A61K31/395;A61K31/436;A61K31/44;A61K31/675;A61K31/70;A61P9/00;A61P29/00;A61P37/06;C07D;C07D221/00;C07D273/00;C07D311/00;C07D487/18;C07D491/06;C07D498/18;C07H19/01;C07J1/00;(IPC1-7):C07D491/06 主分类号 A61K31/435
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