发明名称 Carbamates of rapaycin
摘要 A compound of the structure <IMAGE> II wherein R1 and R2 are each, independently, hydrogen, -CONR3(CR4R5)m(CR6R7)n(CR8R9)pNR10R11, or <IMAGE> or -CONR3R13; R3 is hydrogen, alkyl, or arylalkyl; R4, R5, R8, and R9 are each, independently, hydrogen, alkyl, -OH, -CF3, or -F; R6 is hydrogen or -OR13; R7 is hydrogen or alkyl; R10 is hydrogen, alkyl, or arylalkyl; R11, R12 and R13 are each, independently, -(CR15R16)rR17; R14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl; R15 and R16 are each, independently, hydrogen or alkyl; R17 is <IMAGE> or -C 3BOND C-R21; R18, R19, R20, and R21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; <IMAGE> is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ting may optionally contain NR22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyl, arylalkyl, halogen, -CF3, -OR14, or -CO2R10; R22 is hydrogen, alkyl, or arylalkyl; m=0-6; n=1-6; p=0-6; and r=1-6 with the proviso that R1 and R2 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 US5559227(A) 申请公布日期 1996.09.24
申请号 US19950449593 申请日期 1995.05.24
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 FAILLI, AMEDEO A.;BLEYMAN, OLEG I.;KAO, WENLING;ABOU-GHARBIA, MAGID A.
分类号 A61K31/395;A61K31/44;A61K31/675;C07D491/06;C07D498/04;C07D498/16;(IPC1-7):C07D491/06 主分类号 A61K31/395
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