发明名称 Aminodiesters of rapamycin
摘要 A compound of the structure <IMAGE> wherein R1 is <IMAGE> R3 is hydrogen, alkyl, arylalkyl, (CH2)sNR4R5, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazolylmethyl or phenyl which is optionally mono-, di-, or tri-substituted; R4 is hydrogen, alkyl, or aralkyl; R2 and R5 are each independently hydrogen, formyl, alkanoyl, arylalkanoyl, aryloyl, or CO2R6; R6 is alkyl, arylalkyl, allyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted; m is 0-4; n is 0-4; p is 0-1; q is 0-4; r is 0-4; and s is 0-4; or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, by virtue of its antifungal activity is useful in treating fungal infections; and by virtue of its antitumor activity is useful in treating tumors.
申请公布号 US5162333(A) 申请公布日期 1992.11.10
申请号 US19910757858 申请日期 1991.09.11
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 FAILLI, AMEDEO A.;STEFFAN, ROBERT J.
分类号 C07D498/18;C07D519/00 主分类号 C07D498/18
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