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    • 4. 发明授权
    • Amino acid derivatives of triptolide compounds as immune modulators and anticancer agents
    • 雷公藤内酯化合物的氨基酸衍生物作为免疫调节剂和抗癌剂
    • US06569893B2
    • 2003-05-27
    • US10098009
    • 2002-03-14
    • Dongcheng DaiJohn M. FidlerJohn H. Musser
    • Dongcheng DaiJohn M. FidlerJohn H. Musser
    • A61K31343
    • C07D493/22A61K31/365Y02A50/401
    • Compounds which are prodrugs of triptolide or its derivatives, containing an amino acid or oligopeptide moiety, are used for anticancer or immunosuppressive treatment. The compounds are of the structure: where X1 is OH or OR1, and X2 and X3 are independently OH, OR1 or H, with the proviso that at least one of X1, X2 and X3 is OR1, and at least one of X2 and X3 is H; and R1, is selected from the group consisting of: C(═O)CHY—NHP1  (b): C(═O)CH(NHP1)—(CH2)m—C(═O)OP2  (c): C(═O)(CH2)n—CH(NHP1)—C(═O)OP2 and  (d): [C(═O)CHY—NH]Z—C(═O)CHY—NHP1;  (e): where Y is a side chain of a naturally occurring amino acid or a one- or two-carbon homolog thereof; P1 is selected from the group consisting of H, C(═O)OR2, and C(═O)R3, where each of R2 and R3 is independently H, alkyl, alkenyl, aryl, or aralkyl; m is an integer from 0-5; n is an integer from 0-5; z is an integer from 2-10; and P2 is selected from the group consisting of H, alkyl, alkenyl, aryl, and aralkyl.
    • 作为含有氨基酸或寡肽部分的雷公藤内酯衍生物或其衍生物的前药的化合物用于抗癌或免疫抑制治疗。 该化合物具有以下结构:其中X 1是OH或OR 1,且X 2和X 3独立地是OH,OR 1或H,条件是X 1,X 2和X 3中的至少一个是OR 1,以及X 2和X 3中的至少一个 是H 并且R 1选自:其中Y是天然存在的氨基酸的侧链或其一或二碳同系物; P1选自H,C(= O)OR 2和C(= O)R 3,其中R 2和R 3各自独立地为H,烷基,烯基,芳基或芳烷基; m是0-5的整数; n是0-5的整数; z是2-10的整数; 且P2选自H,烷基,烯基,芳基和芳烷基。