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    • 7. 发明申请
    • SUBSTITUTED LACTOSE DERIVATIVES AS CELL ADHESION INHIBITORS
    • 取代的乳糖衍生物作为细胞粘附抑制剂
    • WO1995021180A1
    • 1995-08-10
    • PCT/US1995001295
    • 1995-02-01
    • GLYCOMED INCORPORATED
    • GLYCOMED INCORPORATEDABBAS, Saeed, A.DASGUPTA, FalguniASA, DarwinMUSSER, John, H.NASHED, Mina, A.
    • C07H03/06
    • C07H11/00C07H3/04C07H3/06C07H15/18C07H23/00Y10S514/825Y10S514/885Y10S514/886Y10S514/921
    • Compounds and methods of making them having formula (I) are described which bind to selectin receptors and thus modulate the course of inflammation, cancer and related diseases by modulating cell-cell adhesion events. In said formula each R is independently H or lower alkyl (1-4C); R is H, OH or lower alkyl (1-4C), or a lipophilic group such as a higher alkyl group (5-15C), alkylaryl or one or more additional saccharide residues; R is a negatively charged moiety including SO4 -, PO4 -, or related group; Y is H or lower alkyl (1-4C); and X is H or -CHR (CHOR )2CHR OR wherein R and R are each independently H, lower alkyl (1-4C), or taken together result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR ; said five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R , CH2OR , OR , OOCR , NR 2, NHCOR , and SR with the proviso that if X represents a hexose substituent R and R , taken together, cannot provide a hexose substituent.
    • 描述了制备它们具有式(I)的化合物和方法,其结合选择素受体,从而通过调节细胞粘附事件来调节炎症,癌症和相关疾病的过程。 在所述式中,R 1独立地为H或低级烷基(1-4C); R 2是H,OH或低级烷基(1-4C),或亲脂基团如高级烷基(5-15C),烷基芳基或一个或多个另外的糖残基; R 3是带负电荷的部分,包括SO 4 2-,PO 4 2-或相关基团; Y为H或低级烷基(1-4C); 并且X是H或-CHR 4(CHOR 1)2 CHR 5 OR 1其中R 4和R 5各自独立地为H,低级烷基(1-4C)或一起 导致任选地含有选自O,S和NR 1的杂原子的五元或六元环; 所述五元或六元环任选被一个选自R 1,CH 2 OR 1,OR 1,OOCR 1,NR 12,NHCOR 1, 和SR 1,条件是如果X表示己糖取代基R 3和R 4一起不能提供己糖取代基。