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    • 5. 发明申请
    • 5-Thioxylopyranose Compounds
    • 5-噻吩基吡喃糖化合物
    • US20090118325A1
    • 2009-05-07
    • US12352382
    • 2009-01-12
    • Didier THOMASMichel BondouxVeronique BarberousseVincent Peyrou
    • Didier THOMASMichel BondouxVeronique BarberousseVincent Peyrou
    • A61K31/437C07D409/02A61K31/428A61K31/423C07D471/02
    • C07H1/00C07H17/00
    • 5-thioxylose compounds, especially 5-thioxylopyranose compounds, a process for their preparation, and their use for treating and/or inhibiting thromboses, especially venous thromboses. The compounds correspond to formula I: in which the pentapyranosyl group represents a free or substituted 5-thio-β-D-xylopyranosyl group; R′, R″ and R′″ each independently represent a hydrogen atom, a C2-C6 acyl group, or two adjacent ones of them form a 1-methylethylidene bridge; X1 and X2 each represent carbon or nitrogen; Y1 and Y2 each independently represent carbon, nitrogen, sulfur or oxygen, with the proviso that if Y2 represents oxygen or sulfur, then Y1 represents carbon or nitrogen; R1, R2, R3, R4 and R5 each independently represent hydrogen, a COOR6 group where R6 represents hydrogen or a C1-C4 alkyl group optionally substituted by a phenyl ring, a halogen atom or a —COOR6 group; a C1-C4 alkoxy group; a C1-C6 acyl group; a benzoyl group or a phenyl ring; and the addition salts and/or active metabolites of such compounds.
    • 5-硫代羟基化合物,特别是5-羟基吡喃糖化合物,其制备方法及其用于治疗和/或抑制血栓形成,特别是静脉血栓形成的用途。 化合物对应于式I:其中五草酰基代表游离或取代的5-硫代-β-D-吡喃木糖基; R',R“和R”'各自独立地表示氢原子,C 2 -C 6酰基或其两个相邻的一个形成1-甲基亚乙基桥; X1和X2各自表示碳或氮; Y1和Y2各自独立地表示碳,氮,硫或氧,条件是如果Y2表示氧或硫,则Y1表示碳或氮; R 1,R 2,R 3,R 4和R 5各自独立地表示氢,COOR 6基团,其中R 6表示氢或任选被苯环,卤素原子或-COOR 6基团取代的C 1 -C 4烷基; C1-C4烷氧基; C1-C6酰基; 苯甲酰基或苯环; 和这些化合物的加成盐和/或活性代谢物。