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    • 19. 发明授权
    • Malonate derivatives of glycolipids as cell adhesion inhibitors
    • 糖脂的丙二酸酯衍生物作为细胞粘附抑制剂
    • US5747463A
    • 1998-05-05
    • US725147
    • 1996-10-02
    • Anne MarinierAlain Martel
    • Anne MarinierAlain Martel
    • C07H15/04A61K31/70C07H15/00
    • C07H15/04
    • There is provided a novel series of malonate derivatives of glycolipid compounds of the formula ##STR1## wherein R is an acyl residue of a fatty acid: R.sup.1 is --(CH.dbd.CH).sub.m --(CH.sub.2).sub.n --CH.sub.3 ; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each are independently hydrogen, unsubstituted or substituted (lower)alkanoyl, arylalkyl or arylcarbonyl wherein said substituent is selected from the group consisting of halogen, C.sub.1-4 alkyl, trifluoromethyl, hydroxy and C.sub.1-4 alkoxy provided that one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 substituents is --(CH.sub.2).sub.p --CH(CO.sub.2 R.sup.7).sub.2 ; m is an integer of 0 or 1; n is an integer of from 5 to 14 inclusive; p is an integer of from 2 to 6 inclusive; and R.sup.7 is hydrogen, a hydrolyzable ester group or a cation to form a non-toxic pharmaceutically acceptable salt; or a solvate or hydrate thereof which are inhibitors of selectin-mediated cellular adhesion and are useful in the treatment or prevention of inflammatory diseases and other pathological conditions in mammals.
    • 提供了一种新型的式I糖脂化合物的丙二酸酯衍生物,其中R是脂肪酸的酰基残基:R 1是 - (CH = CH)m - (CH 2)n -CH 3; R2,R3,R4,R5和R6各自独立地为氢,未取代或取代的(低级)烷酰基,芳基烷基或芳基羰基,其中所述取代基选自卤素,C 1-4烷基,三氟甲基,羟基和C 1-4烷氧基 条件是R2,R3,R4和R6取代基之一为 - (CH2)p-CH(CO2R7)2; m为0或1的整数; n为5〜14的整数, p为2〜6的整数, 和R7是氢,可水解的酯基或阳离子,以形成无毒的药学上可接受的盐; 或其选择素介导的细胞粘附抑制剂的溶剂化物或水合物,并且可用于治疗或预防哺乳动物的炎性疾病和其它病理状况。