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    UREA COMPOUNDS AS INHIBITORS FOR VLA-4
    61.
    发明公开
    UREA COMPOUNDS AS INHIBITORS FOR VLA-4 审中-公开
    脲类化合物作为VLA-4的抑制剂

    公开(公告)号：EP1252152A1

    公开(公告)日：2002-10-30

    申请号：EP01900551.1

    申请日：2001-01-17

    申请人： AstraZeneca AB

    发明人： JOHNSTONE, Craig,AstraZeneca ,  LARGE, Michael Stewart,AstraZeneca

    IPC分类号： C07D295/08 ,  C07D211/22 ,  C07D211/96 ,  C07C275/42 ,  C07C323/12 ,  C07C317/18 ,  A61K31/5375 ,  A61P29/00

    CPC分类号： C07D295/088 ,  C07C275/42 ,  C07C317/18 ,  C07C323/12 ,  C07C2601/08 ,  C07D211/22 ,  C07D211/54

    摘要： A compound of formula (I) where D is a VLA-4 specificity determinant which does not impart significant IIB/IIIa activity; R41 is a group of the formula (V): U - (CH¿2?)d - V - T wherein U is selected from oxygen, sulphur, a direct bond or -CH2O-, V is selected from nitrogen, oxygen, sulphur, S(O), S(O)2 or a direct bond, d is zero or a number from 1 to 4, and T is selected from a range of variables defined in the application; and other variables are defined in the application, or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof. The compounds are useful in the treatment of disease mediated by the interaction between VCAM-1 and/or fibronectin and the integrin receptor α4β1. Pharmaceutical compositions and methods of use or treatment are also described and claimed.

    摘要翻译： 其中D是不赋予显着IIB / IIIa活性的VLA-4特异性决定簇的式（I）化合物; R41是式（V）的基团：其中U选自氧，硫，直接键或-CH2O-，V选自氮，氧，硫 ，S（O），S（O）2或直接键，d为0或1至4的数，并且T选自本申请中定义的一系列变量; 和其他变量在本申请中定义，或其药学上可接受的盐或体内可水解的衍生物。 该化合物可用于治疗由VCAM-1和/或纤连蛋白与整联蛋白受体α4β1之间的相互作用介导的疾病。 药物组合物和使用或治疗方法也被描述和要求保护。

    SUBSTITUTED BETA-ALANINES
    63.
    发明公开
    SUBSTITUTED BETA-ALANINES 有权
    取代的β--丙氨酸

    公开(公告)号：EP1042279A1

    公开(公告)日：2000-10-11

    申请号：EP98962586.8

    申请日：1998-12-23

    申请人： Aventis Pharma Limited

    发明人： ASTLES, Peter, Charles ,  HARRIS, Neil, Victor ,  MORLEY, Andrew, David

    IPC分类号： C07C275/42 ,  C07D207/27 ,  A61K31/17 ,  A61K31/40

    CPC分类号： C07D207/27 ,  C07C275/42

    摘要： The invention is directed to physiologically active compounds of general formula (I), wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X?1, X2 and X6¿ independently represent N or CR2; and one of X?3, X4 and X5¿ represents CR3 and the others independently represents N or CR2 [where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group -L1-(CH2)n-C(=O)-N(R4)-CH2-CH2-Y]; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4(α4β1).