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。