Compounds and methods for modulating CXCR3 function
    18.
    发明授权
    Compounds and methods for modulating CXCR3 function 有权
    用于调节CXCR3功能的化合物和方法

    公开(公告)号:US06992084B2

    公开(公告)日:2006-01-31

    申请号:US10279353

    申请日:2002-10-23

    CPC分类号: C07D239/91

    摘要: The invention provides compounds and compositions of the formula: wherein, the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, R1 is a member selected from the group consisting of substituted or unsubstituted (C5–C15)alkyl and (C8–C14)acyl group; R2 is a member selected from the group consisting of substituted or unsubstituted (C1–C8)alkyl; each R3 is independently a substituent Y is a member selected from the group consisting of substituted or unsubstituted (C2–C8)alkylene and substituted or unsubstituted (C2–C8)heteroalkylene; Z is —NR4R5 R4 and R5 are independently selected from the group consisting of hydrogen and (C1–C8)alkyl or taken together with the nitrogen atom to which each is attached to form a heterocyclyl or heteroaryl; These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the modulation of CXCR3 activity, such as multiple sclerosis, rheumatoid arthritis, psoriasis, cancer, infectious disease, angiogenesis, and graft rejection.

    摘要翻译: 本发明提供下式的化合物和组合物:其中,下标n为0-4的整数; Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员,R 1是选自取代或未取代的(C 5 H 5) -C 15 -C 15烷基和(C 8 -C 14 -C 14)酰基; R 2是选自取代或未取代的(C 1 -C 8 -C 8)烷基的成员; 每个R 3独立地是取代基Y是选自取代或未取代的(C 1 -C 12 -C 8)亚烷基和 取代或未取代的(C 2 -C 8 -C 8)杂亚烷基; Z是-NR 4 R 5,R 4和R 5独立地选自氢和 (C 1 -C 8 -C 8烷基)或与各自连接的氮原子一起形成杂环基或杂芳基; 这些化合物和组合物结合CXCR3趋化因子受体,并且可用于治疗对调节CXCR3活性如多发性硬化,类风湿性关节炎,牛皮癣,癌症,感染性疾病,血管生成和移植物排斥反应的疾病和病症。