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    Classes of Compounds that Interact with Integrins
    9.
    发明申请
    Classes of Compounds that Interact with Integrins 审中-公开
    与整合素相互作用的化合物类

    公开(公告)号：US20080176936A1

    公开(公告)日：2008-07-24

    申请号：US11813737

    申请日：2006-02-02

    申请人： Wim Meutermans ,  Michael L. West ,  Giang Thanh Le ,  Judy Halliday ,  Christopher Clark

    发明人： Wim Meutermans ,  Michael L. West ,  Giang Thanh Le ,  Judy Halliday ,  Christopher Clark

    IPC分类号： A61K31/351 ,  C07D315/00 ,  A61P3/10

    CPC分类号： A61K31/351 ,  A61K31/70

    摘要： A method of inhibiting or effecting the activity of an integral receptor which comprises contacting an integrin with a compound of formula I, or a pharmaceutically acceptable salt thereof; General Formula I Wherein the ring may be of any configuration; Z is sulphur, oxygen, CH2, NH, NRA or hydrogen, in the case where Z is hydrogen then R1 is not present, RA is selected from the set defined for R1 to R5, X is oxygen or NRA providing that at least one X of General Formula I is NRA, X may also combine independently with one of R1 to R5 to form an azide, R1 to R5 are independently selected from the group comprising H, —(CO)R6 or an alkyl, acyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl substituent of 1 to 20 atoms, which is optionally substituted, and can be branched or linear wherein substituents may optionally be further substituted, wherein R6 is selected from the group comprising an alkyl, acyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl substituent of 1 to 20 atoms, which is optionally substituted, and can be branched or linear wherein substituents may optionally be further substituted, with the proviso that XR2 or XR3 or XR4 or XR5 is not NH2, with the further proviso that not more than one of R2 to R5 is hydrogen, where the group X is NRA and RA is not hydrogen, the groups RA and the corresponding group R2 to R5 may combine to form a cycle.

    摘要翻译： 一种抑制或影响整体受体活性的方法，其包括使整联蛋白与式I化合物或其药学上可接受的盐接触; 通式I其中环可以是任何配置; 在Z是氢的情况下，Z是硫，氧，CH 2，NH，NR A或氢，则不存在R 1 R A选自从R 1至R 5定义的集合，X是氧或NR A， 条件是通式I的至少一个X是NR A，X也可以独立地与R 1至R 5中的一个结合形成 叠氮化物，R 1至R 5独立地选自H， - （CO）R 6或烷基，酰基，烯基，炔基，杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基取代基 1至20个原子，其任选被取代，并且可以是支链或直链的，其中取代基可任选被进一步取代，其中R 6选自烷基，酰基，烯基，炔基， 1至20个原子的杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基取代基，其任选被取代，并且可以是支链或直链的 取代基可以任选地被进一步取代，条件是XR 2或XR 3或XR 4或XR 5 不是NH 2，另外条件是R 2至R 5中不超过一个是氢，其中基团X是NR A和R O， A 不是氢，基团R A和相应的基团R 2至R 5可以结合形成一个循环。