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    • 2. 发明申请
    • CLASSES OF COMPOUNDS THAT INTERACT WITH INTEGRINS
    • 与INTEGRINS互动的化合物类
    • WO2006081616A1
    • 2006-08-10
    • PCT/AU2006/000129
    • 2006-02-02
    • ALCHEMIA LIMITEDMEUTERMANS, WimWEST, Michael LeoTHANH LE, GiangHALLIDAY, JudyCLARK, Christopher
    • MEUTERMANS, WimWEST, Michael LeoTHANH LE, GiangHALLIDAY, JudyCLARK, Christopher
    • A61K31/351A61P3/10A61P11/06A61P17/02A61P25/28A61P35/00A61P37/08
    • A61K31/351A61K31/70
    • 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, CH 2 , NH, NR A or hydrogen, in the case where Z is hydrogen then R 1 is not present, R A is selected from the set defined for R 1 to R 5 , X is oxygen or NR A providing that at least one X of General Formula I is NR A , X may also combine independently with one of R 1 to R 5 to form an azide, R1 to R5 are independently selected from the group comprising H, -(CO)R 6 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 R 6 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 XR 2 or XR 3 or XR 4 or XR 5 is not NH 2 , with the further proviso that not more than one of R2 to R5 is hydrogen, where the group X is NR A and R A is not hydrogen, the groups R A and the corresponding group R 2 to R 5 may combine to form a cycle.
    • 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; Z是硫,氧,CH 2,NH,NR A或氢,在Z是氢的情况下,R 1不存在 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为NR A,X还可以独立地与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 N或烷基,酰基,烯基,炔基,杂烷基,芳基,杂芳基,芳烷基或杂芳基烷基取代基 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,杂烷基, 1至20个原子的芳基,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 在取代基中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 A, / SUP>不是氢,基团R A和相应的R 2至R 5可以组合形成一个周期。