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    • 12. 发明授权
    • Compounds and methods for modulating cxcr3 function
    • 调节cxcr3功能的化合物和方法
    • US06559160B1
    • 2003-05-06
    • US09648329
    • 2000-08-25
    • Thomas J. SchallDaniel J. DairaghiBrian E. McMaster
    • Thomas J. SchallDaniel J. DairaghiBrian E. McMaster
    • C07D23988
    • C07D239/91
    • 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; R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl; each R3 is independently a substituent selected from -halogen, —OR′, —OC(O)R′, —NR′R″, —SR′, —R′, —CN, —NO2, —CO2R′, —CONR′R″, —C(O)R′, —OC(O)NR′R″, —NR″C(O)R′, —NR″C(O)2R′, , —NR′—C(O)NR″R′″, —NH—C(NH2)═NH, —NR′C(NH2)═NH, —NH—C(NH2)═NR—, —S(O)R′, —S(O)2R′, —S(O)2NR′R″, —N3, —CH(Ph)2, perfluoro(C1-C4)alkoxy, and perfluoro(C1-C4)alkyl, and where R′, R″ and R′″ are independently selected from hydrogen, (C1-C8)alkyl and heteroalkyl, unsubstituted aryl and heteroaryl, (unsubstituted aryl)-(C1-C4)alkyl, and (unsubstituted aryl)oxy-(C1-C4)alkyl; Y is a member selected from the group consisting of substituted or unsubstituted (C2-C8)alkylene and substituted or unsubstituted (C2-C8)heteroalkylene; and Z is —NR4R5, wherein R4 and R5 are independently selected from the group consisting of hydrogen and (C1-C8)alkyl. 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.
    • 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为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; R1为选自 由取代或未取代的(C 5 -C 15)烷基组成; R 2为选自取代或未取代的(C 1 -C 8)烷基的成员;每个R 3独立地为选自卤素,-OR',-OC( O)R',-NR'R“,-SR',-R',-CN,-NO 2,-CO 2 R',-CONR'R”,-C(O)R',-OC(O) NR'R“,-NR''C(O)R',-NR''C(O)2 R', - NR'-C(O)NR''R”',-NH-C( NH2)= NH,-NR'C(NH2)= NH,-NH-C(NH2)= NR-,-S(O)R',-S(O)2R',-S(O) ',-N3,-CH(Ph)2,全氟(C1-C4)烷氧基和全氟(C1-C4)烷基,其中R',R“和R”'独立地选自氢,( C1-C8)烷基和杂烷基,未取代的芳基和杂芳基,(未取代的芳基) - (C1-C4)烷基和(未取代的芳基)氧基 - (C1-C4)烷基; Y是 选自取代或未取代的(C 2 -C 8)亚烷基和取代或未取代的(C 2 -C 8)杂亚烷基的基团; Z为-NR 4 R 5,其中R 4和R 5独立地选自氢和(C1- C8)烷基。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CXCR3活性调节作用的疾病和病症,例如多发性硬化症,类风湿性关节炎,牛皮癣,癌症,感染性疾病,血管生成和移植排斥 。