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11 条记录 (耗时 0.015 秒)

    Compounds and methods for modulating CXCR3 function
    1.
    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

    申请人： Thomas J. Schall ,  Daniel J. Dairaghi ,  Brian E. McMaster

    发明人： Thomas J. Schall ,  Daniel J. Dairaghi ,  Brian E. McMaster

    IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/472 ,  A61K31/4725 ,  A61P11/06

    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。

    Compounds and methods for modulating cxcr3 function
    6.
    发明授权
    Compounds and methods for modulating cxcr3 function 有权
    调节cxcr3功能的化合物和方法

    公开(公告)号：US06559160B1

    公开(公告)日：2003-05-06

    申请号：US09648329

    申请日：2000-08-25

    申请人： Thomas J. Schall ,  Daniel J. Dairaghi ,  Brian E. McMaster

    发明人： Thomas J. Schall ,  Daniel J. Dairaghi ,  Brian E. McMaster

    IPC分类号： C07D23988

    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; 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.

    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 。

    Bicyclic compounds as inhibitors of chemokine binding to US28
    7.
    发明授权
    Bicyclic compounds as inhibitors of chemokine binding to US28 有权
    双环化合物作为趋化因子结合US28的抑制剂

    公开(公告)号：US07101894B2

    公开(公告)日：2006-09-05

    申请号：US10233326

    申请日：2002-08-29

    申请人： Brian E. McMaster ,  Thomas J. Schall ,  Mark Penfold ,  J. J. Wright ,  Daniel J. Dairaghi

    发明人： Brian E. McMaster ,  Thomas J. Schall ,  Mark Penfold ,  J. J. Wright ,  Daniel J. Dairaghi

    IPC分类号： A61K31/44 ,  A61K31/47

    CPC分类号： C07D207/08 ,  A61K31/075 ,  A61K31/135 ,  A61K31/4709 ,  C07D207/27 ,  C07D211/14 ,  C07D211/26 ,  C07D231/12 ,  C07D241/04 ,  C07D295/088 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D453/04

    摘要： Methods for treating CMV or a CMV-related disease are provided that use compounds having the formula: wherein Ar is a substituted or unsubstituted 5–14 membered heteroaryl group having from 1 to 5 heteroatoms as ring members; R1 is selected from the group consisting of substituted or unsubstituted aryl(C1–C4)alkyl, heteroaryl(C1–C4)alkyl, —C(O)R11, and —C(O)NR11R12, wherein each R11 and R12 independently is substituted or unsubstituted aryl, substituted or unsubstituted aryl(C1–C4)alkyl, substituted or unsubstituted (C4–C8)cycloalkyl(C1–C4)alkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl(C1–C4)alkyl and substituted or unsubstituted hetero(C4–C8)cycloalkyl(C1–C4)alkyl; R2 is H or (C1–C8)alkyl; and ZN is a substituted or unsubstituted hetero(C6–C10)bicycloalkyl group.

    摘要翻译： 提供了使用具有下式的化合物治疗CMV或CMV相关疾病的方法：其中Ar是具有1至5个杂原子作为环成员的取代或未取代的5-14元杂芳基; R 1选自取代或未取代的芳基（C 1 -C 4 -C 4）烷基，杂芳基（C 1 H 4） -C（O）R 11和-C（O）NR 11 R 12 > 12，其中每个R 11和R 12独立地是取代或未取代的芳基，取代或未取代的芳基（C 1〜 C 1 -C 4烷基，取代或未取代的（C 1 -C 4 -C 8）环烷基（C 1 -C 4 - 取代或未取代的杂芳基，取代或未取代的杂芳基（C 1 -C 4 -C 4）烷基和取代或未取代的杂原子（C