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15 条记录 (耗时 0.025 秒)

    Protease inhibitors
    1.
    发明授权
    Protease inhibitors 失效
    蛋白酶抑制剂

    公开(公告)号：US06583137B1

    公开(公告)日：2003-06-24

    申请号：US10129674

    申请日：2002-05-06

    申请人： Robert Wells Marquis, Jr. ,  Daniel Frank Veber

    发明人： Robert Wells Marquis, Jr. ,  Daniel Frank Veber

    IPC分类号： A61K3155

    CPC分类号： C07D401/14 ,  A61K31/55 ,  Y02A50/411 ,  Y02A50/423

    摘要： This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvent thereof, which is an inhibitor of cysteine proteases, particularly cathespin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，水合物或溶剂，其是半胱氨酸蛋白酶，特别是cathespin K的抑制剂，并且可用于治疗其中抑制骨丢失或 软骨退化是一个因素

    Protease inhibitors
    7.
    发明授权
    Protease inhibitors 失效
    蛋白酶抑制剂

    公开(公告)号：US06596715B1

    公开(公告)日：2003-07-22

    申请号：US10129671

    申请日：2002-05-06

    申请人： Robert W. Marquis, Jr. ,  Daniel Frank Veber

    发明人： Robert W. Marquis, Jr. ,  Daniel Frank Veber

    IPC分类号： C07D41300

    CPC分类号： C07D401/14 ,  C07B2200/05

    摘要： This invention relates to the compound of Formula (I): or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，水合物或溶剂化物，其是半胱氨酸蛋白酶，特别是组织蛋白酶K的抑制剂，并且可用于治疗其中抑制骨丢失或 的软骨退化是一个因素。

    Protease inhibitors
    9.
    发明授权
    Protease inhibitors 失效
    蛋白酶抑制剂

    公开(公告)号：US06534498B1

    公开(公告)日：2003-03-18

    申请号：US10129681

    申请日：2002-05-06

    申请人： Robert W. Marquis, Jr. ,  Yu Ru ,  Daniel Frank Veber

    发明人： Robert W. Marquis, Jr. ,  Yu Ru ,  Daniel Frank Veber

    IPC分类号： A61K3155

    CPC分类号： C07D401/14 ,  A61K31/55 ,  Y02A50/411

    摘要： This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，水合物或溶剂合物，其是半胱氨酸蛋白酶，特别是组织蛋白酶K的抑制剂，并且可用于治疗其中抑制骨丢失或 软骨退化是一个因素。

    Phenyl urea antagonists of the IL-8 receptor
    10.
    发明授权
    Phenyl urea antagonists of the IL-8 receptor 失效
    苯基脲拮抗剂的IL-8受体

    公开(公告)号：US06211373B1

    公开(公告)日：2001-04-03

    申请号：US09111663

    申请日：1998-07-08

    申请人： Katherine Louisa Widdowson ,  Daniel Frank Veber ,  Anthony Joseph Jurewicz ,  Robert Philip Hertzberg ,  Melvin Clarence Rutledge, Jr.

    发明人： Katherine Louisa Widdowson ,  Daniel Frank Veber ,  Anthony Joseph Jurewicz ,  Robert Philip Hertzberg ,  Melvin Clarence Rutledge, Jr.

    IPC分类号： C07D33310

    CPC分类号： A61K31/426 ,  A61K31/18 ,  A61K31/277 ,  A61K31/381 ,  A61K31/47 ,  Y02A50/411

    摘要： This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor. Compounds of Formula (1) are represented by the structure: wherein interalia, X is oxygen or sulfur; R is any functional moiety having an ionizable hydrogen and a pKa of 10 or less; R1 is independently selected from hydrogen; halogen; nitro; cyano; C1-C10 alkyl; halosubstituted C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-10 alkoxy; azide; (CR8R8)qS(O)tR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryl C2-10 alkenyl; aryloxy; aryl C1-4 alkyloxy; heteroaryl; heteroarylalkyl; heteroaryl C2-10 alkenyl; heteroaryl C1-4 alkyloxy; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C1-4 alkyloxy; heterocyclic C2-10 alkenyl; q is 0 or an integer having a value of 1 to 10; n is an integer having a value of 1 to 3; m is an integer having a value of 1 to 3; n is an integer having a value of 1 to 3; Y is hydrogen; halogen; nitro; cyano; halosubstituted C1-10 alkyl; C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-1- alkoxy; azide; (CR8R8)qS(O)tR4, (CR8R8)qOR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryloxy; aryC1-4 alkyloxy; aryl C2-10 alkenyl; heteroaryl; heteroarylalkyl; heteroaryl C1-4 alkyloxy; heteroaryl C2-10 alkenyl; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C2-10 alkenyl; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及式（I）的新型化合物，以及这些化合物在治疗趋化因子介导的疾病中的新用途，其中趋化因子与IL-8α或b受体结合。 式（1）的化合物由以下结构表示：其中间隔，X是氧或硫; R是具有可电离的氢和pKa为10或更小的任何官能部分; R 1独立地选自氢; 卤素; 硝基 氰基; C1-C10烷基; 卤代C 1-10烷基; C 2-10烯基; C 1-10烷氧基; 卤代C 1-10烷氧基; 叠氮化物 （CR8R8）qS（O）tR4; 羟基; 羟基取代的C 1-4烷基; 芳基; 芳基C 1-4烷基; 芳基C2-10烯基; 芳氧基 芳基C 1-4烷氧基; 杂芳基; 杂芳基烷基; 杂芳基C2-10烯基; 杂芳基C 1-4烷氧基; 杂环，杂环C 1-4烷基; 杂环C 1-4烷氧基; 杂环C 2-10烯基; q为0或值为1至10的整数; n为1〜3的整数，m为1〜3的整数，n为1〜3的整数，Y为氢; 卤素; 硝基 氰基; 卤代C 1-10烷基; C 1-10烷基; C 2-10烯基; C 1-10烷氧基; 卤代C 1-1烷氧基; 叠氮化物 （CR8R8）qS（O）tR4，（CR8R8）qOR4; 羟基; 羟基取代的C 1-4烷基; 芳基; 芳基C 1-4烷基; 芳氧基 aryC1-4烷氧基; 芳基C2-10烯基; 杂芳基; 杂芳基烷基; 杂芳基C 1-4烷氧基; 杂芳基C2-10烯基; 杂环，杂环C 1-4烷基; 杂环C 2-10烯基;或其药学上可接受的盐。