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    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION
    3.
    发明授权
    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION 有权
    蛋白酶抑制剂化合物

    公开(公告)号：EP3101026B1

    公开(公告)日：2018-03-28

    申请号：EP16166492.5

    申请日：2005-08-08

    申请人： Onyx Therapeutics, Inc.

    发明人： SMYTH, Mark S. ,  LAIDIG, Guy J.

    IPC分类号： C07K5/087

    CPC分类号： C07K5/1016 ,  A61K38/00 ,  A61K38/07 ,  C07K5/0812 ,  C07K5/0827 ,  C07K5/1008 ,  C07K5/1024

    摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

    Compounds for Proteasome Enzyme Inhibition
    7.
    发明公开
    Compounds for Proteasome Enzyme Inhibition 审中-公开
    Verbindungen zur Proteasomenzyminhibition

    公开(公告)号：EP2564834A3

    公开(公告)日：2013-08-21

    申请号：EP12189466.1

    申请日：2005-05-09

    申请人： Onyx Therapeutics, Inc.

    发明人： Smyth, Mark S. ,  Laidig, Guy J. ,  Borchardt, Ronald T. ,  Binin, Barry A. ,  Crews, Craig M. ,  Musser, John H. ,  Shenk, Kevin D. ,  Radel, Peggy A.

    IPC分类号： A61K9/19 ,  A61K31/336 ,  A61K31/396 ,  A61K47/40 ,  A61K9/00 ,  C07K5/062

    CPC分类号： C07K5/0812 ,  C07K5/06034 ,  C07K5/0827 ,  Y02A50/412

    摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

    摘要翻译： 包含含杂原子的三元环的基于肽的化合物有效地选择性地抑制N-末端亲核试剂（Nin）水解酶的特异性活性。 具有多种活性的那些Ntn的活性可被她描述的化合物差别地抑制。 例如，20S蛋白酶体的胰凝乳蛋白酶样活性可以用本发明化合物选择性地抑制。 基于肽的化合物包括环氧化物或氮丙啶，并且在N-末端官能化。 除了其它治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。