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    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION
    1.
    发明申请
    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION 有权

    公开(公告)号：US20210179663A1

    公开(公告)日：2021-06-17

    申请号：US17169990

    申请日：2021-02-08

    申请人： Onyx Therapeutics, Inc.

    发明人： Mark S. Smyth ,  Guy J. Laidig

    IPC分类号： C07K5/107 ,  C07K5/087 ,  C07K5/103 ,  C07K5/08 ,  A61K38/07 ,  C07K5/117

    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
    2.
    发明申请
    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION 审中-公开
    抗生素抑制剂的化合物

    公开(公告)号：US20140342977A1

    公开(公告)日：2014-11-20

    申请号：US14452844

    申请日：2014-08-06

    申请人： Onyx Therapeutics, Inc.

    发明人： Mark S. Smyth ,  Guy J. Laidig

    IPC分类号： C07K5/117

    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.

    摘要翻译： 包括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（Ntn）水解酶的比活性。 具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。 例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。 肽类化合物包括环氧化物或氮丙啶，并且在N-末端官能化。 除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

    COMPOUNDS FOR PROTEASOME
    6.
    发明申请
    COMPOUNDS FOR PROTEASOME 审中-公开

    公开(公告)号：US20200071356A1

    公开(公告)日：2020-03-05

    申请号：US16669601

    申请日：2019-10-31

    申请人： Onyx Therapeutics, Inc.

    发明人： Mark S. Smyth ,  Guy J. Laidig

    IPC分类号： C07K5/107 ,  C07K5/117 ,  A61K38/07 ,  C07K5/08 ,  C07K5/103 ,  C07K5/087

    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
    8.
    发明申请
    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION 审中-公开

    公开(公告)号：US20180170962A1

    公开(公告)日：2018-06-21

    申请号：US15895120

    申请日：2018-02-13

    申请人： Onyx Therapeutics, Inc.

    发明人： Mark S. Smyth ,  Guy J. Laidig

    IPC分类号： C07K5/107 ,  C07K5/117

    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
    9.
    发明申请
    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION 审中-公开

    公开(公告)号：US20160222057A1

    公开(公告)日：2016-08-04

    申请号：US15094088

    申请日：2016-04-08

    申请人： Onyx Therapeutics, Inc.

    发明人： Mark S. Smyth ,  Guy J. Laidig

    IPC分类号： C07K5/107

    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.