Compounds for enzyme inhibition
    2.
    发明授权
    Compounds for enzyme inhibition 有权
    用于酶抑制的化合物

    公开(公告)号:US08088741B2

    公开(公告)日:2012-01-03

    申请号:US11596028

    申请日:2005-05-09

    IPC分类号: A61K38/06 C12Q1/34

    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 chymotrypsinlike 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 Enzyme Inhibition
    4.
    发明申请
    Compounds For Enzyme Inhibition 审中-公开
    化合物用于酶抑制

    公开(公告)号:US20120277146A1

    公开(公告)日:2012-11-01

    申请号:US13411044

    申请日:2012-03-02

    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 at least three peptide units, 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。 基于肽的化合物包括至少三个肽单元,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 enzyme inhibition
    6.
    发明授权
    Compounds for enzyme inhibition 有权
    用于酶抑制的化合物

    公开(公告)号:US07232818B2

    公开(公告)日:2007-06-19

    申请号:US11106879

    申请日:2005-04-14

    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 at least three peptide units, 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。 基于肽的化合物包括至少三个肽单元,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 enzyme inhibition
    9.
    发明授权
    Compounds for enzyme inhibition 有权
    用于酶抑制的化合物

    公开(公告)号:US07491704B2

    公开(公告)日:2009-02-17

    申请号:US11786217

    申请日:2007-04-11

    IPC分类号: A61K38/08

    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 at least three peptide units, 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。 基于肽的化合物包括至少三个肽单元,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。