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6 条记录 (耗时 0.023 秒)

    Enzyme inhibition
    1.
    发明授权
    Enzyme inhibition 有权
    酶抑制

    公开(公告)号：US06831099B1

    公开(公告)日：2004-12-14

    申请号：US09569748

    申请日：2000-05-11

    申请人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Ny Sin ,  Kyung Bo Kim

    发明人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Ny Sin ,  Kyung Bo Kim

    IPC分类号： A01N4320

    CPC分类号： C07K5/1016 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/06

    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 and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.

    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和PGPH活性。 基于肽的化合物包括与环官能团相邻的吸电子基团，并且肽包括至少三个肽单元。 在其他治疗用途中，基于肽的化合物表现出抗炎和抑制细胞增殖，涉及这些化合物的治疗应用。

    Enzyme inhibition
    2.
    发明授权
    Enzyme inhibition 有权
    酶抑制

    公开(公告)号：US07476650B2

    公开(公告)日：2009-01-13

    申请号：US10871752

    申请日：2004-06-17

    申请人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Kyung Bo Kim

    发明人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Kyung Bo Kim

    IPC分类号： A01N43/02 ,  A61K38/00

    CPC分类号： C07K5/1016 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/06

    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 and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.

    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和PGPH活性。 基于肽的化合物包括与环官能团相邻的吸电子基团，并且肽包括至少三个肽单元。 在其他治疗用途中，基于肽的化合物表现出抗炎和抑制细胞增殖，涉及这些化合物的治疗应用。

    Enzyme inhibition
    3.
    发明申请
    Enzyme inhibition 审中-公开

    公开(公告)号：US20090099097A1

    公开(公告)日：2009-04-16

    申请号：US12291236

    申请日：2008-11-07

    申请人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Kyung Bo Kim

    发明人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Kyung Bo Kim

    IPC分类号： A61K38/08

    CPC分类号： C07K5/1016 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/06

    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 and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.