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15 条记录 (耗时 0.034 秒)

    Compounds for enzyme inhibition
    13.
    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

    申请人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser

    发明人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser

    IPC分类号： A61K38/08

    CPC分类号： C07K5/1016 ,  A61K38/00 ,  A61K38/07 ,  C07K5/0812 ,  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 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。

    Enzyme inhibition
    14.
    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。