发明名称 Compounds For Enzyme Inhibition
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.
申请公布号 US2012101025(A1) 申请公布日期 2012.04.26
申请号 US201113341022 申请日期 2011.12.30
申请人 SMYTH MARK S.;LAIDIG GUY J.;BORCHARDT RONALD T.;BUNIN BARRY A.;CREWS CRAIG M.;MUSSER JOHN H.;SHENK KEVIN D.;RADEL PEGGY A.;ONYX THERAPEUTICS, INC. 发明人 SMYTH MARK S.;LAIDIG GUY J.;BORCHARDT RONALD T.;BUNIN BARRY A.;CREWS CRAIG M.;MUSSER JOHN H.;SHENK KEVIN D.;RADEL PEGGY A.
分类号 A61K38/06;A61P1/00;A61P1/16;A61P1/18;A61P9/04;A61P9/10;A61P11/00;A61P11/06;A61P11/08;A61P13/12;A61P17/00;A61P17/06;A61P19/02;A61P21/00;A61P25/00;A61P25/02;A61P25/16;A61P25/28;A61P27/02;A61P29/00;A61P31/00;A61P31/04;A61P31/12;A61P31/18;A61P33/00;A61P35/00;A61P37/00;A61P37/06;A61P37/08;C07K5/06;C07K5/08;C07K5/087 主分类号 A61K38/06
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