专利检索 ap:("Tomi K. SAWYER" OR "Pietro ARONICA" OR "Christopher J. BROWN" OR "Fernando J. FERRER" OR "Charles W. JOHANNES" OR "Srinivasaraghavan KANNAN" OR "David P. LANE" OR "Anthony W. PARTRIDGE" OR "Yaw Sing TAN" OR "Chandra S. VERMA" OR "Tsz Ying YUEN" OR "Merck Sharp & Dohme Corp." OR "Agency for Science, Technology AND Research" OR "MSD International GMBH (Singapore Branch)") AND inv:"Fernando J. Ferrer" 第 1 页

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发明申请
P53 ACTIVATOR PEPTIDOMIMETIC MACROCYCLES 有权

公开(公告)号：US20220267376A1

公开(公告)日：2022-08-25

申请号：US17618751

申请日：2020-06-16

申请人： Tomi K. SAWYER , Pietro ARONICA , Christopher J. BROWN , Fernando J. FERRER , Charles W. JOHANNES , Srinivasaraghavan KANNAN , David P. LANE , Anthony W. PARTRIDGE , Yaw Sing TAN , Chandra S. VERMA , Tsz Ying YUEN , Merck Sharp & Dohme Corp. , Agency for Science, Technology and Research , MSD International GMBH (Singapore Branch)

发明人： Pietro Aronica , Christopher J. Brown , Fernando J. Ferrer , Charles W. Johannes , Srinivasaraghavan Kannan , David P. Lane , Anthony W. Partridge , Tomi K. Sawyer , Yaw Sing Tan , Chandra S. Verma , Tsz Ying Yuen

IPC分类号： C07K7/08 , A61K45/06 , C07K7/06 , A61P35/00

摘要： Peptidomimetic macrocycles that comprise all-D configuration ?-amino acids and bind mouse double minute 2 (MDM2 aka E3 ubiquitin-protein ligase) and MDMX (aka MDM4) are described. These all-D configuration α-amino acid peptidomimetic macrocycles are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX thereby antagonizing MDM2 and MDMX binding to p53. These peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.