公开(公告)号：US20230131867A1

公开(公告)日：2023-04-27

申请号：US17947716

申请日：2022-09-19

申请人： SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH

发明人： David GIN ,  Michelle ADAMS ,  Kai DENG ,  Philip LIVINGSTON ,  Govindaswami RAGUPATHI ,  Eric CHEA ,  Alberto FERNANDEZ-TEJADA ,  Lars Ulrik NORDSTROEM ,  William WALKOWICZ ,  Jeffrey GARDNER ,  Derek TAN

IPC分类号： C07H15/256 ,  C07H13/08 ,  A61K31/7024 ,  A61K31/704 ,  C07H15/24 ,  A61K39/385

摘要： The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.

公开(公告)号：US20170283450A1

公开(公告)日：2017-10-05

申请号：US15626046

申请日：2017-06-16

申请人： MEMORIAL SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH

发明人： David GIN ,  Michelle ADAMS ,  Kai DENG ,  Philip LIVINGSTON ,  Govindaswami RAGUPATHI ,  Eric CHEA ,  Alberto FERNANDEZ-TEJADA ,  Lars Ulrik NORDSTROEM ,  William WALKOWICZ ,  Jeffrey GARDNER ,  Derek TAN

IPC分类号： C07H15/256 ,  C07H13/08 ,  A61K31/7024 ,  A61K31/704 ,  A61K39/385 ,  C07H15/24

CPC分类号： C07H15/256 ,  A61K31/7024 ,  A61K31/704 ,  A61K39/385 ,  C07H13/08 ,  C07H15/24

摘要： The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.