公开(公告)号：WO2019152536A1

公开(公告)日：2019-08-08

申请号：PCT/US2019/015875

申请日：2019-01-30

Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

Inventor： JUNG, Michael, E. ,  CHEN, Xiaohong ,  WANG, Cun-Yu ,  LI, Jiong ,  ZHENG, Jie

IPC: C07C233/32 ,  C07C233/33 ,  C07C233/62 ,  C07C233/76 ,  C07C311/07 ,  C07D213/68 ,  C07D213/89 ,  C07D213/26 ,  C07D295/145 ,  C07D295/10 ,  C07D279/12 ,  C07D401/12 ,  C07D401/06 ,  C07D413/06 ,  C07D413/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07F9/44 ,  A61K31/45 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/164 ,  A61K31/18 ,  A61K31/664 ,  A61P35/00

Abstract: The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.

公开(公告)号：WO2021247889A1

公开(公告)日：2021-12-09

申请号：PCT/US2021/035735

申请日：2021-06-03

Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

Inventor： WANG, Cun-Yu ,  JIA, Lingfei

IPC: A61K35/00 ,  A61K38/00 ,  A61K38/19 ,  A61K31/44

Abstract: The present disclosure reports that pharmacological or genetic inhibition of Moloney murine leukemia virus insertion site 1 (BMI1) not only helped to eliminate BMI1+ cancer stem cells (CSCs), but can also augment PD1 blockade by strongly induced tumor cell-intrinsic immune responses by recruiting and activating CD8+ T cells. Taken together, the results indicate that in addition to purging CSCs, targeting BMI1 would enable immune checkpoint blockade to inhibit metastatic tumor growth and prevent tumor relapse by activating cell-intrinsic immunity.