公开(公告)号：US20230098016A1

公开(公告)日：2023-03-30

申请号：US17944757

申请日：2022-09-14

申请人： China Pharmaceutical University

发明人： Qidong YOU ,  Xiaoke GUO ,  Dongdong LI ,  Weilin CHEN ,  Zhihui WANG

IPC分类号： C07D405/12 ,  C07D249/06 ,  C07D401/12 ,  C07D403/10

摘要： The present disclosure relates to the field of medicinal chemistry, in particular to a phenyl triazole MLL1-WDR5 protein-protein interaction inhibitor (I) and a preparation method thereof, and pharmacodynamics experiments prove that the compound of the present disclosure has relatively strong MLL1-WDR5 protein-protein interaction inhibition activity.

公开(公告)号：US20210139466A1

公开(公告)日：2021-05-13

申请号：US17078052

申请日：2020-10-22

申请人： China Pharmaceutical University

发明人： Qidong YOU ,  Xiaoke GUO ,  Dongdong LI ,  Weilin CHEN ,  Zhihui WANG

IPC分类号： C07D405/12 ,  C07D249/06 ,  C07D401/12 ,  C07D403/10

摘要： The present disclosure relates to the field of medicinal chemistry, in particular to a phenyl triazole MLL1-WDR5 protein-protein interaction inhibitor (I) and a preparation method thereof, and pharmacodynamics experiments prove that the compound of the present disclosure has relatively strong MLL1-WDR5 protein-protein interaction inhibition activity.

公开(公告)号：US20220152027A1

公开(公告)日：2022-05-19

申请号：US17434353

申请日：2019-03-22

申请人： CHINA PHARMACEUTICAL UNIVERSITY

发明人： Qi Dong YOU ,  Xiaoke GUO ,  Weilin CHEN ,  Dongdong LI ,  Jing GU ,  Jun XU ,  Xin CHEN ,  Zhengyu JIANG ,  Xiaoli XU

IPC分类号： A61K31/517 ,  A61P35/00 ,  A61K31/506 ,  A61K31/5355

摘要： The present disclosure discloses a WDR5 protein-protein interaction inhibitor, including a compound having a structure represented by general formula (I). Experiments show that the inhibitor acts on a WDR5 protein and an interacting protein thereof including, but not limited to, MLL, selectively inhibits the proliferation of leukemia cells, and inhibits the methylation of H3K4 and the expression of downstream Hox/Meis-1 gene at the cellular level. The present disclosure also discloses a method for preparing the inhibitor and use thereof in the preparation of a drug for treating acute leukemia and other related diseases.