公开(公告)号：US20240366774A1

公开(公告)日：2024-11-07

申请号：US18488912

申请日：2023-10-17

Applicant: The regents of the University of Michigan

Inventor： Jolanta GREMBECKA ,  Szymon Klossowski ,  Jing Deng ,  Tomasz Cierpicki ,  Hao Li ,  Hongzhi Miao ,  Trupta Purohit ,  EunGi Kim ,  Dong Chen

IPC: A61K47/64 ,  A61K9/00 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K38/45 ,  A61K47/54 ,  A61P35/02 ,  C07D209/24 ,  C07D471/04

Abstract: Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.

公开(公告)号：US20220288217A1

公开(公告)日：2022-09-15

申请号：US17504159

申请日：2021-10-18

Applicant: The Regents of the University of Michigan

Inventor： Jolanta Grembecka ,  Szymon Klossowski ,  Jing Deng ,  Tomasz Cierpicki ,  Hao Li ,  Hongzhi Miao ,  Trupta Purohit ,  EunGi Kim

IPC: A61K47/64 ,  A61K9/00 ,  A61K31/454 ,  A61K38/45 ,  A61P35/02 ,  A61K47/54 ,  A61K31/404 ,  A61K31/4545 ,  C07D209/24 ,  C07D471/04

Abstract: Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

公开(公告)号：US20190142961A1

公开(公告)日：2019-05-16

申请号：US16186012

申请日：2018-11-09

Applicant: The Regents of the University of Michigan

Inventor： Jolanta Grembecka ,  Szymon Klossowski ,  Jing Deng ,  Tomasz Cierpicki ,  Hao Li ,  Hongzhi Miao ,  Trupta Purohit ,  EunGi Kim ,  Dong Chen

IPC: A61K47/64 ,  A61K9/00 ,  A61P35/02 ,  A61K38/45 ,  A61K31/454

Abstract: Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.