公开(公告)号：US11633490B2

公开(公告)日：2023-04-25

申请号：US17468308

申请日：2021-09-07

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 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K35/02 ,  A61K38/45 ,  C07D309/24 ,  C07D471/04 ,  A61K9/00 ,  A61P35/02 ,  A61K47/54 ,  C07D209/24

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：US11110177B2

公开(公告)日：2021-09-07

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 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K35/02 ,  A61K38/45 ,  C07D309/24 ,  C07D471/04 ,  A61K9/00 ,  A61P35/02 ,  A61K47/54 ,  C07D209/24

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：US20190144442A1

公开(公告)日：2019-05-16

申请号：US16186018

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

IPC: C07D471/04 ,  A61K9/00 ,  A61P35/02 ,  A61K31/4545 ,  A61K31/454 ,  C07D209/24 ,  A61K31/404

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：US12285490B2

公开(公告)日：2025-04-29

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：US11883381B2

公开(公告)日：2024-01-30

申请号：US16300421

申请日：2017-05-12

Applicant: The Regents of the University of Michigan

Inventor： Jolanta Grembecka ,  Tomasz Cierpicki ,  David Rogawski ,  Dmitry Borkin ,  Szymon Klossowski ,  Zhuang Jin ,  Deanna Montgomery ,  Jing Deng ,  Marta Krotoska ,  Hao Li

IPC: A61K31/404 ,  A61K45/06 ,  C07D209/18 ,  C07D209/08 ,  A61P35/02

CPC classification number: A61K31/404 ,  A61K45/06 ,  A61P35/02 ,  C07D209/08 ,  C07D209/18

Abstract: Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation 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：US11833210B2

公开(公告)日：2023-12-05

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

CPC classification number: A61K47/64 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K38/45 ,  A61K47/545 ,  A61K47/556 ,  A61P35/02 ,  C07D209/24 ,  C07D471/04 ,  C12Y203/02

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：US20220072142A1

公开(公告)日：2022-03-10

申请号：US17468308

申请日：2021-09-07

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 ,  A61K31/454 ,  A61K38/45 ,  A61P35/02 ,  A61K47/54 ,  A61K31/404 ,  A61K31/4545 ,  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：US20200246474A1

公开(公告)日：2020-08-06

申请号：US16854527

申请日：2020-04-21

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

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：US11786602B2

公开(公告)日：2023-10-17

申请号：US17468308

申请日：2021-09-07

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 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K35/02 ,  A61K38/45 ,  C07D309/24 ,  C07D471/04 ,  A61K9/00 ,  A61P35/02 ,  A61K47/54 ,  C07D209/24

CPC classification number: A61K47/64 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K38/45 ,  A61K47/545 ,  A61K47/556 ,  A61P35/02 ,  C07D209/24 ,  C07D471/04 ,  C12Y203/02

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：US11147885B2

公开(公告)日：2021-10-19

申请号：US16854527

申请日：2020-04-21

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

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.