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.

公开(公告)号：US11324729B2

公开(公告)日：2022-05-10

申请号：US16213564

申请日：2018-12-07

Applicant: The Regents of the University of Michigan

Inventor： Tomasz Cierpicki ,  Jolanta Grembecka ,  Huang Huang ,  Sergei Zari ,  Hyo Je Cho ,  Mykhaylo Potopnyk ,  Sergii Dudkin ,  Wenbing Chen ,  Yassir Adam ,  Christina Howard ,  EunGi Kim

IPC: A61K31/428 ,  A61P35/00

Abstract: Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.

公开(公告)号：US20220017509A1

公开(公告)日：2022-01-20

申请号：US17159916

申请日：2021-01-27

Applicant: The Regents of the University of Michigan

Inventor： Alyssa Winkler ,  Brian Linhares ,  Dymytrii Listunov ,  Jolanta Grembecka ,  Tomasz Cierpicki ,  EunGi Kim

IPC: C07D417/14 ,  A61P35/00 ,  A61K47/55 ,  C07D409/06 ,  C07D409/14 ,  C07D487/10 ,  C07D495/04

Abstract: Provided herein are small molecules that bind to GAS41 and inhibit GAS41 activity, and methods of use thereof for the treatment of cancer.

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：US11858925B2

公开(公告)日：2024-01-02

申请号：US17159916

申请日：2021-01-27

Applicant: The Regents of the University of Michigan

Inventor： Alyssa Winkler ,  Brian Linhares ,  Dymytrii Listunov ,  Jolanta Grembecka ,  Tomasz Cierpicki ,  EunGi Kim

IPC: C07D417/14 ,  C07D495/04 ,  C07D409/14 ,  C07D487/10 ,  C07D409/06 ,  A61P35/00 ,  A61K47/55

CPC classification number: C07D417/14 ,  A61K47/55 ,  A61P35/00 ,  C07D409/06 ,  C07D409/14 ,  C07D487/10 ,  C07D495/04

Abstract: Provided herein are small molecules that bind to GAS41 and inhibit GAS41 activity, and methods of use thereof for the treatment of cancer.

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：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：US20230046569A1

公开(公告)日：2023-02-16

申请号：US17729836

申请日：2022-04-26

Applicant: The Regents of the University of Michigan

Inventor： Tomasz Cierpicki ,  Jolanta Grembecka ,  Huang Huang ,  Sergei Zari ,  Hyo Je Cho ,  Mykhaylo Potopnyk ,  Sergii Dudkin ,  Wenbing Chen ,  Yassir Adam ,  Christina Howard ,  EunGi Kim

IPC: A61K31/428 ,  A61P35/00

Abstract: Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.