公开(公告)号：US20190144442A1

公开(公告)日：2019-05-16

申请号：US16186018

申请日：2018-11-09

申请人： The Regents of the University of Michigan

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

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

摘要： 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：US11833210B2

公开(公告)日：2023-12-05

申请号：US17504159

申请日：2021-10-18

申请人： The Regents of the University of Michigan

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

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

CPC分类号： 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

摘要： 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

申请人： The Regents of the University of Michigan

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

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

摘要： 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

申请人： The Regents of the University of Michigan

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

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

摘要： 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：USRE49687E1

公开(公告)日：2023-10-10

申请号：US17165794

申请日：2021-02-02

申请人： The Regents of The University of Michigan ,  Kura Oncology, Inc.

发明人： Jolanta Grembecka ,  Tomasz Cierpicki ,  Dmitry Borkin ,  Jonathan Pollock ,  Hongzhi Miao ,  Duxin Sun ,  Liansheng Li ,  Tao Wu ,  Jun Feng ,  Pingda Ren ,  Yi Liu

IPC分类号： C07D495/04 ,  C07D519/00 ,  C07F9/53 ,  C07F9/6558

CPC分类号： C07D495/04 ,  C07D519/00 ,  C07F9/5325 ,  C07F9/65583

摘要： The present disclosure provides compounds and methods for inhibiting the interaction of menin with its upstream or downstream signaling molecules including but not limited to MLL1, MLL2 and MLL-fusion oncoproteins. Compounds of the disclosure may be used in methods for the treatment of a wide variety of cancers and other diseases associated with one or more of MLL1, MLL2, MLL fusion proteins, and menin.

公开(公告)号：US20220288217A1

公开(公告)日：2022-09-15

申请号：US17504159

申请日：2021-10-18

申请人： The Regents of the University of Michigan

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

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

摘要： 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

申请人： The Regents of the University of Michigan

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

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

摘要： 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：US11633490B2

公开(公告)日：2023-04-25

申请号：US17468308

申请日：2021-09-07

申请人： The Regents of the University of Michigan

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

IPC分类号： A61K47/64 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K35/02 ,  A61K38/45 ,  C07D309/24 ,  C07D471/04 ,  A61K9/00 ,  A61P35/02 ,  A61K47/54 ,  C07D209/24

摘要： 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

申请人： The Regents of the University of Michigan

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

IPC分类号： A61K47/64 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4545 ,  A61K35/02 ,  A61K38/45 ,  C07D309/24 ,  C07D471/04 ,  A61K9/00 ,  A61P35/02 ,  A61K47/54 ,  C07D209/24

摘要： 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：US10246464B2

公开(公告)日：2019-04-02

申请号：US15509989

申请日：2015-09-08

申请人： The Regents of the University of Michigan ,  Kura Oncology, Inc

发明人： Jolanta Grembecka ,  Tomasz Cierpicki ,  Dmitry Borkin ,  Jonathan Pollock ,  Hongzhi Miao ,  Duxin Sun ,  Liansheng Li ,  Tao Wu ,  Jun Feng ,  Pingda Ren ,  Yi Liu

IPC分类号： C07D495/04 ,  C07D519/00 ,  C07F9/53 ,  C07F9/6558

摘要： The present disclosure provides compounds and methods for inhibiting the interaction of menin with its upstream or downstream signaling molecules including but not limited to MLL1, MLL2 and MLL-fusion oncoproteins. Compounds of the disclosure may be used in methods for the treatment of a wide variety of cancers and other diseases associated with one or more of MLL1, MLL2, MLL fusion proteins, and menin.