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公开(公告)号：US11786602B2
公开(公告)日：2023-10-17
申请号：US17468308
申请日：2021-09-07
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
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 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.
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公开(公告)号：US11147885B2
公开(公告)日：2021-10-19
申请号：US16854527
申请日：2020-04-21
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 , A61K31/454 , A61K31/404 , A61K47/64 , A61K9/00 , A61K38/45 , A61P35/02 , A61K47/54 , C07D209/24
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.
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公开(公告)号：US20230046569A1
公开(公告)日：2023-02-16
申请号：US17729836
申请日：2022-04-26
发明人： Tomasz Cierpicki , Jolanta Grembecka , Huang Huang , Sergei Zari , Hyo Je Cho , Mykhaylo Potopnyk , Sergii Dudkin , Wenbing Chen , Yassir Adam , Christina Howard , EunGi Kim
IPC分类号： A61K31/428 , A61P35/00
摘要： 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.
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公开(公告)号：US20220288217A1
公开(公告)日：2022-09-15
申请号：US17504159
申请日：2021-10-18
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.
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公开(公告)号：US20190142961A1
公开(公告)日：2019-05-16
申请号：US16186012
申请日：2018-11-09
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.
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公开(公告)号：US11324729B2
公开(公告)日：2022-05-10
申请号：US16213564
申请日：2018-12-07
发明人： Tomasz Cierpicki , Jolanta Grembecka , Huang Huang , Sergei Zari , Hyo Je Cho , Mykhaylo Potopnyk , Sergii Dudkin , Wenbing Chen , Yassir Adam , Christina Howard , EunGi Kim
IPC分类号： A61K31/428 , A61P35/00
摘要： 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.
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公开(公告)号：US20220017509A1
公开(公告)日：2022-01-20
申请号：US17159916
申请日：2021-01-27
发明人： Alyssa Winkler , Brian Linhares , Dymytrii Listunov , Jolanta Grembecka , Tomasz Cierpicki , EunGi Kim
IPC分类号： C07D417/14 , A61P35/00 , A61K47/55 , C07D409/06 , C07D409/14 , C07D487/10 , C07D495/04
摘要： Provided herein are small molecules that bind to GAS41 and inhibit GAS41 activity, and methods of use thereof for the treatment of cancer.
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公开(公告)号：US20190144442A1
公开(公告)日：2019-05-16
申请号：US16186018
申请日：2018-11-09
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.
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公开(公告)号：US11858925B2
公开(公告)日：2024-01-02
申请号：US17159916
申请日：2021-01-27
发明人： Alyssa Winkler , Brian Linhares , Dymytrii Listunov , Jolanta Grembecka , Tomasz Cierpicki , EunGi Kim
IPC分类号： C07D417/14 , C07D495/04 , C07D409/14 , C07D487/10 , C07D409/06 , A61P35/00 , A61K47/55
CPC分类号： C07D417/14 , A61K47/55 , A61P35/00 , C07D409/06 , C07D409/14 , C07D487/10 , C07D495/04
摘要： Provided herein are small molecules that bind to GAS41 and inhibit GAS41 activity, and methods of use thereof for the treatment of cancer.
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公开(公告)号：US11633490B2
公开(公告)日：2023-04-25
申请号：US17468308
申请日：2021-09-07
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.
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