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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：US20190092783A1
公开(公告)日：2019-03-28
申请号：US16082645
申请日：2017-03-15
发明人： Tao Wu , Liansheng Li , Yi Wang , Pingda Ren , Jolanta Grembecka , Tomasz Cierpicki , Szymon Klossowski , Jonathan Pollock , Dmitry Borkin
IPC分类号： C07D495/04 , A61P35/02
摘要： The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.
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5.发明授权Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof 有权包含噻吩并嘧啶和噻吩并吡啶化合物的组合物及其使用方法公开(公告)号：US09216993B2
公开(公告)日：2015-12-22
申请号：US14203233
申请日：2014-03-10
发明人： Jolanta Grembecka , Tomasz Cierpicki , Dmitry Borkin , Jay L. Hess , Duxin Sun , Xiaoqin Li
IPC分类号： C07D495/04 , C07D495/16
CPC分类号： C07D495/04 , C07D495/16 , C07D519/00
摘要： The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 4: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.
摘要翻译： 本公开一般涉及噻吩并嘧啶和噻吩并吡啶化合物及其使用方法。 在具体实施方案中，本公开提供了包含式4的噻吩并嘧啶和噻吩并吡啶化合物的组合物：以及用于抑制menin与MLL1，MLL2和MLL-融合癌蛋白相互作用的方法。
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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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公开(公告)号：US11110177B2
公开(公告)日：2021-09-07
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 , 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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公开(公告)号：US10246464B2
公开(公告)日：2019-04-02
申请号：US15509989
申请日：2015-09-08
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.
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公开(公告)号：US20180327414A1
公开(公告)日：2018-11-15
申请号：US16014996
申请日：2018-06-21
发明人： Jolanta Grembecka , Tomasz Cierpicki , Dmitry Borkin , Jonathan Pollock , Liansheng Li , Tao Wu , Jun Feng , Pingda Ren , Yi Liu , Szymon Klossowski
IPC分类号： C07D487/04 , C07D519/00 , C07D513/04 , C07D498/04 , C07D473/34 , C07D491/048 , C07D495/04
CPC分类号： C07D487/04 , C07D473/34 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
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