公开(公告)号：US11542248B2

公开(公告)日：2023-01-03

申请号：US16619423

申请日：2018-06-07

申请人： KURA ONCOLOGY, INC. ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN

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

IPC分类号： C07D401/14 ,  A61P35/00 ,  C07D207/32 ,  C07D413/14 ,  C07D417/14 ,  C07K14/47 ,  A61K9/00 ,  A61K38/00

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.

公开(公告)号：US10781218B2

公开(公告)日：2020-09-22

申请号：US16082649

申请日：2017-03-15

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

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： A61K31/519 ,  C07D495/04 ,  A61P35/00

摘要： The present disclosure provides compounds of Formula (II-A), which inhibit the interaction of menin with one or more of MLL1, MLL2 and MLL-fusion oncoproteins. Also disclosed are methods for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.

公开(公告)号：US10752639B2

公开(公告)日：2020-08-25

申请号：US16082645

申请日：2017-03-15

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

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： A61K31/519 ,  C07D495/04 ,  A61K31/445 ,  A61P35/02

摘要： The present disclosure provides compounds of Formula (I-E) for inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compounds 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.

公开(公告)号：US20190092784A1

公开(公告)日：2019-03-28

申请号：US16082649

申请日：2017-03-15

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

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 ,  A61P35/00

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.

公开(公告)号：US20170247391A1

公开(公告)日：2017-08-31

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 ,  C07F9/6558

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：US09216993B2

公开(公告)日：2015-12-22

申请号：US14203233

申请日：2014-03-10

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

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。

公开(公告)号：US20170253611A1

公开(公告)日：2017-09-07

申请号：US15296842

申请日：2016-10-18

申请人： The Regents of the University of Michigan

发明人： Jolanta Grembecka ,  Tomasz Cierpicki ,  Dmitry Borkin ,  Jay L. Hess ,  Duxin Sun ,  Xiaoqin Li

IPC分类号： C07D495/04 ,  C07D495/16 ,  C07D519/00

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 3: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.

公开(公告)号：US20160046647A1

公开(公告)日：2016-02-18

申请号：US14773686

申请日：2014-03-10

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Jolanta Grembecka ,  Tomasz Cierpicki ,  Dmitry Borkin ,  Jay Hess ,  Duxin Sun ,  Xiaoqin Li

IPC分类号： C07D495/04

CPC分类号： C07D495/04 ,  C07D495/16 ,  C07D519/00

摘要： The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine and thienopyridine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin).

摘要翻译： 本发明一般涉及噻吩并嘧啶和噻吩并吡啶类化合物及其使用方法。 在具体实施方案中，本发明提供了包含噻吩并嘧啶和噻吩并吡啶类化合物的组合物和用于抑制menin与MLL1，MLL2和MLL-融合癌蛋白相互作用的方法（例如，用于治疗白血病，固体癌症和依赖于 MLL1，MLL2，MLL融合蛋白和/或menin的活性）。

公开(公告)号：US11883381B2

公开(公告)日：2024-01-30

申请号：US16300421

申请日：2017-05-12

申请人： The Regents of the University of Michigan

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

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

CPC分类号： A61K31/404 ,  A61K45/06 ,  A61P35/02 ,  C07D209/08 ,  C07D209/18

摘要： 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：US09505781B2

公开(公告)日：2016-11-29

申请号：US14773686

申请日：2014-03-10

申请人： The Regents of the University of Michigan

发明人： Jolanta Grembecka ,  Tomasz Cierpicki ,  Dmitry Borkin ,  Jay Hess ,  Duxin Sun ,  Xiaoqin Li

IPC分类号： C07D495/04 ,  C07D519/00 ,  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 4b: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.