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：US20190092783A1

公开(公告)日：2019-03-28

申请号：US16082645

申请日：2017-03-15

Applicant: Kura Oncology, Inc. ,  The Regents of The University of Michigan

Inventor： Tao Wu ,  Liansheng Li ,  Yi Wang ,  Pingda Ren ,  Jolanta Grembecka ,  Tomasz Cierpicki ,  Szymon Klossowski ,  Jonathan Pollock ,  Dmitry Borkin

IPC: C07D495/04 ,  A61P35/02

Abstract: 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：US09216993B2

公开(公告)日：2015-12-22

申请号：US14203233

申请日：2014-03-10

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

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

IPC: C07D495/04 ,  C07D495/16

CPC classification number: C07D495/04 ,  C07D495/16 ,  C07D519/00

Abstract: 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.

Abstract translation: 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：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：US11542248B2

公开(公告)日：2023-01-03

申请号：US16619423

申请日：2018-06-07

Applicant: KURA ONCOLOGY, INC. ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN

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

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

Abstract: 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：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：US10781218B2

公开(公告)日：2020-09-22

申请号：US16082649

申请日：2017-03-15

Applicant: Kura Oncology, Inc. ,  The Regents of The University of Michigan

Inventor： Tao Wu ,  Liansheng Li ,  Yi Wang ,  Pingda Ren ,  Jolanta Grembecka ,  Tomasz Cierpicki ,  Szymon Klossowski ,  Jonathan Pollock ,  Dmitry Borkin

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

Abstract: 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

Applicant: Kura Oncology, Inc. ,  The Regents of The University of Michigan

Inventor： Tao Wu ,  Liansheng Li ,  Yi Wang ,  Pingda Ren ,  Jolanta Grembecka ,  Tomasz Cierpicki ,  Szymon Klossowski ,  Jonathan Pollock ,  Dmitry Borkin

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

Abstract: 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.