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.

公开(公告)号：US20190092784A1

公开(公告)日：2019-03-28

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: C07D495/04 ,  A61P35/00

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：US10160769B2

公开(公告)日：2018-12-25

申请号：US15296842

申请日：2016-10-18

Applicant: The Regents of the University of Michigan

Inventor： Jolanta Grembecka ,  Tomasz Cierpicki ,  Dmitry Borkin ,  Jay L. Hess ,  Duxin Sun ,  Xiaoqin Li ,  Kevin Greenman ,  Mohamed Ibrahim ,  Artem Plekhov

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

公开(公告)号：US20170247391A1

公开(公告)日：2017-08-31

申请号：US15509989

申请日：2015-09-08

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

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

IPC: C07D495/04 ,  C07D519/00 ,  C07F9/6558

CPC classification number: C07D495/04 ,  C07D519/00 ,  C07F9/5325 ,  C07F9/65583

Abstract: 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：US20160137665A1

公开(公告)日：2016-05-19

申请号：US14937421

申请日：2015-11-10

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 ,  C07D519/00

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 2: 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2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。