公开(公告)号：US10253044B2

公开(公告)日：2019-04-09

申请号：US15443336

申请日：2017-02-27

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yujun Zhao ,  Bing Zhou ,  Angelo Aguilar ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Duxin Sun ,  Bo Wen ,  Ruijuan Luo ,  Ting Zhao ,  Arul Chinnaiyan ,  Irfan A. Asangani ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Xu Ran ,  Yang Hu

IPC: A61K31/519 ,  C07D519/00 ,  C07D487/04 ,  C07D487/14 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/538

Abstract: The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

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。

公开(公告)号：US09096625B2

公开(公告)日：2015-08-04

申请号：US14155809

申请日：2014-01-15

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianfang Chen ,  Donna McEachern ,  Longchuan Bai ,  Liu Liu ,  Duxin Sun ,  Xiaoqin Li ,  Angelo Aguilar

IPC: A61K31/675 ,  C07F9/6558 ,  A61K45/06 ,  A61K33/30

CPC classification number: C07F9/65583 ,  A61K31/675 ,  A61K33/30 ,  A61K45/06 ,  A61N5/10 ,  A61K2300/00

Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

Abstract translation: 公开了Bcl-2 / Bcl-xL的抑制剂及其组合物。 还公开了使用Bcl-2 / Bcl-xL抑制剂治疗其中Bcl-2 / Bcl-xL的抑制提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20130243874A1

公开(公告)日：2013-09-19

申请号：US13783563

申请日：2013-03-04

Applicant: IMRA of America, Inc. ,  The Regents of the University of Michigan

Inventor： Duxin Sun ,  Hongwei Chen ,  Masayuki Ito ,  Wei Qian ,  Yong Che

IPC: A61K47/02 ,  A61K9/14 ,  G01N21/47

CPC classification number: A61K47/02 ,  A61K9/143 ,  B22F1/0022 ,  B22F1/0062 ,  B82Y30/00 ,  G01N21/47

Abstract: The present provides amphiphilic block copolymer coated surfaces (e.g., nanoparticles, medical devices, etc.) and methods of preparing such surfaces. In certain embodiments, the present invention provides amphiphilic block copolymer coated single dispersed nanoparticles, which are stable in buffer (e.g., PBS) and have neutral but functionable surfaces, and methods of preparing the same.

Abstract translation: 本发明提供两亲嵌段共聚物涂覆表面（例如纳米颗粒，医疗装置等）和制备这种表面的方法。 在某些实施方案中，本发明提供了两性嵌段共聚物涂覆的单分散纳米颗粒，其在缓冲液（例如，PBS）中是稳定的并且具有中性但可功能的表面及其制备方法。

公开(公告)号：US11701433B2

公开(公告)日：2023-07-18

申请号：US16619802

申请日：2018-06-01

Applicant: The Regents of the University of Michigan

Inventor： Yu Lei ,  Yee Sun Tan ,  Kanokwan Sansanaphongpricha ,  Duxin Sun ,  Hongwei Chen ,  Hongxiang Hu

IPC: A61K9/00 ,  A61K47/69 ,  A61K47/64 ,  A61P35/00 ,  A61K39/00 ,  A61K39/02 ,  A61K39/118 ,  A61K39/385 ,  B82Y5/00

CPC classification number: A61K47/6929 ,  A61K39/0003 ,  A61K39/0011 ,  A61K39/02 ,  A61K39/118 ,  A61K39/385 ,  A61K47/643 ,  A61K47/646 ,  A61K47/6923 ,  A61P35/00 ,  A61K2039/55561 ,  A61K2039/572 ,  A61K2039/60 ,  A61K2039/622 ,  B82Y5/00

Abstract: The present invention provides methods, compositions, systems, and kits comprising nano-satellite complexes and/or serum albumin carrier complexes, which are used for modulating antigen-specific immune response (e.g., enhancing anti-tumor immunity). In certain embodiments, the nano-satellite complexes comprise: a) a core nanoparticle complex comprising a biocompatible coating surrounding a nanoparticle core; b) at least one satellite particle attached to, or absorbed to, the biocompatible coating; and c) an antigenic component conjugated to, or absorbed to, the at least one satellite particle component. In certain embodiments, the complexes further comprise: d) an type I interferon agonist agent. In some embodiments, the serum albumin complexes comprise: a) at least part of a serum albumin protein, b) an antigenic component conjugated to the carrier protein, and c) a type I interferon agonist agent.

公开(公告)号：US20200164094A1

公开(公告)日：2020-05-28

申请号：US16694715

申请日：2019-11-25

Applicant: The Regents of the University of Michigan

Inventor： Hongwei Chen ,  Duxin Sun

IPC: A61K49/18 ,  A61K41/00 ,  G01R33/56 ,  G01R33/48

Abstract: The present invention provides methods, compositions, systems, and kits comprising core-satellite nanocomposites useful for photothermal and/or MRI applications (e.g., tumor treatment and/or imaging). In certain embodiments, the core-satellite nanocomposites comprise: i) a core nanoparticle complex comprising a biocompatible coating surrounding a nanoparticle core, and ii) at least one satellite component attached to, or absorbed to, the biocompatible coating. In some embodiments, the nanoparticle core and satellite component are composed of near-infrared photothermal agent material and/or MRI contrast agent material. In further embodiments, the satellite component is additionally or alternatively composed of near-infrared optical dye material.

公开(公告)号：US10391175B2

公开(公告)日：2019-08-27

申请号：US15619671

申请日：2017-06-12

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xu Ran ,  Yujun Zhao ,  Chao-Yie Yang ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Duxin Sun ,  Xiaoqin Li ,  Bing Zhou ,  Hacer Karatas ,  Ruijuan Luo ,  Arul Chinnaiyan ,  Irfan A. Asangani

IPC: A61K31/519 ,  C07D471/04 ,  A61K45/06 ,  C07D487/04 ,  C07D491/056

Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

公开(公告)号：US10246464B2

公开(公告)日：2019-04-02

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 ,  C07F9/53 ,  C07F9/6558

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.