公开(公告)号：US09580430B2

公开(公告)日：2017-02-28

申请号：US14633360

申请日：2015-02-27

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: A01N43/54 ,  A61K31/505 ,  C07D491/00 ,  C07D487/04 ,  A61K31/519 ,  C07D487/14 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  C07D487/14

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.

Abstract translation: 本公开提供取代的9H-嘧啶并[4,5-b]吲哚和5H-吡啶并[4,3-b]吲哚和由式I表示的相关类似物及其药学上可接受的盐，水合物和溶剂合物，其中R1a A，B1，B2，G，X1，Y1，Y2和Y3如说明书中所述。 本公开还涉及式I化合物用于治疗对抑制BET溴结构域有反应的病症或病症。 本公开的化合物特别可用于治疗癌症。

公开(公告)号：US09394303B2

公开(公告)日：2016-07-19

申请号：US14678267

申请日：2015-04-03

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Zaneta Nikolovska-Coleska ,  Fardokht Abulwerdi ,  Hollis Showalter ,  Lei Miao ,  Jeanne Stuckey ,  Ahmed Mady

IPC: C07D401/14 ,  A61K31/437 ,  C07D471/04 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10

CPC classification number: C07D471/04 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.

Abstract translation: 本发明在医药化学领域。 特别地，本发明涉及一类新颖的具有吡唑并吡啶结构的小分子，其作为Mcl-1蛋白的抑制剂，其用作治疗癌症和其它疾病的治疗剂。

公开(公告)号：US20140256706A1

公开(公告)日：2014-09-11

申请号：US14204076

申请日：2014-03-11

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: A61K31/5377 ,  A61K31/437 ,  A61K45/06 ,  C07D471/04 ,  C07D491/056 ,  A61K31/519 ,  C07D487/04

CPC classification number: A61K45/06 ,  C07D471/04 ,  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.

Abstract translation: 公开了BET溴结构域的抑制剂和含有它们的组合物。 还公开了使用BET溴域结构域抑制剂治疗其中抑制BET溴结构域提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20250034162A1

公开(公告)日：2025-01-30

申请号：US18887703

申请日：2024-09-17

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Rohan Rej ,  Changwei Wang ,  Mi Wang ,  Jianfeng Lu ,  Chao-Yie Yang ,  Ester Fernandez-Salas ,  Jeanne Stuckey

IPC: C07D491/22 ,  A61K45/06 ,  A61P35/00 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D495/14 ,  C07D495/22 ,  C07D498/22 ,  C07D513/22 ,  C07F9/6561

Abstract: The present disclosure provides compounds represented by Formula I: wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are EED inhibitors. EED inhibitors are useful for the treatment of cancer and other diseases.

公开(公告)号：US20230083015A1

公开(公告)日：2023-03-16

申请号：US17442666

申请日：2020-03-26

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Haibin Zhou ,  Renqi Xu ,  Longchuan Bai ,  Donna McEachern ,  Jeanne Stuckey ,  Chao-Yie Yang

IPC: C07F9/38 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I or Formula VIII: wherein R1a, R1b, M, A, E, QA, and QB are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are degraders of STAT3 or degraders of STAT3 and STAT1. Compounds of Formula VIII are inhibitors of STAT3. STAT3 degraders and inhibitors are useful for the treatment of cancer and other diseases.

公开(公告)号：US20220227778A1

公开(公告)日：2022-07-21

申请号：US16971472

申请日：2020-07-16

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Rohan Rej ,  Changwei Wang ,  Mi Wang ,  Jianfeng Lu ,  Chao-Yie Yang ,  Ester Fernandez-Salas ,  Jeanne Stuckey

IPC: C07D491/22 ,  C07D487/14 ,  C07D471/22 ,  C07D495/14 ,  C07D495/22 ,  C07D513/22 ,  C07D487/04 ,  C07F9/6561 ,  C07D498/22 ,  A61P35/00 ,  A61K45/06

Abstract: The present disclosure provides compounds represented by Formula I: wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are EED inhibitors. EED inhibitors are useful for the treatment of cancer and other diseases.

公开(公告)号：US20200022953A1

公开(公告)日：2020-01-23

申请号：US16497856

申请日：2018-03-30

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Angelo Aguilar ,  Shilin Xu ,  Liyue Huang ,  Jeanne Stuckey ,  Tianfeng Xu

IPC: A61K31/397 ,  C07D401/14 ,  C07D401/06 ,  C07D413/14 ,  C07D401/12 ,  C07D205/04 ,  A61K31/4523 ,  A61K31/4709 ,  A61K31/454 ,  A61K31/5377

Abstract: The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, R1a, R1b, R1c, R1d, R2, R3, R8a, R8b, R10, X, Z2, m, and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer.

公开(公告)号：US20170281773A1

公开(公告)日：2017-10-05

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: A61K45/06 ,  C07D487/04 ,  C07D471/04 ,  C07D491/056

CPC classification number: A61K45/06 ,  C07D471/04 ,  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：US09675697B2

公开(公告)日：2017-06-13

申请号：US14204076

申请日：2014-03-11

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

CPC classification number: A61K45/06 ,  C07D471/04 ,  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.