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：US20140199234A1

公开(公告)日：2014-07-17

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: C07F9/6558 ,  A61K45/06 ,  A61K31/675

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：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：US10759808B2

公开(公告)日：2020-09-01

申请号：US16091544

申请日：2017-04-06

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yangbing Li ,  Angelo Aguilar ,  Bing Zhou ,  Jiantao Hu ,  Fuming Xu ,  Chong Qin ,  Yang Hu ,  Weiguo Xiang ,  Rohan Rej ,  Jiuling Yang ,  Xin Han ,  Longchuan Bai ,  Chao-Yie Yang

IPC: C07D401/04 ,  C07D487/10 ,  C07D401/14 ,  C07D487/04 ,  C07D495/14

Abstract: The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein X, L, Y, and B are as defined in the specification. Compounds having Formula I are immunomodulators and/or monofunctional synthetic intermediates that can be used to prepare small-molecule drug conjugates.

公开(公告)号：US20190169195A1

公开(公告)日：2019-06-06

申请号：US16093160

申请日：2017-04-06

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Bing Zhou ,  Fuming Xu ,  Jiantao Hu ,  Longchuan Bai ,  Chao-Yie Yang

IPC: C07D487/04 ,  A61P35/00 ,  C07K5/083

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein B, R1, R5, Q1, Q″, L, X, Y, and Z are as defined as set forth in the specification. The present disclosure also provids compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains 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.

公开(公告)号：US20240166647A1

公开(公告)日：2024-05-23

申请号：US18279225

申请日：2022-03-03

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Tianfeng Xu ,  Dimin Wu ,  Zhixiang Chen ,  Xin Han ,  Weiguo Xiang ,  Rohan Rej ,  Angelo Aguilar ,  Longchuan Bai

IPC: C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04 ,  C07D498/14

CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04 ,  C07D498/14

Abstract: The present disclosure provides compounds of Formula (I), wherein A, A1, A2, A3, R3, Z and Z1 are as defined in the specification, and the salts and solvates thereof. The present disclosure also relates to uses of the compounds as cereblon (CRBN) ubiquitination inhibitors, as synthetic intermediates that can be used to prepare PROTAC molecules, or as PROTAC molecules. The present disclosure also relates to uses of the compounds, e.g., in treating or preventing cancer and other diseases.

公开(公告)号：US20230159573A1

公开(公告)日：2023-05-25

申请号：US17911728

申请日：2021-03-26

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: C07F9/6561 ,  C07F9/6553

CPC classification number: C07F9/6561 ,  C07F9/655354

Abstract: The present disclosure provides compounds represented by Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R3a, R4, A, E1, E2, M, and Q are as set forth in the specification. Compounds of Formula (I) are STAT protein degraders and thus are useful for the treatment of cancer and other diseases.

公开(公告)号：US20210002289A1

公开(公告)日：2021-01-07

申请号：US17007191

申请日：2020-08-31

Applicant: The Regents of the University of Michigan

Inventor： Yangbing Li ,  Angelo Aguilar ,  Bing Zhou ,  Jiantao Hu ,  Fuming Xu ,  Chong Qin ,  Yang Hu ,  Weiguo Xiang ,  Rohan Rej ,  Jiuling Yang ,  Xin Han ,  Longchuan Bai ,  Chao-Yie Yang

IPC: C07D487/10 ,  C07D401/04 ,  C07D401/14 ,  C07D487/04 ,  C07D495/14

Abstract: The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein X, L, Y, and B are as defined in the specification. Compounds having Formula I are immunomodulators and/or monofunctional synthetic intermediates that can be used to prepare small-molecule drug conjugates.