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：US20210002277A1

公开(公告)日：2021-01-07

申请号：US17023426

申请日：2020-09-17

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

IPC: C07D471/04 ,  A61P35/02 ,  A61P35/00

Abstract: The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1, X2, X3 R1a, R1b, E, and are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer

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：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：US20190315741A1

公开(公告)日：2019-10-17

申请号：US16347630

申请日：2017-11-17

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Jianyong Chen ,  Liu Liu ,  Xuyuan Dong ,  Chao-Yie Yang ,  Donna McEachern ,  Shaomeng Wang

IPC: C07D471/04 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula (I), and the pharmaceutically acceptable salts and solvates thereof wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7, E and (B) 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 inhibition of ALK such as cancer. and (R)

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：US20180354950A1

公开(公告)日：2018-12-13

申请号：US16051816

申请日：2018-08-01

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

IPC: C07D471/04 ,  A61P35/00

CPC classification number: C07D471/04 ,  A61P35/00

Abstract: The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1, X2, X3 R1a, R1b, E, and are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein 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.