公开(公告)号：US20220411432A1

公开(公告)日：2022-12-29

申请号：US17462355

申请日：2021-08-31

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yangbing Li ,  Jiuling Yang ,  Angelo Aguilar ,  Bing Zhou ,  Jiantao Hu ,  Fuming Xu ,  Rohan Rej ,  Xin Han

IPC: C07D487/10 ,  C07D401/04 ,  A61P35/00 ,  C07D401/14 ,  C07D417/14

Abstract: The present disclosure provides compounds represented by Formula I-A: A1-L1-B1  I-A and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein A1, B1, and L1 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 protein such as cancer.

公开(公告)号：US20230257365A1

公开(公告)日：2023-08-17

申请号：US18012369

申请日：2021-07-09

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xin Han ,  Weiguo Xiang ,  Chong Qin ,  Tianfeng Xu ,  Lijie Zhao

IPC: C07D401/14 ,  C07D451/06 ,  C07D451/14 ,  C07D519/00 ,  C07D487/04 ,  C07D487/10 ,  C07D471/04 ,  C07D491/08

CPC classification number: C07D401/14 ,  C07D451/06 ,  C07D451/14 ,  C07D519/00 ,  C07D487/04 ,  C07D487/10 ,  C07D471/04 ,  C07D491/08

Abstract: The present disclosure provides compounds represented by Formula I: A-L-B1 I, and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification. Compounds having Formula I are androgen receptor degraders useful for the treatment of cancer and other diseases.

公开(公告)号：US20230233690A1

公开(公告)日：2023-07-27

申请号：US18012267

申请日：2021-07-09

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xin Han ,  Weiguo Xiang ,  Chong Qin ,  Lijie Zhao

IPC: A61K47/55 ,  A61K47/54

CPC classification number: A61K47/55 ,  A61K47/545

Abstract: The present disclosure provides compounds represented by Formula I: A-L-B1 and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification. Compounds having Formula I are androgen receptor degraders 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：US20240190874A1

公开(公告)日：2024-06-13

申请号：US18279229

申请日：2022-03-03

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Lijie Zhao ,  Xin Han ,  Weiguo Xiang

IPC: C07D471/10 ,  A61K31/438

CPC classification number: C07D471/10 ,  A61K31/438

Abstract: The present disclosure provides compounds of Formula (I): and the salts or solvates thereof, wherein A1, B1, L, and X2 are as defined in the specification. The present disclosure also relates to uses of the compounds, e.g., as androgen receptor degraders useful for the treatment of diseases (e.g., cancer).

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：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.

公开(公告)号：US20230357249A1

公开(公告)日：2023-11-09

申请号：US17924242

申请日：2021-05-14

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xin Han ,  Weiguo Xiang ,  Chong Qin ,  Tianfeng Xu ,  Lijie Zhao ,  Mingliang Wang ,  Rohan Rej

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present disclosure provides compounds represented by Formula I : A-L-B 1 I, and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification, ompounds having Formula I are androgen receptor degraders useful for the treatment of ancer and other diseases.

公开(公告)号：US20220380368A1

公开(公告)日：2022-12-01

申请号：US17760786

申请日：2020-09-18

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xin Han ,  Weiguo Xiang ,  Bukeyan Miao ,  Chong Qin ,  Lijie Zhao ,  Jianfeng Lu ,  Tianfeng Xu ,  Chao-Yie Yang

IPC: C07D471/10 ,  A61P35/00 ,  A61P13/08

Abstract: The present disclosure provides compounds represented by Formula (I) and the salts or solvates thereof, wherein R3a, E, L, A1, B1, X1, X2, Z1, and Z2 are as defined in the specification. Compounds having Formula (I) are androgen receptor degraders useful for the treatment of cancer and other diseases.

公开(公告)号：US20190127387A1

公开(公告)日：2019-05-02

申请号：US16091541

申请日：2017-04-06

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yangbing Li ,  Jiuling Yang ,  Angelo Aguilar ,  Bing Zhou ,  Jiantao Hu ,  Fuming Xu ,  Rohan Rej ,  Xin Han

IPC: C07D487/10 ,  C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I-A: A1-L1-B1 I-A and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein A1, B1, and L1 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 protein such as cancer.