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：US20220081435A1

公开(公告)日：2022-03-17

申请号：US17420421

申请日：2019-12-19

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xin Han ,  Chao Wang ,  Chong Qin ,  Weiguo Xiang ,  Tianfeng Xu ,  Chao-Yie Yang

IPC: C07D417/14 ,  A61K47/55 ,  A61K45/06

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

公开(公告)号：US20190119289A1

公开(公告)日：2019-04-25

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

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：US11267822B2

公开(公告)日：2022-03-08

申请号：US16645953

申请日：2018-09-12

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Weiguo Xiang ,  Fuming Xu ,  Longchuan Bai ,  Ester Fernandez-Salas ,  Donna McEachern

IPC: C07D495/14 ,  C07D498/14 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Y, ═, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer.

公开(公告)号：US20190263827A1

公开(公告)日：2019-08-29

申请号：US16332544

申请日：2017-09-13

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yang Hu ,  Chong Qin ,  Fuming Xu ,  Jiantao Hu ,  Weiguo Xiang ,  Bing Zhou

IPC: C07D495/14 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, R4, Ar, L, X, Y, 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 degradation of BET bromodomains 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).