公开(公告)号：US11192898B2

公开(公告)日：2021-12-07

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 ,  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：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：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：US20210236474A1

公开(公告)日：2021-08-05

申请号：US17052626

申请日：2019-05-13

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Rohan Rej

IPC: A61K31/4545 ,  C07D471/04 ,  A61K31/437 ,  A61K31/538 ,  A61K31/55 ,  C07D519/00 ,  A61K31/439

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, and R4 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 LSD1 inhibition such as cancer.

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.

公开(公告)号：US12145944B2

公开(公告)日：2024-11-19

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: A61K31/277 ,  A61K45/06 ,  A61P35/00 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D491/22 ,  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：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：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：US11944614B2

公开(公告)日：2024-04-02

申请号：US17052626

申请日：2019-05-13

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Rohan Rej

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/538 ,  A61K31/55 ,  C07D519/00

CPC classification number: A61K31/4545 ,  A61K31/437 ,  A61K31/439 ,  A61K31/538 ,  A61K31/55 ,  C07D471/04 ,  C07D519/00

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, and R4 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 LSD1 inhibition such as cancer.

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.