公开(公告)号：US12012467B2

公开(公告)日：2024-06-18

申请号：US16496974

申请日：2018-03-28

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Haibin Zhou ,  Jianfeng Lu ,  Liu Liu ,  Yi Sun ,  Denzil Bernard

IPC: A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K45/06 ,  C07D277/30 ,  C07D277/64 ,  C07D417/12 ,  C07K5/02 ,  C07K5/062 ,  C07K5/078 ,  C07K5/097 ,  C07K5/113 ,  C07K5/117 ,  C07K7/02

CPC classification number: C07K5/1021 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K45/06 ,  C07D277/30 ,  C07D277/64 ,  C07D417/12 ,  C07K5/02 ,  C07K5/021 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/0821 ,  C07K5/1024 ,  C07K7/02

Abstract: Compounds of formula (I) as inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

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：US20220185831A1

公开(公告)日：2022-06-16

申请号：US17442726

申请日：2020-03-27

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Haibin Zhou ,  Renqi Xu

IPC: C07F9/6561 ,  A61P35/00 ,  C07F9/6558

Abstract: The present disclosure provides compounds represented by Formulae I and IV: wherein R1a, R1b, R2a, R2b, A, E, QD, and QE are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are degraders of STAT3. Compounds of Formula IV are inhibitors of STAT3. STAT3 degraders and inhibitors are useful for the treatment of cancer and other diseases.

公开(公告)号：US20180289677A1

公开(公告)日：2018-10-11

申请号：US15949799

申请日：2018-04-10

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Haibin Zhou ,  Jianfeng Lu ,  Liu Liu ,  Jeanne Stuckey ,  Liangyou Rui ,  Yi Sun

IPC: A61K31/428 ,  A61P1/16

Abstract: Small molecule covalent inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 covalent inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

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.