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：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：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：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：US20220396587A1

公开(公告)日：2022-12-15

申请号：US17048688

申请日：2020-01-22

Applicant: ASCENTAGE PHARMA (SUZHOU) CO., LTD. ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  ASCENTAGE PHARMA GROUP CORP LIMITED

Inventor： Guozhi Tang ,  Dongbo Li ,  Liugen Li ,  Xianchan Zha ,  Wenming Chen ,  Shaomeng Wang ,  Chao-Yie Yang

IPC: C07D515/22 ,  C07D497/22 ,  A61P35/00

Abstract: Provided are compounds represented by Formula IA: (IA), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R1a, R1b, L1, L2, L3, X, A, B and C are as defined as set forth in the specification. Also provided compounds of Formula IA for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

公开(公告)号：US20220356192A1

公开(公告)日：2022-11-10

申请号：US17227641

申请日：2021-04-12

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 ,  C07K5/06 ,  A61K45/06

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：US11168082B2

公开(公告)日：2021-11-09

申请号：US16611238

申请日：2018-05-15

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Dengyou Zhang ,  Canhui Zheng ,  Zhuo Chen ,  Liu Liu ,  Liyue Huang ,  Chao-Yie Yang

IPC: C07D471/04 ,  A61P35/00 ,  C07D519/00

Abstract: The present disclosure provides compounds represented by Formula I and II: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, X, W, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I and II for use to treat a condition or disorder responsive to LSD1 inhibition such as cancer.

公开(公告)号：US11110090B2

公开(公告)日：2021-09-07

申请号：US16914518

申请日：2020-06-29

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

IPC: A61K31/506 ,  C07D405/14 ,  C07D401/12 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 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.

公开(公告)号：US11046703B2

公开(公告)日：2021-06-29

申请号：US16594344

申请日：2019-10-07

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Angelo Aguilar ,  Yangbing Li ,  Jiuling Yang ,  Donna McEachern

IPC: C07D487/10

Abstract: The present disclosure provides compounds represented by Formula I: wherein R1a, R1b, R2a, R2b, R3a, R3b, R4, A, L, X, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to degradation of MDM2 protein.