公开(公告)号：US20230218765A1

公开(公告)日：2023-07-13

申请号：US17924794

申请日：2021-05-19

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Mingliang Wang ,  Jianfeng Lu ,  Mi Wang

IPC: A61K47/54 ,  A61K47/55 ,  A61P35/00

CPC classification number: A61K47/545 ,  A61K47/55 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein R1, R3, L, Y, and B1 are as defined in the specification. Compounds having Formula I are SHP2 protein degraders useful for the treatment of cancer and other diseases.

公开(公告)号：US11498928B2

公开(公告)日：2022-11-15

申请号：US17049100

申请日：2020-01-17

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

Inventor： Jianyong Chen ,  Yunlong Zhou ,  Guozhi Tang ,  Chengzhe Wu ,  Leilei Zhao ,  Lingling Jiao ,  Binghua Sheng ,  Shaomeng Wang ,  Chao-Yie Yang ,  Hao Chen ,  Wenliang Hu ,  Yu Jing

IPC: C07D513/20 ,  C07D515/20 ,  C07D498/08 ,  A61K31/553 ,  A61P35/00 ,  C07D513/10 ,  C07D519/00

Abstract: Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R8, R9a, R9b, R9c, R9d, X, Y, Z, Z1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

公开(公告)号：US20220340595A1

公开(公告)日：2022-10-27

申请号：US17047423

申请日：2019-11-20

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

Inventor： Hao Chen ,  Wenming Chen ,  Chao Li ,  Dongbo Li ,  Yu Jing ,  Guozhi Tang ,  Yunlong Zhou ,  Shaomeng Wang ,  Chao-Yie Yang

IPC: C07D515/22 ,  A61P35/00

Abstract: Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R1a, R1b, R1h, L2, L3, #, #, # are as defined as set forth in the re) specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

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：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：US20220079931A1

公开(公告)日：2022-03-17

申请号：US17420417

申请日：2019-12-19

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jiantao Hu ,  Biao Hu ,  Mingliang Wang ,  Fuming Xu ,  Bukeyan Miao

IPC: A61K31/454 ,  A61K31/381 ,  A61K47/54 ,  A61K31/427 ,  A61K31/40 ,  A61P35/00 ,  A61K31/337 ,  A61K31/566 ,  A61K31/7068 ,  A61K31/704 ,  A61K31/513 ,  A61K31/475 ,  A61K31/138 ,  A61K31/519 ,  A61K31/565

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

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：US20210198237A1

公开(公告)日：2021-07-01

申请号：US17101323

申请日：2020-11-23

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Angelo Aguilar ,  Ke Zheng ,  Shilin Xu ,  Tianfeng Xu ,  Denzil Bernard ,  Liyue Huang

IPC: C07D401/14 ,  C07D401/04 ,  C07D405/04 ,  C07D211/34 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R2, R3a, R3b, A, G, X, and Y 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 menin inhibition such as cancer.

公开(公告)号：US11046709B2

公开(公告)日：2021-06-29

申请号：US16481501

申请日：2018-02-02

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jiantao Hu ,  Fuming Xu

IPC: C07D498/12 ,  C07D498/04 ,  C07D495/14 ,  C07D487/04

Abstract: The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.

公开(公告)号：US20210130401A1

公开(公告)日：2021-05-06

申请号：US16605057

申请日：2018-05-15

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yangbing Li ,  Hacer Karatas ,  Liu Liu ,  Jeanne Stuckey ,  Yali Dou ,  Liyue Huang ,  Atsunori Kaneshige

IPC: C07K5/11 ,  A61K38/07 ,  A61K45/06

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3a, R3b, R4a, R4b, R5a and R5b are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition, disease, or disorder responsive to inhibition of the WDR5 interaction with its binding partners including, but not limited to, the WDR5-MLL protein-protein interaction.