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：US11548899B2

公开(公告)日：2023-01-10

申请号：US16077844

申请日：2017-02-15

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Bing Zhou ,  Yang Hu ,  Chao-Yie Yang ,  Chong Qin

IPC: C07D495/14 ,  C07D498/14 ,  C07D498/04 ,  A61K45/06 ,  A61P35/04

Abstract: The present disclosure provides fused 1,4-oxazepines and related analogs represented by Formula (I) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, A, and Y are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer.

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：US11466028B2

公开(公告)日：2022-10-11

申请号：US16332533

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 ,  Bing Zhou ,  Zhuo Chen ,  Ester Fernandez-Salas ,  Longchuan Bai ,  Donna McEachern

IPC: C07D498/14 ,  A61P35/02 ,  A61P35/04

Abstract: The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, 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：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：US20210309666A1

公开(公告)日：2021-10-07

申请号：US17342974

申请日：2021-06-09

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.

公开(公告)号：US20210284657A1

公开(公告)日：2021-09-16

申请号：US16332533

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 ,  Bing Zhou ,  Zhuo Chen ,  Ester Fernandez-Salas ,  Longchuan Bai ,  Donna McEachern

IPC: C07D498/14 ,  A61P35/04 ,  A61P35/02

Abstract: The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, 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：US11045448B2

公开(公告)日：2021-06-29

申请号：US16497856

申请日：2018-03-30

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Angelo Aguilar ,  Shilin Xu ,  Liyue Huang ,  Jeanne Stuckey ,  Tianfeng Xu

IPC: A61K31/397 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/5377 ,  C07D205/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

Abstract: The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, R1a, R1b, R1c, R1d, R2, R3, R8a, R8b, R10, X, Z2, m, and n 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：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：US09745314B2

公开(公告)日：2017-08-29

申请号：US14688553

申请日：2015-04-16

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Angelo Aguilar ,  Liu Liu ,  Jianfeng Lu ,  Donna McEachern

IPC: C07D487/10 ,  C07D209/96 ,  C07D209/54 ,  A61K31/404 ,  A61K31/407 ,  A61K45/06 ,  A61N5/10

CPC classification number: C07D487/10 ,  A61K31/407 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098

Abstract: Inhibitors of MDM2 and MDM2-related proteins and compositions containing the same are disclosed. Methods of using the MDM2 inhibitors in the treatment of diseases and conditions wherein inhibition of an interaction between p53 and MDM2 provides a benefit, like cancers, also are disclosed.