公开(公告)号：US20150299211A1

公开(公告)日：2015-10-22

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 ,  A61K45/06 ,  A61N5/10 ,  A61K31/407

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.

Abstract translation: 公开了MDM2和MDM2相关蛋白的抑制剂和含有它们的组合物。 还公开了使用MDM2抑制剂治疗其中抑制p53和MDM2之间的相互作用提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20130150309A1

公开(公告)日：2013-06-13

申请号：US13686475

申请日：2012-11-27

Applicant: The Regents of the University of Michigan

Inventor： Shaomeng Wang ,  Hacer Karatas ,  Yali Dou ,  Elizabeth Townsend ,  Denzil Bernard ,  Fang Cao

IPC: C07K5/12 ,  A61N5/10 ,  C07D255/02 ,  A61K38/12 ,  A61K45/00

CPC classification number: C07K5/126 ,  A61K38/12 ,  A61K45/00 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D255/02 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/0215 ,  C07K5/06034 ,  C07K5/0815 ,  C07K5/101 ,  C07K5/1019 ,  C07K5/123 ,  A61K2300/00

Abstract: Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.

Abstract translation: 公开了抑制MLL1和WDR5之间相互作用的循环肽模拟物。 还公开了抑制MLL1活性的方法和治疗癌症的方法。

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：US11691989B2

公开(公告)日：2023-07-04

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: C07D497/22 ,  C07D515/22 ,  C07D231/12 ,  A61K31/395 ,  A61P35/00

CPC classification number: 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：US20220380368A1

公开(公告)日：2022-12-01

申请号：US17760786

申请日：2020-09-18

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xin Han ,  Weiguo Xiang ,  Bukeyan Miao ,  Chong Qin ,  Lijie Zhao ,  Jianfeng Lu ,  Tianfeng Xu ,  Chao-Yie Yang

IPC: C07D471/10 ,  A61P35/00 ,  A61P13/08

Abstract: The present disclosure provides compounds represented by Formula (I) and the salts or solvates thereof, wherein R3a, E, L, A1, B1, X1, X2, Z1, and Z2 are as defined in the specification. Compounds having Formula (I) are androgen receptor degraders useful for the treatment of cancer and other diseases.

公开(公告)号：US20210340158A1

公开(公告)日：2021-11-04

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 ,  C07D513/10 ,  C07D519/00 ,  A61P35/00

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：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：US10829488B2

公开(公告)日：2020-11-10

申请号：US16317056

申请日：2017-08-04

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

IPC: C07D471/04 ,  A61P35/02 ,  A61P35/00

Abstract: The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1, X2, X3 R1a, R1b E, and = are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer.

公开(公告)号：US10709705B2

公开(公告)日：2020-07-14

申请号：US15559445

申请日：2017-08-28

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：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.