公开(公告)号：US10221174B2

公开(公告)日：2019-03-05

申请号：US16051816

申请日：2018-08-01

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

IPC: C07D471/04 ,  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：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：US20170210761A1

公开(公告)日：2017-07-27

申请号：US15443336

申请日：2017-02-27

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yujun Zhao ,  Bing Zhou ,  Angelo Aguilar ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Duxin Sun ,  Bo Wen ,  Ruijuan Luo ,  Ting Zhao ,  Arul Chinnaiyan ,  Irfan A. Asangani ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Xu Ran ,  Yang Hu

IPC: C07D519/00 ,  A61K31/519 ,  C07D487/14 ,  A61K31/538 ,  A61K31/437 ,  C07D487/04 ,  A61K31/5377

CPC classification number: C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  C07D487/14

Abstract: The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 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. Compounds of the present disclosure are especially useful for treating cancer.

公开(公告)号：US09302120B2

公开(公告)日：2016-04-05

申请号：US14170101

申请日：2014-01-31

Applicant: The Regents of the University of Michigan

Inventor： Shaomeng Wang ,  Yujun Zhao ,  Wei Sun

IPC: C07D487/10 ,  A61N5/10 ,  A61K31/407 ,  A61K45/06

CPC classification number: A61N5/10 ,  A61K31/407 ,  A61K45/06 ,  C07D487/10 ,  A61K2300/00

Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

公开(公告)号：US20140378680A1

公开(公告)日：2014-12-25

申请号：US14485054

申请日：2014-09-12

Applicant: The Regents of the University of Michigan

Inventor： Shaomeng Wang ,  Shanghai Yu ,  Wei Sun ,  SanJeev Kumar ,  Duxin Sun ,  Peng Zou ,  Donna McEachern ,  Yujun Zhao

IPC: C07D487/10 ,  C07D471/20 ,  C07F9/6561

CPC classification number: C07D487/10 ,  A61K31/407 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/675 ,  A61K45/06 ,  C07D471/20 ,  C07D491/107 ,  C07D495/10 ,  C07F9/6561 ,  A61K2300/00

Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

公开(公告)号：US08883771B2

公开(公告)日：2014-11-11

申请号：US13969030

申请日：2013-08-16

Applicant: The Regents of the University of Michigan

Inventor： Shaomeng Wang ,  Rong Sheng ,  Haiying Sun ,  Liu Liu ,  Jianfeng Lu ,  Donna McEachern

IPC: C07D225/00 ,  A61K31/545 ,  C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

CPC classification number: C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

Abstract: Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.

Abstract translation: 公开了IAP蛋白的抑制剂和含有其的组合物。 还公开了使用IAP蛋白抑制剂治疗其中抑制IAP蛋白提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20140148494A1

公开(公告)日：2014-05-29

申请号：US14170101

申请日：2014-01-31

Applicant: The Regents of the University of Michigan ,  Sanofi ,  Ascenta Licensing Corporation

Inventor： Shaomeng Wang ,  Yujun Zhao ,  Wei Sun ,  Sanjeev Kumar ,  Lance Leopold ,  Laurent Debussche ,  Cedric Barriere ,  Jean-Christophe Carry ,  Kwame Amaning

IPC: C07D487/10 ,  A61K31/407 ,  A61N5/10 ,  A61K45/06

CPC classification number: A61N5/10 ,  A61K31/407 ,  A61K45/06 ,  C07D487/10 ,  A61K2300/00

Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

Abstract translation: 本文提供了药物化学领域中的化合物，组合物和方法。 本文提供的化合物和组合物涉及用作p53和MDM2之间相互作用的拮抗剂的螺 - 羟基吲哚，以及它们作为治疗癌症和其它疾病的治疗剂的用途。

公开(公告)号：US20140057924A1

公开(公告)日：2014-02-27

申请号：US13969030

申请日：2013-08-16

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Rong Sheng ,  Haiying Sun ,  Liu Liu ,  Jianfeng Lu ,  Donna McEachern

IPC: C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

CPC classification number: C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

Abstract: Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.

Abstract translation: 公开了IAP蛋白的抑制剂和含有其的组合物。 还公开了使用IAP蛋白抑制剂治疗其中抑制IAP蛋白提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20240150360A1

公开(公告)日：2024-05-09

申请号：US18279232

申请日：2022-03-03

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Zhixiang Chen ,  Dimin Wu ,  Mi Wang

IPC: C07D487/04 ,  C07D401/04 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D471/04 ,  C07D519/00

Abstract: The present disclosure relates to compounds of Formula (I), and the pharmaceutically


A—(CH2)m—X—Y—Z—B1  I,

acceptable salts and solvates thereof, wherein A, m, X, Y, Z, and B1 are as defined as set forth in the specification. The present disclosure also relates to uses of the compounds, e.g., in treating or preventing a condition or disorder responsive to the degradation of CBP/P300 proteins (e.g., cancer).

公开(公告)号：US11718613B2

公开(公告)日：2023-08-08

申请号：US17023426

申请日：2020-09-17

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

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

CPC classification number: C07D471/04 ,  A61P35/00 ,  A61P35/02

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.