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：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。