公开(公告)号：US20190119289A1

公开(公告)日：2019-04-25

申请号：US16091544

申请日：2017-04-06

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yangbing Li ,  Angelo Aguilar ,  Bing Zhou ,  Jiantao Hu ,  Fuming Xu ,  Chong Qin ,  Yang Hu ,  Weiguo Xiang ,  Rohan Rej ,  Jiuling Yang ,  Xin Han ,  Longchuan Bai ,  Chao-Yie Yang

IPC: C07D487/10 ,  C07D401/04 ,  C07D401/14 ,  C07D495/14 ,  C07D487/04

Abstract: The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein X, L, Y, and B are as defined in the specification. Compounds having Formula I are immunomodulators and/or monofunctional synthetic intermediates that can be used to prepare small-molecule drug conjugates.

公开(公告)号：US10253044B2

公开(公告)日：2019-04-09

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

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.