9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors

US9580430B2 · kind B2 · utility

Assignee

• THE REGENTS OF THE UNIVERSITY OF MICHIGAN · US

Inventors

• Shaomeng Wang · Saline, US
• Yujun Zhao · Ann Arbor, US
• Bing Zhou · Ann Arbor, US
• Angelo Aguilar · Ann Arbor, US
• Liu Liu · San Diego, US
• Longchuan Bai · Ann Arbor, US
• Donna McEachern · Ann Arbor, US
• Duxin Sun · Ann Arbor, US
• Bo Wen · Tangxia, CN
• Ruijuan Luo · Ann Arbor, US
• Ting Zhao · Nanhu, CN
• Arul M. Chinnaiyan · Plymouth, US
• Irfan A. Asangani · Ann Arbor, US
• Jeanne Stuckey · Fenton, US
• Jennifer Lynn Meagher · Ann Arbor, US
• Xu Ran · Ann Arbor, US
• Yang Hu · Brookline, US

Key dates

• Filing date: Feb 27, 2015
• Grant date: Feb 28, 2017
• Expiry date: Feb 27, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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.