The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 26, 2020
Filed:
Dec. 30, 2016
Shanghai Pharmaceuticals Holding Co., Ltd., Shanghai, CN;
Guangxin Xia, Shanghai, CN;
Qian Wang, Shanghai, CN;
Chen Shi, Shanghai, CN;
Xiong Zhai, Shanghai, CN;
Hui Ge, Shanghai, CN;
Xuemei Liao, Shanghai, CN;
Yu Mao, Shanghai, CN;
Zhixiong Xiang, Shanghai, CN;
Yanan Han, Shanghai, CN;
Guoyong Huo, Shanghai, CN;
Yanjun Liu, Shanghai, CN;
SHANGHAI PHARMACEUTICALS HOLDING CO., LTD., Shanghai, CN;
Abstract
The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.