Invention Grant
- Patent Title: Substituted pyrimidines as cyclin-dependent kinase inhibitors
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Application No.: US16067158Application Date: 2016-12-30
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Publication No.: US10662186B2Publication Date: 2020-05-26
- Inventor: Guangxin Xia , Qian Wang , Chen Shi , Xiong Zhai , Hui Ge , Xuemei Liao , Yu Mao , Zhixiong Xiang , Yanan Han , Guoyong Huo , Yanjun Liu
- Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
- Applicant Address: CN Shanghai
- Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
- Current Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
- Current Assignee Address: CN Shanghai
- Agency: Pilloff Passino & Cosenza LLP
- Agent Sean A. Passino; Rachel K. Pilloff
- Priority: com.zzzhc.datahub.patent.etl.us.BibliographicData$PriorityClaim@7adf383f com.zzzhc.datahub.patent.etl.us.BibliographicData$PriorityClaim@163e2cc5 com.zzzhc.datahub.patent.etl.us.BibliographicData$PriorityClaim@51b9ae37
- International Application: PCT/CN2016/113887 WO 20161230
- International Announcement: WO2017/114512 WO 20170706
- Main IPC: A61K31/506
- IPC: A61K31/506 ; C07D239/30 ; C07D471/04 ; A61P35/00 ; C07F5/02 ; C07F7/08 ; C07F9/6561 ; C07F9/6584

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.
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