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公开(公告)号：US10988476B2
公开(公告)日：2021-04-27
申请号：US16848942
申请日：2020-04-15
发明人： Guangxin Xia , Qian Wang , Chen Shi , Xiong Zhai , Hui Ge , Xuemei Liao , Yu Mao , Zhixiong Xiang , Yanan Han , Guoyong Huo , Yanjun Liu
IPC分类号： A61K31/506 , C07D239/30 , C07D471/04 , A61P35/00 , C07F5/02 , C07F7/08 , C07F9/6561 , C07F9/6584
摘要： The present invention discloses a substituted pyridine compound represented by formula I, and a pharmaceutically acceptable salt, stereoisomer and tautomer thereof. The compounds of the present invention are useful in the treatment of cancers.
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公开(公告)号：US10662186B2
公开(公告)日：2020-05-26
申请号：US16067158
申请日：2016-12-30
发明人： Guangxin Xia , Qian Wang , Chen Shi , Xiong Zhai , Hui Ge , Xuemei Liao , Yu Mao , Zhixiong Xiang , Yanan Han , Guoyong Huo , Yanjun Liu
IPC分类号： A61K31/506 , C07D239/30 , C07D471/04 , A61P35/00 , C07F5/02 , C07F7/08 , C07F9/6561 , C07F9/6584
摘要： 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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