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专利概况
专利名称 A nitrogen-containing condensed heterocyclic compound, production, intermediate, and use of the composition
申请号 JP2018534536 申请日
公开(公告)号 JP2019500389A 公开(公告)日 2016-12-30
申请(专利权)人 发明人 シア コアンシン; ワン チエン; シー チェン; チャイ シオン; ケ ホイ; リャオ シュエメイ; マオ ユイ; シアン チーシオン; ハン ヤナン; フオ クオヨン; リウ イェンチュン
专利来源 国家知识产权局 转化方式
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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