NITROGEN-CONTAINING FUSED HETEROCYCLIC COMPOUND, AS WELL AS PREPARATION METHOD, INTERMEDIATE, COMPOSITION AND APPLICATION THEREOF
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 pharmaceut...
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Main Authors | , , , , , , , , , , |
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Format | Patent |
Language | English French German |
Published |
07.08.2019
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Subjects | |
Online Access | Get full text |
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Summary: | 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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Bibliography: | Application Number: EP20160881301 |