Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T40694 Target Info
Target Name Polo-like kinase 1 (PLK1)
Synonyms Serine/threonine-protein kinase PLK1; Serine/threonine-protein kinase 13; Serine-threonine protein kinase 13; STPK13; Plk1; PLK-1; PLK; Mitoticserine-threonine kinase polo-like kinase 1
Target Type Clinical trial Target
Gene Name PLK1
Biochemical Class Kinase
UniProt ID
PLK1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015011084
Title Substituted Dihydropyrido[3,4-B]Pyrazinones As Dual Inhibitors of Bet Proteins and Polo-Like Kinases.
Abstract The present invention relates to substituted dihydropyrido[3,4-b]pyrazinones as dual inhibitors of BET proteins, especially BRD4 proteins and polo-like kinases, especially Plk-1 proteins, of the general formula (I) in which A, X, R1, R2, R3, R4, R5, R6, R7 and n are each as defined in the description, to intermediates for preparation of the inventive compounds, to pharmaceutical compositions comprising the inventive compounds and to the prophylactic and therapeutic use thereof in hyperproliferative disorders, especially in neoplastic disorders. This invention further relates to the use of the inventive dihydropyrido[3,4-b]pyrazinones in viral infections, in neurodegenerative disorders, in inflammation disorders, in atherosclerotic disorders and in male fertility control.
Applicant(s) Bayer Pharma Aktiengesellschaft
Representative Drug(s) D0F3GC Drug Info IC50(prominent PLK-1 inhibitory activity at 10 microM ATP) = 7 nM Click to Show More [1]
2 D0S0HQ Drug Info IC50 = 7 nM [1]
References  Top
REF 1 BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.

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