Dihydropyranopyrimidinone derivatives, and use thereof
Inventors
Kim, Kyungjin • KIM, Uk-Il • YOON, Ji Hye
Assignees
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Publication Number
US-10336765-B2
Publication Date
2019-07-02
Expiration Date
Abstract
The present invention relates to a novel dihydropyranopyrimidinone derivative, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating a tankyrase-related disease, which contains the same as an active ingredient.
Core Innovation
The patent describes compounds represented by Chemical Formula 1, including tautomers, stereoisomers, mixtures thereof, and pharmaceutically acceptable salts. The compounds are dihydropyranopyrimidinone derivatives with structural variables including X and Y, substituent groups denoted by R1, R2, R4-R10, and linker elements such as Z, (CH2)m, and the integers l, m, n, p, and q.
The patent further describes 2-(4-(2,6-difluoro-4-aryl/heteroaryl-alkoxy)phenyl)piperazin-1-yl and related piperazinyl variants connected to the 7,8-dihydro-3H-pyrano[4,3-d]pyrimidin-4(5H)-one scaffold. The ether side chain varies while maintaining the 2,6-difluoro and 4-(aryl/heteroaryl-alkoxy)phenyl piperazin-1-yl connection, with enumerated examples including methoxyethoxy, morpholinoethoxy, piperidinylethoxy, hydroxyethoxy, dihydroxypropoxy, and other hydroxy-containing side chains.
The compounds are positioned as tankyrase 1/2 inhibitors for preventing or treating tankyrase-related diseases. The document explains a tankyrase-related mechanism in connection with Wnt/β-catenin signaling, including axin stabilization and β-catenin, and reports tankyrase 1 inhibitory activity for synthesized examples using an ELISA-based PAR assay with IC50 values reported for multiple example compounds.
Claims Coverage
The independent claim coverage centers on a compound represented by Chemical Formula 1 with broad structural variability, including tautomers, stereoisomers, mixtures, and pharmaceutically acceptable salts. Additional independent claim coverage is provided for pharmaceutical composition embodiments with the same active compound, including optional carriers, diluents, or excipients.
Chemical Formula 1 dihydropyranopyrimidinone scaffold as tankyrase inhibitor
A compound represented by Chemical Formula 1, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof, wherein X, Y, l, R1, R2, R4, m, n, R5, Z, p, q, R6, and R8-R10 are defined according to the claim's variable definitions.
Pharmaceutical composition with Chemical Formula 1 active compound
A pharmaceutical composition whose active ingredient is the compound represented by Chemical Formula 1, a tautomer thereof, a stereoisomer thereof, their mixture, or a pharmaceutically acceptable salt.
Pharmaceutical composition with pharmaceutically acceptable carrier, diluent, or excipient
A pharmaceutical composition further comprising a pharmaceutically acceptable carrier, diluent, or excipient.
Overall claim coverage centers on Chemical Formula 1 dihydropyranopyrimidinone derivatives, including tautomers, stereoisomers, mixtures, and salts, defined by extensive variable substituent rules, with further coverage for pharmaceutical compositions using these compounds as active ingredients, including optional carrier, diluent, or excipient formulation components.
Stated Advantages
Compounds are described as tankyrase 1/2 inhibitors for preventing or treating tankyrase-related diseases.
Documented Applications
Preventing or treating tankyrase-related diseases, including cancers, using tankyrase 1/2 inhibitor compounds represented by Chemical Formula 1.
Use in the context of Wnt/β-catenin signaling via axin stabilization and β-catenin, as described in the background.
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