Pyrimidine pro drug, preparation method thereof and application thereof

By improving the structure of pyrazolopyrimidine prodrugs, the problems of insufficient solubility, stability and bioavailability are solved, and the effective inhibition of CK2 and the treatment of CK2-related diseases are achieved, especially when combined with other anti-cancer agents. Significantly inhibits tumor growth when used in combination.

CN104844605AInactive Publication Date: 2015-08-19SENHWA BIOSCIENCES INC
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Patent Information

Application Number
CN201410228164.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2014-02-13
Filing Date
2014-05-27
Publication Date
2015-08-19
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing pyrazolopyrimidine compounds have problems with insufficient solubility, stability and bioavailability when treating CK2-related diseases, which affects their pharmacokinetic properties and leads to poor therapeutic effects.

Method used

A new pyrazolopyrimidine prodrug was designed with a structure that improves solubility, stability, and bioavailability, and is metabolically converted into active compounds to modulate CK2 activity for the treatment of CK2-related diseases. The prodrug can be combined with solvents and buffers to form pharmaceutical compositions, and can be used in combination with other anticancer agents to enhance therapeutic effects.

Benefits of technology

Through the improved structure, the bioavailability and pharmacokinetic properties of pyrazolopyrimidines are improved, the inhibitory effect on CK2 is significantly enhanced, and the CK2-related diseases are effectively treated, such as cancer, inflammatory and immune diseases, and are compatible with Other anticancer agents can be more effective at inhibiting tumor growth when used in combination.

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Abstract

The invention relates to a pyrimidine pro drug, a preparation method thereof and an application thereof. The pyrimidine pro drug as illustrated in formula I is characterized by making pyrimidine with suppressed protein kinase CK2 biological activity have improved solubility, stability, biological usability and pharmacodynamic performance. The invention further relates to a drug composition using the pro drug and the use thereof. The drug composition is characterized in that it is used for treating related hyperplastic diseases such as cancer and other diseases related to kinases including inflammatory diseases, infectious diseases, pains, immune diseases or neurodegenerative diseases, etc.
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