Alkynyl-substituted pyrazole compound as well as preparation method and application thereof

By developing alkynyl-substituted pyrazole compounds as LRRK2 inhibitors, the problems of insufficient pharmacokinetics and blood-brain barrier crossing ability of existing LRRK2 inhibitors have been solved, and effective inhibition of LRRK2 has been achieved, with potential treatment of Parkinson's disease and Other drug application value of LRRK2-mediated diseases.

CN119143724APending Publication Date: 2024-12-17JIANGSU SKYRUN PHARMA CO LTD
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Patent Information

Application Number
CN202310717668.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2023-06-16
Publication Date
2024-12-17

AI Technical Summary

Technical Problem

The existing leucine-rich repeat kinase 2 (LRRK2) inhibitors still have problems with insufficient pharmacokinetic characteristics and poor ability to cross the blood-brain barrier in the treatment of Parkinson's disease, resulting in limited treatment effects.

Method used

Develop an alkynyl-substituted pyrazole compound as a selective LRRK2 inhibitor, optimizes its pharmacokinetic properties and blood-brain barrier crossing capabilities through specific structural design and synthetic routes for prevention and treatment with LRRK2 mediation neurodegenerative disease.

Benefits of technology

The alkynyl-substituted pyrazole compound showed good LRRK2 inhibition effect, and the IC50 value of some compounds was better than that of existing positive controls, and had potential drug application value for the treatment of Parkinson's disease and other LRRK2-mediated diseases.

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Abstract

The invention relates to an alkynyl-substituted pyrazole compound as shown in a formula I or pharmaceutically acceptable salt, prodrug, crystal form, stereoisomer, tautomer, hydrate or solvate thereof, and a pharmaceutical composition containing the alkynyl-substituted pyrazole compound. The compound can be used as a leucine-rich repeat kinase 2 (LRRK2) inhibitor, and is used for preparing medicines for preventing and / or treating leucine-rich repeat kinase 2 (LRRK2) mediated related diseases. # imgabs0 #
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