Deuterated compound of benzodiazepine and use thereof

By synthesizing deuterated compounds of benzodiazepines, the problem of mydriasis side effects of existing muscarinic receptor antagonists in the treatment of myopia was solved, highly selective inhibition of M2 receptors was achieved, and the effect of myopia treatment was significantly improved.

WO2025214176A1 Publication Date: 2025-10-16SHENZHEN NEWROSETTA BIOSCIENCES CO LTD
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Patent Information

Application Number
PCT/CN2025/085700
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-04-09
Filing Date
2025-03-28
Publication Date
2025-10-16

AI Technical Summary

Technical Problem

Existing muscarinic receptor antagonists such as atropine have the side effect of mydriasis when used to treat myopia, affecting pupil size and accommodation ability, leading to adverse reactions.

Method used

Design and synthesize deuterated compounds of benzodiazepines, and through specific deuterium substitution positions and quantities, enhance the selective antagonism of M2 receptors and reduce the effect on M3 receptors. Prepare them into eye drops, eye gels, eye ointments or injections for local administration to the eye.

Benefits of technology

Without affecting pupil size, it significantly improves the inhibitory activity on M2 receptors, prolongs the inhibition time, reduces the side effect of mydriasis, effectively treats myopia and inhibits the progression of myopia.

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Abstract

Disclosed are a deuterated compound of benzodiazepine, and a use thereof. The deuterated compound of benzodiazepine has the following general formula (I), R1 and R2 being independently selected from ethyl or deuterated ethyl, R3-R18 being independently selected from hydrogen or deuterium, and R1-R18 containing at least one deuterium. The deuterated compound of benzodiazepine provided by the present invention, or a pharmaceutically acceptable salt, hydrate or solvate thereof, has antagonistic activity against muscarinic M2 receptors. Compared with known selective M2 receptor inhibitors, the compound of the present invention has better inhibitory activity and pharmacodynamic properties, and has minimal activity on M3 receptors, thereby avoiding the side effect of pupil dilation (mydriasis). It has promising prospects for clinical applications in treating myopia, preventing myopia, and / or inhibiting the progression of myopia.
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