Peripheral restriction GABA allosteric positive regulator for the treatment of irritable bowel syndrome and other peripheral nervous system disorders

Peripherally restricted GABA-A receptor allosteric modulators address the limitations of current IBS treatments by targeting the peripheral nervous system, effectively treating IBS and other disorders without CNS side effects.

JP7884738B2Active Publication Date: 2026-07-06JOHNS HOPKINS UNIVERSITY +1
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Patent Information

Application Number
JP2023546485
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2021-02-02
Filing Date
2022-02-01
Publication Date
2026-07-06
Estimated Expiration
2042-02-01

AI Technical Summary

Technical Problem

Current treatments for irritable bowel syndrome (IBS) are limited, with existing medications providing only symptom relief and potential severe side effects, and there is a need for alternative approaches that target the peripheral nervous system without crossing the blood-brain barrier.

Method used

Development of peripherally restricted GABA-A receptor allosteric modulators that selectively target the peripheral nervous system, avoiding the blood-brain barrier, to modulate GABAergic neurons and treat conditions like IBS and other systemic diseases.

Benefits of technology

The modulators effectively treat visceral pain and regulate bowel motility in IBS without CNS side effects, providing therapeutic benefits for a range of gastrointestinal and neurological disorders.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present disclosure features a chemical compound (e.g., a compound or its pharma- ceutically acceptable salt, or its N-oxide) that is a positive allosteric modulator of one or more GABA-A receptors, e.g., a peripherally restricted positive allosteric modulator of one or more GABA-A receptors that selectively targets the peripheral nervous system and organs of the body and does not substantially cross the blood-brain barrier. The compound is useful, for example, for treating systemic diseases of the body, e.g., diseases in which modulation of one or more peripherally restricted GABA-A receptors is beneficial (e.g., diseases or disorders mediated by GABA-A neuronal activity). The present disclosure also features pharmaceutical compositions containing the chemical compounds described herein, and methods of use thereof for treating systemic diseases of the body.
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Citation Information

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