Bicyclic sigma-1 receptor inhibitors

By designing σ1 receptor inhibitor compounds with a bicyclic structure, the problems of insufficient selectivity and pharmacodynamics in existing technologies have been solved, achieving highly efficient inhibition of σ1 receptors and pain relief, especially showing significant efficacy in the treatment of neuropathic pain and inflammatory pain.

CN117447376BActive Publication Date: 2026-06-09SUZHOU NHWA PHARM RES CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2020-11-25
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

There is a lack of compounds with high selectivity and good pharmaceutical value for σ1 receptors in the current technology for the treatment of central nervous system diseases such as pain and mental illness.

Method used

A compound with a bicyclic structure, having specific aromatic ring groups and alkylamine substituents, was designed as a selective inhibitor of the σ1 receptor. Compounds with different substitution forms were synthesized to improve the affinity and selectivity for the σ1 receptor.

Benefits of technology

This compound exhibits significant inhibitory activity against σ1 receptors, effectively treating pain, particularly neuropathic and inflammatory pain, and its pain-relieving effect is enhanced when used in combination with morphine.

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Abstract

The present application relates to the chemical medicine field, especially to a kind of sigma-1 receptor inhibitor of double ring structure. Specifically provide a kind of unique double ring structure compound of structure, it has good σ1 receptor affinity and selectivity, is the strong selective inhibitor of σ1 receptor. The double ring structure compound has the basic group structure of double aromatic ring, and the characteristic that the isoside skew symmetry position of intermediate aromatic bicyclic is respectively replaced by another double aromatic ring and alkylamine directly connected with aromatic ring.
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Citation Information

Patent Citations

  • Bicyclic sigma-1 receptor inhibitors

    CN114702428B

  • 2-(1-phenyl-4,5,6,7-tetrahydro-1h-indazol-4-YL)ethylamine derivatives useful as sigma receptor inhibitors

    WO2012072791A2

  • Sigma receptor inhibitors

    CN101014575A

  • 5-methyl-1-(naphthalen-2-yl)-1H-pyrazoles useful as sigma receptor inhibitors

    CN102066333A