Tricyclic tetrahydroisoquinoline derivatives, processes for their preparation and their use in medicine

By developing tricyclic tetrahydroisoquinoline derivatives, the side effects of existing SERMs and SERDs in the treatment of estrogen-dependent diseases have been resolved, achieving safer and more effective estrogen receptor regulation and prolonging the therapeutic effect.

CN116731064BActive Publication Date: 2026-06-16JIANGSU HENGRUI MEDICINE CO LTD +1

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JIANGSU HENGRUI MEDICINE CO LTD
Filing Date
2021-01-08
Publication Date
2026-06-16

AI Technical Summary

Technical Problem

Existing selective estrogen receptor modulators (SERMs) and selective estrogen receptor downregulators (SERDs) have serious side effects in the treatment of estrogen-dependent diseases such as breast cancer, and there is a need to find safe and effective alternatives.

Method used

A tricyclic tetrahydroisoquinoline derivative was developed as a selective estrogen receptor modulator. Its binding ability to the estrogen receptor was optimized through specific structural modifications to reduce side effects.

🎯Benefits of technology

This compound can effectively regulate estrogen receptors, reduce side effects, prolong the efficacy of anti-estrogenic therapy, and provide a safer treatment option.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present disclosure relates to tricyclic tetrahydroisoquinoline derivatives, processes for their preparation and their use in medicine. In particular, the present disclosure relates to tricyclic tetrahydroisoquinoline derivatives of general formula (I), processes for their preparation and pharmaceutical compositions containing them, as well as their use as estrogen receptor modulators and their use in the manufacture of a medicament for the treatment of a disease or disorder mediated or dependent on the estrogen receptor. Wherein the substituents of general formula (I) are as defined in the description.
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