Antagonisten des schilddrüsenstimulierenden hormonrezeptors (TSHR)

AT1917968TUndetermined Publication Date: 2026-05-15FORSCHUNGSVERBUND BERLIN EV
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Patent Information

Application Number
AT2017720091T
Authority / Receiving Office
AT · AT
Patent Type
Patents
Current Assignee / Owner
Priority Date
2016-04-27
Filing Date
2017-04-26
Publication Date
2026-05-15
Estimated Expiration
2037-04-26

AI Technical Summary

Technical Problem

Current treatments for hyperthyroidism and Graves' disease primarily target thyroid hormone synthesis rather than the underlying molecular activation of the thyroid-stimulating hormone receptor (TSHR), leading to adverse effects and inadequate management of Graves' ophthalmopathy, which requires targeted TSHR antagonists.

Method used

Development of specific chemical compounds, such as those following Formula I, that act as TSHR antagonists with stereoisomeric configurations enabling selective inhibition of TSHR activity, reducing cross-reactivity with other hormone receptors like FSHR.

Benefits of technology

These compounds effectively inhibit TSHR-mediated signaling, providing a therapeutic option for hyperthyroidism and Graves' disease with reduced side effects and improved treatment of Graves' ophthalmopathy by selectively targeting the TSHR.

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Abstract

The invention relates to chemical compounds that are useful in the treatment of a subject afflicted by a thyroid disease, in particular to compounds that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and their use in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
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