Low molecular weight thyroid stimulating hormone receptor (tshr) agonists (U.S. Patent Application Number WO 2010047674 A1)

Acronym: Not Available NIDDK Contact: Principal Investigator(s): Susanne Neumann, Marvin Gershengorn


NIH investigators have discovered a series of low molecular weight thyroid-stimulating hormone (TSH) receptor modulators for use in the procedure to detect residual thyroid cancer cells following thyroidectomy. As small molecules, these compounds are orally available and are expected to be less costly and more straightforward to produce than recombinant protein counterparts currently on the market.  These compounds appear be orally available, would be less difficult and expensive to produce, and are also more potent and/or specific for the TSH receptor than other known small-molecule TSH receptor agonists. In addition to use in thyroid cancer screening, these compounds may also be useful for adjunctive treatment (with radioactive iodide) of thyroid cancer, and certain forms of hypothyroidism.

Disclosed are oxo-hydroquinazolines of formula I that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.

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