Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist

Willem F.J. Karstens, Wiro M.B.P. Menge, Gijs Martens, Sanne J.N. op het Veld, Jacobus Th.H. van Eupen, Marco Demon, Tanja A.E. van Achterberg, Monica J. Arisse-Thijssen, Ellen W.H. Santegoeds-Lenssen,Miranda M.C. van der Lee,Ruud Ubink, Roel J. Arends,Aloys Sesink, Marion Blomenröhr,C. Marco Timmers

Bioorganic & Medicinal Chemistry（2023）

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摘要

•Discovery of a novel class of thyrotropin receptor antagonists.•A highly potent compound with oral efficacy was identified.•Risk of mutagenicity of compounds strongly reduced.•Efficacy correlates with exposure after oral dosing.

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