Retinoid-related orphan receptor gamma t (RORγt) inhibitors from Vitae Pharmaceuticals (WO2015116904) and structure proposal for their Phase I candidate VTP-43742

Expert Opinion on Therapeutic Patents
Christian Gege

Abstract

Retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt or RORC2) is a key transcription factor for the differentiation of naïve proinflammatory CD4(+) T cells and the production of T helper-17 (TH17) cells. Inhibiting RORγt activity is thought to be beneficial in targeting a variety of inflammatory and autoimmune disorders, however current candidates remain to be validated in the clinic. Recently Vitae Pharmaceuticals successfully finished its Phase 1 single ascending dose clinical study with their proprietary RORγt inverse agonist VTP-43742. On the basis of the reported promising results, Vitae Pharmaceuticals could currently be considered as having the leading clinical candidate in the RORγt inverse agonist category. This prompts the interest on the exact chemical structure of their clinical candidate. The first relevant patent application (WO2014179564) from Vitae Pharmaceuticals describes RORγt inverse agonists with a 5,6-dihydro-4H-pyrrolo[3,4-d]thiazole core, while in the second and latest patent application (WO2015116904) this element has changed towards a 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine core. By combining information from Vitae's patent applications and trustworthy online information, the potential ...Continue Reading

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Citations

Aug 21, 2016·Bioorganic & Medicinal Chemistry Letters·Patrick CyrJames J Crawford
Sep 16, 2016·Expert Opinion on Therapeutic Patents·Sarah M BronnerJames J Crawford
Jan 19, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Patrizia FaschingJohannes Fessler
Jun 24, 2018·Chemistry & Biodiversity·Moustafa T Gabr, Mohammed S Abdel-Raziq
Oct 30, 2019·ChemMedChem·Ayumu SatoSatoshi Yamamoto
Dec 6, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nannan SunWei Fu
Aug 4, 2019·The Journal of Pharmacology and Experimental Therapeutics·Stephen GauldPhilippe Masson
Aug 7, 2019·Annual Review of Pharmacology and Toxicology·Anton M Jetten, Donald N Cook
Jul 6, 2019·Mediators of Inflammation·Carmen Rodríguez-CerdeiraJosé Luís González-Cespón
Aug 11, 2018·Journal of Medicinal Chemistry·Frank NarjesThomas G Hansson

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