title: Retinoid-related orphan receptor γ t modulators: comparison of Glenmark's me-too patent application (WO2015008234) with the originator application from Merck Sharp and Dohme (WO2012106995).
abstract: Retinoic acid receptor-related orphan nuclear receptor γ t (RORγt) is a key transcription factor for the development of TH17 cells. Inhibiting RORγt activity is thought to be beneficial in targeting a variety of inflammatory and autoimmune disorders. In their patent application WO2015008234, Glenmark applied a scaffold-hop approach regarding to the originator application from Merck Sharp & Dohme (WO2012106995): a 6-membered annelated aromatic moiety is replaced by an annelated 5-membered heteroaryl (exemplified and claimed is however only thiophene), resulting in potent RORγt inverse agonists with a thieno[3,2-b]pyrrole or thieno[3,2-c]pyrazole core. Based on the patent disclosure, the novelty and utility of these me-too compounds is discussed.
authors.affiliation: a Phenex Pharmaceuticals AG , Waldhofer Straße 104, 69123 Heidelberg, Germany christian.gege@web.de.
authors.forename: Christian
authors.initials: C
authors.lastname: Gege
mesh_terms: D000818:Animals; D001327:Autoimmune Diseases / Q000188:drug therapy; D015195:Drug Design; D054314:Drug Inverse Agonism; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D057132:Nuclear Receptor Subfamily 1, Group F, Member 3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010330:Patents as Topic; D058504:Th17 Cells / Q000378:metabolism*
chemical_list: D057132:Nuclear Receptor Subfamily 1, Group F, Member 3
keywords: RORc; me-too compounds; retinoid-related orphan receptor γ t; scaffold-hop