Abstract
Three patent applications, from two different companies, claim structurally novel Tyk2 inhibitors and their uses for the treatment of autoimmune diseases. In EP-2634185 Sareum claims 5-anilino-2-(2-halophenyl)-oxazole-4-carboxamide derivatives which are shown to be nanomolar potency Tyk2 inhibitors with 10 – 100-fold selectivity over JAK1, JAK2 and JAK3. Takeda's WO-2013125543 and WO-2013146963 claim two distinct structural classes of Tyk2 inhibitors. The first application claims inhibitors based on an unusual 1,5-dihydro-4H-pyrazolo[4,3-c]pyridine-4-one scaffold and the second claims 1-(2-arylaminopyrimidin-4-yl)-pyrrolidin-2-one derivatives. One example of the latter was shown to be orally active in an IL-23-induced inflammation model.
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