title: Evaluation of WO2013125543, WO2013146963 and EP2634185: the first Tyk2 inhibitors from Takeda and Sareum.
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.
authors.affiliation: Norman Consulting , 18 Pink Lane, Burnham, Bucks, SL1 8JW , UK peter.norman2@btinternet.com.
authors.forename: Peter
authors.initials: P
authors.lastname: Norman
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000627:therapeutic use*; D001327:Autoimmune Diseases / Q000188:drug therapy* / Q000201:enzymology / Q000276:immunology; D004195:Disease Models, Animal; D006801:Humans; D007249:Inflammation / Q000517:prevention & control; D007880:Legislation, Drug; D015394:Molecular Structure; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship; D053634:TYK2 Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D047428:Protein Kinase Inhibitors; D053634:TYK2 Kinase