title: Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.
abstract: Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly linked to both cancer and inflammatory diseases. There are currently two launched JAK inhibitors for the treatment of human conditions: tofacitinib for Rheumatoid arthritis (RA) and ruxolitinib for myeloproliferative neoplasms including intermediate or high risk myelofibrosis and polycythemia vera. Areas covered: This review covers patents claiming activity against one or more JAK family members in the period 2013-2015 inclusive, and covers 95 patents from 42 applicants, split over two parts. The authors have ordered recent patents according to the primary applicant's name, with part 1 covering A through to I. Expert opinion: Inhibition of JAK-family kinases is an area of growing interest, catalysed by the maturity of data on marketed inhibitors ruxolitinib and tofacitinib in late stage clinical trials. Many applicants are pursuing traditional fast-follower strategies around these inhibitors, with a range of chemical strategies adopted. The challenge will be to show sufficient differentiation to the originator compounds, since dose limiting toxicities with such agents appear to be on target and mechanism-related and also considering that such agents may be available as generic compounds by the time follower agents reach market.
authors: a AstraZeneca, Oncology iMED, Mereside, Alderley Park , Stockport , United Kingdom.
authors: Jason G
authors: JG
authors: Kettle
authors: b AstraZeneca, Respiratory, Inflammation and Autoimmunity iMED Pepparedsleden 1 , Mölndal , Sweden.
authors: Annika
authors: A
authors: Åstrand
authors: b AstraZeneca, Respiratory, Inflammation and Autoimmunity iMED Pepparedsleden 1 , Mölndal , Sweden.
authors: Matthew
authors: M
authors: Catley
authors: c AstraZeneca, Oncology iMED , Waltham , MA , USA.
authors: Neil P
authors: NP
authors: Grimster
authors: b AstraZeneca, Respiratory, Inflammation and Autoimmunity iMED Pepparedsleden 1 , Mölndal , Sweden.
authors: Magnus
authors: M
authors: Nilsson
authors: c AstraZeneca, Oncology iMED , Waltham , MA , USA.
authors: Qibin
authors: Q
authors: Su
authors: c AstraZeneca, Oncology iMED , Waltham , MA , USA.
authors: Richard
authors: R
authors: Woessner
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000201:enzymology; D053612:Janus Kinases / Q000037:antagonists & inhibitors*; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D053612:Janus Kinases
keywords: JAK; JAK1 inhibitor; JAK2 inhibitor; JAK3 inhibitor; Janus kinase inhibitors; TYK2 inhibitor; myelofibrosis; oncology; rheumatoid arthritis; ruxolitinib; tofacitinib