Leucine-rich repeat kinase 2 inhibitors: a patent review (2014-2016)

ABSTRACTIntroduction: Leucine-rich repeat kinase 2 (LRRK2) is a member of the Tyrosine Kinase-Like (TKL) branch of the kinome tree and is a multi-domain protein that includes GTPase and kinase activity. While genome-wide association studies (GWAS) has linked LRRK2 with Crohn’s disease and leprosy, it has received the greatest attention due to it being implicated as one of the genetic loci associated with autosomal dominant inheritance in Parkinson’s disease (PD).Areas covered: In this review, the small molecule patent literature from 2014–2016 with a focus on composition of matter and use patents was surveyed. Scifinder was primarily searched using ‘LRRK2ʹ as the query to identify all relevant literature and then triaged for small molecule patents.Expert opinion: The patent landscape around LRRK2 continues to develop. The early patents covered using existing kinase inhibitors for use against LRRK2. This evolved to compounds specifically designed for selectivity against LRRK2, but key exemplified compounds...