Leena Patel

TL;DR: The optimization of the dihydropyrone series inhibitors to improve compound aqueous solubility and reduce CYP2D6 inhibition led to the discovery of compound 24 (PF-00868554), a potent and selective HCV polymerase inhibitor with a favorable pharmacokinetic profile.

TL;DR: In this article, the authors describe compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, for treating conditions mediated by one or more PI3K isoforms.

TL;DR: This work has investigated a series of substituted 2-methylbenzofurans as “partial activators” of the glucokinase enzyme leading to the identification of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benz ofuran-4-yloxy)pyrimidine- 2-carboxamide as an early development candidate.

TL;DR: This medicinal chemistry effort culminated in the identification of 52, a potent and highly selective inhibitor of PI3Kδ that demonstrates efficacy in a rat model of arthritis.

TL;DR: This work led to the discovery of 35, a highly selective inhibitor of PI3Kδ which displays an excellent pharmacokinetic profile and is efficacious in a rodent model of rheumatoid arthritis.