molecules of the month

“Compound 19”

JAK1/TYK2-selective dual kinase inhibitor

oral activity in arthritis model

from SBDD of prior internal matter

Bioorg. Med. Chem. Lett., Mar. 31, 2020

Pfizer, Cambridge, MA and Groton, CT

Compound 19
1 min read

“Compound 19” is a JAK1/TYK2 dual kinase inhibitor from Pfizer, related to its clinical JAK1/TYK2 dual inhibitor, brepocitinib, in Ph. II for a variety of inflammatory diseases. The cyclopropyl amide group was designed to displace a high energy water molecule. It was probably fortunate for their manufacturing colleagues that brepocitinib was taken forward instead, as the [3.1.0] core of this molecule was prepared through a Ti-mediated cyclopropanation in <20% yield.

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