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.
Search By Structure
- tucatinib
- S6821
- MRTX849
- BAY1161909
- ORN0829
- BMS-986251
- GSK2818713
- CPI-1612
- “Compound 19”
- AZD4205
- QPX7728
- “Compound 9”
- “Compound (P)-14″
- FT385
Molecules of the Month
2023
2022
2021
2020