Hopkins, Brian T. published the artcileDiscovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis, Quality Control of 1462286-01-6, the publication is Journal of Medicinal Chemistry (2022), 65(2), 1206-1224, database is CAplus and MEDLINE.
Multiple Sclerosis is a chronic autoimmune neurodegenerative disorder of the central nervous system (CNS) that is characterized by inflammation, demyelination, and axonal injury leading to permeant disability. In the early stage of MS, inflammation is the primary driver of the disease progression. There remains an unmet need to develop high efficacy therapies with superior safety profiles to prevent the inflammation processes leading to disability. Herein, we describe the discovery of BIIB091 (I), a structurally distinct orthosteric ATP competitive, reversible inhibitor that binds the BTK protein in a DFG-in confirmation designed to sequester Tyr-551, an important phosphorylation site on BTK, into an inactive conformation with excellent affinity. Preclin. studies demonstrated BIB091 to be a high potency mol. with good drug-like properties and a safety/tolerability profile suitable for clin. development as a highly selective, reversible BTKi for treating autoimmune diseases such as MS.
Journal of Medicinal Chemistry published new progress about 1462286-01-6. 1462286-01-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazoles, name is 4-Chloro-N-(1-methyl-1H-pyrazol-4-yl)pyrimidin-2-amine, and the molecular formula is C8H8ClN5, Quality Control of 1462286-01-6.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics