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Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin

Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin

Peter Jones, R Ian Storer, Yogesh A Sabnis, Florian M Wakenhut, Gavin A Whitlock, Katherine S England, Takasuke Mukaiyama, Christoph M Dehnhardt, Jotham W Coe, Steve W Kortum, Jill E Chrencik, David G Brown, etc.

J Med Chem. 2017 Jan 26;60(2):767-786.

PMID: 27983835

Abstract:

By use of a structure-based computational method for identification of structurally novel Janus kinase (JAK) inhibitors predicted to bind beyond the ATP binding site, a potent series of indazoles was identified as selective pan-JAK inhibitors with a type 1.5 binding mode. Optimization of the series for potency and increased duration of action commensurate with inhaled or topical delivery resulted in potent pan-JAK inhibitor 2 (PF-06263276), which was advanced into clinical studies.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1421502626	PF-06263276		1421502-62-6	Price

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