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
1, 2, 3
,
R Ian Storer
1, 2, 3
,
Yogesh A Sabnis
1, 2, 3
,
Florian M Wakenhut
1, 2, 3
,
Gavin A Whitlock
1, 2, 3
,
Katherine S England
1, 2, 3
,
Takasuke Mukaiyama
1, 2, 3
,
Christoph M Dehnhardt
1, 2, 3
,
Jotham W. Coe
1, 2, 3
,
Steve W Kortum
1, 2, 3
,
Jill E. Chrencik
1, 2, 3
,
David G. Brown
1, 2, 3
,
Rhys M Jones
1, 2, 3
,
John R. Murphy
1, 2, 3
,
Thean Yeoh
1, 2, 3
,
Paul Morgan
1, 2, 3
,
Iain Kilty
1, 2, 3
1
Medicine Design, ‡Pharmacokinetics, Dynamics and Metabolism, and §Inflammation and
Immunology Research
Unit, Pfizer Inc., 610 Main Street, Cambridge, Massachusetts 02139, United States
|
2
Medicine Design, and ⊥Medicinal Sciences, Pfizer Inc., 445 Eastern Point Road, Groton, Connecticut 06340, United States
|
3
Worldwide Medicinal Chemistry, ∇Structural Biology
and Biophysics, and ○Pharmaceutical
Sciences, Pfizer Ltd., Ramsgate Road, Sandwich, CT13 9NJ, U.K.
|
Publication type: Journal Article
Publication date: 2017-01-04
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
27983835
Drug Discovery
Molecular Medicine
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.
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Metrics
47
Total citations:
47
Citations from 2024:
6
(12.76%)
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GOST
Copy
Jones P. et al. 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 // Journal of Medicinal Chemistry. 2017. Vol. 60. No. 2. pp. 767-786.
GOST all authors (up to 50)
Copy
Jones P. et al. 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 // Journal of Medicinal Chemistry. 2017. Vol. 60. No. 2. pp. 767-786.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/acs.jmedchem.6b01634
UR - https://doi.org/10.1021/acs.jmedchem.6b01634
TI - 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
T2 - Journal of Medicinal Chemistry
AU - Jones, Peter
AU - Storer, R Ian
AU - Sabnis, Yogesh A
AU - Wakenhut, Florian M
AU - Whitlock, Gavin A
AU - England, Katherine S
AU - Mukaiyama, Takasuke
AU - Dehnhardt, Christoph M
AU - Coe, Jotham W.
AU - Kortum, Steve W
AU - Chrencik, Jill E.
AU - Brown, David G.
AU - Jones, Rhys M
AU - Murphy, John R.
AU - Yeoh, Thean
AU - Morgan, Paul
AU - Kilty, Iain
PY - 2017
DA - 2017/01/04
PB - American Chemical Society (ACS)
SP - 767-786
IS - 2
VL - 60
PMID - 27983835
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2017_Jones,
author = {Peter Jones and R Ian Storer and Yogesh A Sabnis and Florian M Wakenhut and Gavin A Whitlock and Katherine S England and Takasuke Mukaiyama and Christoph M Dehnhardt and Jotham W. Coe and Steve W Kortum and Jill E. Chrencik and David G. Brown and Rhys M Jones and John R. Murphy and Thean Yeoh and Paul Morgan and Iain Kilty and others},
title = {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},
journal = {Journal of Medicinal Chemistry},
year = {2017},
volume = {60},
publisher = {American Chemical Society (ACS)},
month = {jan},
url = {https://doi.org/10.1021/acs.jmedchem.6b01634},
number = {2},
pages = {767--786},
doi = {10.1021/acs.jmedchem.6b01634}
}
Cite this
MLA
Copy
Jones, Peter, et al. “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.” Journal of Medicinal Chemistry, vol. 60, no. 2, Jan. 2017, pp. 767-786. https://doi.org/10.1021/acs.jmedchem.6b01634.