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Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1

Journal Article · · Bioorganic and Medicinal Chemistry
Not Available
Sponsoring Organization:
USDOE
Grant/Contract Number:
AC02-06CH11357
OSTI ID:
1703820
Alternate ID(s):
OSTI ID: 1833659
OSTI ID: 1837295
Journal Information:
Bioorganic and Medicinal Chemistry, Journal Name: Bioorganic and Medicinal Chemistry Journal Issue: 10 Vol. 28; ISSN 0968-0896
Publisher:
ElsevierCopyright Statement
Country of Publication:
United Kingdom
Language:
English

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Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS) journal July 2015
Selective JAKinibs: Prospects in Inflammatory and Autoimmune Diseases journal January 2019
The γc Family of Cytokines: Basic Biology to Therapeutic Ramifications journal April 2019
Cytokine receptor signaling through the Jak–Stat–Socs pathway in disease journal April 2007
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S )-2,2-Difluorocyclopropyl)((1 R ,5 S )-3-(2-((1-methyl-1 H -pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841) journal May 2018
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165 journal July 2019
ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling journal May 2014
Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases: Miniperspective journal January 2014
Stereochemistry of the Kulinkovich Cyclopropanation of Nitriles journal June 2009
Preclinical to Clinical Translation of Tofacitinib, a Janus Kinase Inhibitor, in Rheumatoid Arthritis journal November 2013
Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity journal November 2016
Utility of animal models for identification of potential therapeutics for rheumatoid arthritis journal November 2007
Prediction of Human Pharmacokinetics From Preclinical Information: Comparative Accuracy of Quantitative Prediction Approaches journal May 2009
Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms journal April 2010
In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494) journal August 2018
Predicting Clearance in Humans from In Vitro Data journal February 2011
Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050 journal April 2010

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