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

Fensome, Andrew; Ambler, Catherine M.; Arnold, Eric; Banker, Mary Ellen; Clark, James D.; Dowty, Martin E.; Efremov, Ivan V.; Flick, Andrew; Gerstenberger, Brian S.; Gifford, Roger S.; Gopalsamy, Ariamala; Hegen, Martin; Jussif, Jason; Limburg, David C.; Lin, Tsung H.; Pierce, Betsy S.; Sharma, Raman; Trujillo, John I.; Vajdos, Felix F.; Vincent, Fabien; Wan, Zhao-Kui; Xing, Li; Yang, Xiaojing; Yang, Xin

doi:10.1016/j.bmc.2020.115481

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

Journal Article · Fri May 01 04:00:00 EDT 2020 · Bioorg. Med. Chem. Lett.

DOI:https://doi.org/10.1016/j.bmc.2020.115481· OSTI ID:1837295

Fensome, Andrew; Ambler, Catherine M.; Arnold, Eric; Banker, Mary Ellen; Clark, James D.; Dowty, Martin E.; Efremov, Ivan V.; Flick, Andrew; Gerstenberger, Brian S.; Gifford, Roger S.; Gopalsamy, Ariamala; Hegen, Martin; Jussif, Jason; Limburg, David C.; Lin, Tsung H.; Pierce, Betsy S.; Sharma, Raman; Trujillo, John I.; Vajdos, Felix F.; Vincent, Fabien more »

Research Organization:: Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)

Sponsoring Organization:: DOE - Office Of Science; INDUSTRY

OSTI ID:: 1837295

Journal Information:: Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (10) Vol. 28

Country of Publication:: United States

Language:: ENGLISH

References (19)

Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity Dendrou, C. A.; Cortes, A.; Shipman, L. Science Translational Medicine, Vol. 8, Issue 363 https://doi.org/10.1126/scitranslmed.aag1974	journal	November 2016
Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases: Miniperspective Clark, James D.; Flanagan, Mark E.; Telliez, Jean-Baptiste Journal of Medicinal Chemistry, Vol. 57, Issue 12 https://doi.org/10.1021/jm401490p	journal	January 2014
In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494) Parmentier, Julie M.; Voss, Jeff; Graff, Candace BMC Rheumatology, Vol. 2, Issue 1 https://doi.org/10.1186/s41927-018-0031-x	journal	August 2018
Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050 Fridman, Jordan S.; Scherle, Peggy A.; Collins, Robert The Journal of Immunology, Vol. 184, Issue 9 https://doi.org/10.4049/jimmunol.0902819	journal	April 2010
Preclinical to Clinical Translation of Tofacitinib, a Janus Kinase Inhibitor, in Rheumatoid Arthritis Dowty, Martin E.; Jesson, Michael I.; Ghosh, Sarbani Journal of Pharmacology and Experimental Therapeutics, Vol. 348, Issue 1 https://doi.org/10.1124/jpet.113.209304	journal	November 2013
The γc Family of Cytokines: Basic Biology to Therapeutic Ramifications Leonard, Warren J.; Lin, Jian-Xin; O'Shea, John J. Immunity, Vol. 50, Issue 4 https://doi.org/10.1016/j.immuni.2019.03.028	journal	April 2019
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165 Wrobleski, Stephen T.; Moslin, Ryan; Lin, Shuqun Journal of Medicinal Chemistry, Vol. 62, Issue 20 https://doi.org/10.1021/acs.jmedchem.9b00444	journal	July 2019
Stereochemistry of the Kulinkovich Cyclopropanation of Nitriles Astashko, Dmitry; Lee, Hyung Goo; Bobrov, Denis N. The Journal of Organic Chemistry, Vol. 74, Issue 15 https://doi.org/10.1021/jo900823h	journal	June 2009
Selective JAKinibs: Prospects in Inflammatory and Autoimmune Diseases T. Virtanen, Anniina; Haikarainen, Teemu; Raivola, Juuli BioDrugs, Vol. 33, Issue 1 https://doi.org/10.1007/s40259-019-00333-w	journal	January 2019
Utility of animal models for identification of potential therapeutics for rheumatoid arthritis Hegen, M.; Keith, J. C.; Collins, M. Annals of the Rheumatic Diseases, Vol. 67, Issue 11 https://doi.org/10.1136/ard.2007.076430	journal	November 2007
Anti-IL-23 and Anti-IL-17 Biologic Agents for the Treatment of Immune-Mediated Inflammatory Conditions Frieder, Jillian; Kivelevitch, Dario; Haugh, Isabel Clinical Pharmacology & Therapeutics, Vol. 103, Issue 1 https://doi.org/10.1002/cpt.893	journal	October 2017
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) Fensome, Andrew; Ambler, Catherine M.; Arnold, Eric Journal of Medicinal Chemistry, Vol. 61, Issue 19 https://doi.org/10.1021/acs.jmedchem.8b00917	journal	May 2018
Predicting Clearance in Humans from In Vitro Data Scott Obach, R. Current Topics in Medicinal Chemistry, Vol. 11, Issue 4 https://doi.org/10.2174/156802611794480873	journal	February 2011
Cytokine receptor signaling through the Jak–Stat–Socs pathway in disease O'Sullivan, Lynda A.; Liongue, Clifford; Lewis, Rowena S. Molecular Immunology, Vol. 44, Issue 10 https://doi.org/10.1016/j.molimm.2006.11.025	journal	April 2007
Prediction of Human Pharmacokinetics From Preclinical Information: Comparative Accuracy of Quantitative Prediction Approaches Hosea, Natilie A.; Collard, Wendy T.; Cole, Susan The Journal of Clinical Pharmacology, Vol. 49, Issue 5 https://doi.org/10.1177/0091270009333209	journal	May 2009
Development of a new permeability assay using low‐efflux MDCKII cells Di, Li; Whitney‐Pickett, Carrie; Umland, John P. Journal of Pharmaceutical Sciences, Vol. 100, Issue 11 https://doi.org/10.1002/jps.22674	journal	November 2011
Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS) Varma, Manthena V.; Steyn, Stefanus J.; Allerton, Charlotte Pharmaceutical Research, Vol. 32, Issue 12 https://doi.org/10.1007/s11095-015-1749-4	journal	July 2015
Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms Quintás-Cardama, Alfonso; Vaddi, Kris; Liu, Phillip Blood, Vol. 115, Issue 15 https://doi.org/10.1182/blood-2009-04-214957	journal	April 2010
ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling Thorarensen, Atli; Banker, Mary Ellen; Fensome, Andrew ACS Chemical Biology, Vol. 9, Issue 7 https://doi.org/10.1021/cb5002125	journal	May 2014

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