Discovery of highly potent and selective Bruton’s tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability

Young, Wendy B.; Barbosa, James; Blomgren, Peter; Bremer, Meire C.; Crawford, James J.; Dambach, Donna; Eigenbrot, Charles; Gallion, Steve; Johnson, Adam R.; Kropf, Jeffrey E.; Lee, Seung H.; Liu, Lichuan; Lubach, Joseph W.; Macaluso, Jen; Maciejewski, Pat; Mitchell, Scott A.; Ortwine, Daniel F.; Di Paolo, Julie; Reif, Karin; Scheerens, Heleen; Schmitt, Aaron; Wang, Xiaojing; Wong, Harvey; Xiong, Jin-Ming; Xu, Jianjun; Yu, Christine; Zhao, Zhongdong; Currie, Kevin S.

doi:10.1016/j.bmcl.2015.11.076

Title: Discovery of highly potent and selective Bruton’s tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability

Journal Article · Fri Jan 01 00:00:00 EST 2016 · Bioorganic and Medicinal Chemistry Letters

DOI:https://doi.org/10.1016/j.bmcl.2015.11.076· OSTI ID:1358848

Young, Wendy B.; Barbosa, James; Blomgren, Peter; Bremer, Meire C.; Crawford, James J.; Dambach, Donna; Eigenbrot, Charles; Gallion, Steve; Johnson, Adam R.; Kropf, Jeffrey E.; Lee, Seung H.; Liu, Lichuan; Lubach, Joseph W.; Macaluso, Jen; Maciejewski, Pat; Mitchell, Scott A.; Ortwine, Daniel F.; Di Paolo, Julie; Reif, Karin; Scheerens, Heleen more »

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Sponsoring Organization:: USDOE

Grant/Contract Number:: AC02-76SF00515

OSTI ID:: 1358848

Journal Information:: Bioorganic and Medicinal Chemistry Letters, Journal Name: Bioorganic and Medicinal Chemistry Letters Vol. 26 Journal Issue: 2; ISSN 0960-894X

Publisher:: ElsevierCopyright Statement

Country of Publication:: United Kingdom

Language:: English

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Cited by: 32 works

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References (12)

B-Cell Receptor Signaling Inhibitors for Treatment of Autoimmune Inflammatory Diseases and B-Cell Malignancies Puri, Kamal D.; Di Paolo, Julie A.; Gold, Michael R. International Reviews of Immunology, Vol. 32, Issue 4 https://doi.org/10.3109/08830185.2013.818140	journal	July 2013
A Novel Reaction Mediated by Human Aldehyde Oxidase: Amide Hydrolysis of GDC-0834 Sodhi, Jasleen K.; Wong, Susan; Kirkpatrick, Donald S. Drug Metabolism and Disposition, Vol. 43, Issue 6 https://doi.org/10.1124/dmd.114.061804	journal	April 2015
Mini-Review: Bmx Kinase Inhibitors for Cancer Therapy Jarboe, John; Dutta, Shilpa; Velu, Sadanandan Recent Patents on Anti-Cancer Drug Discovery, Vol. 8, Issue 3 https://doi.org/10.2174/15748928113089990043	journal	June 2013
Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase Inhibitor Liu, Lichuan; Halladay, Jason S.; Shin, Young Drug Metabolism and Disposition, Vol. 39, Issue 10 https://doi.org/10.1124/dmd.111.040840	journal	July 2011
Tec kinases regulate T-lymphocyte development and function: new insights into the roles of Itk and Rlk/Txk Readinger, Julie A.; Mueller, Kristen L.; Venegas, Ana M. Immunological Reviews, Vol. 228, Issue 1 https://doi.org/10.1111/j.1600-065X.2008.00757.x	journal	March 2009
The role of Bruton's tyrosine kinase in B-cell development and function: a genetic perspective Satterthwaite1, Anne B.; Witte1,2, Owen N. Immunological Reviews, Vol. 175, Issue 1 https://doi.org/10.1111/j.1600-065X.2000.imr017504.x	journal	June 2000
Specific Btk inhibition suppresses B cell– and myeloid cell–mediated arthritis Di Paolo, Julie A.; Huang, Tao; Balazs, Mercedesz Nature Chemical Biology, Vol. 7, Issue 1 https://doi.org/10.1038/nchembio.481	journal	November 2010
Potent and selective Bruton’s tyrosine kinase inhibitors: Discovery of GDC-0834 Young, Wendy B.; Barbosa, James; Blomgren, Peter Bioorganic & Medicinal Chemistry Letters, Vol. 25, Issue 6 https://doi.org/10.1016/j.bmcl.2015.01.032	journal	March 2015
Design, synthesis, and molecular modelling of pyridazinone and phthalazinone derivatives as protein kinases inhibitors Elagawany, Mohamed; Ibrahim, Mohamed A.; Ali Ahmed, Hany Emary Bioorganic & Medicinal Chemistry Letters, Vol. 23, Issue 7 https://doi.org/10.1016/j.bmcl.2013.02.027	journal	April 2013
BMX and Its Role in Inflammation, Cardiovascular Disease, and Cancer Cenni, Bruno; Gutmann, Sascha; Gottar-Guillier, Marie International Reviews of Immunology, Vol. 31, Issue 2 https://doi.org/10.3109/08830185.2012.663838	journal	March 2012
Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders Robak, Tadeusz; Robak, Ewa Expert Opinion on Investigational Drugs, Vol. 21, Issue 7 https://doi.org/10.1517/13543784.2012.685650	journal	May 2012
The Role of Tec Family Kinases in Myeloid Cells Schmidt, Uwe; Boucheron, Nicole; Unger, Bernd International Archives of Allergy and Immunology, Vol. 134, Issue 1 https://doi.org/10.1159/000078339	journal	January 2004

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