Details

Autor(en) / Beteiligte

• Liddle, John
• Atkinson, Francis L.
• Barker, Michael D.
• Carter, Paul S.
• Curtis, Neil R.
• Davis, Rob P.
• Douault, Clement
• Dickson, Marion C.
• Elwes, Dorothy
• Garton, Neil S.
• Gray, Matthew
• Hayhow, Thomas G.
• Hobbs, Clare I.
• Jones, Emma
• Leach, Stuart
• Leavens, Karen
• Lewis, Huw D.
• McCleary, Scott
• Neu, Margarete
• Patel, Vipulkumar K.
• Preston, Alex G.S.
• Ramirez-Molina, Cesar
• Shipley, Tracy J.
• Skone, Philip A.
• Smithers, Nick
• Somers, Donald O.
• Walker, Ann L.
• Watson, Robert J.
• Weingarten, Gordon G.

Titel

Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2011-10, Vol.21 (20), p.6188-6194

Ort / Verlag

Amsterdam: Elsevier Ltd

Erscheinungsjahr

2011

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over liability kinases and hERG activity. GSK143 is a potent and highly selective SYK inhibitor showing good efficacy in the rat Arthus model. The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over liability kinases and hERG activity. GSK143 is a potent and highly selective SYK inhibitor showing good efficacy in the rat Arthus model.