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Paper | Regular issue | Vol 68, No. 10, 2006, pp.2037-2044
Published online, 28th July, 2006
DOI: 10.3987/COM-06-10806
Synthesis of Novel Pyrimido[4,5-c]pyridazines and 1,2-Dihydro-3a,7,9,9b-Tetraaza-cyclopenta[a]naphthalen-3-ones as Potent Inhibitors of Lymphocyte Specific Kinase (LCK)

John C. VanRens, Mark Sabat,* Todd A. Brugel, Jennifer Maier, Matthew J. Laufersweiler, Adam Golebiowski, Steve Berberich, and Biswanath De

*P&G Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Rd, Mason, OH 45040, USA

Abstract

This paper details the synthesis of a novel class of 1,2-dihydro-pyrimido[4,5-c]pyridazines and substituted 1,2-dihydro-3a,7,9,9b- tetraaza-cyclopenta[a]naphthalen-3-one. The most potent analogs disclosed showed low nanomolar activity for the inhibition of lck kinase.