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Mui Cheung,
Philip A Harris,
Jennifer G Badiang,
Gregory E Peckham,
Stanley D Chamberlain, Michael J Alberti,
David K Jung,
Stephanie S Harris,
Neal H Bramson,
Andrea H Epperly,
Stephen A Stimpson,
Michael R Peel
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ABSTRACT: A series of pyrazolo[1,5-a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series are described.
Bioorganic & medicinal chemistry letters 10/2008; 18(20):5428-30. · 2.65 Impact Factor
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ABSTRACT: [reaction: see text] A convergent synthesis of substituted pyrazolo[1,5-a]pyridines has been achieved either via a regioselective [3 + 2] cycloaddition of N-aminopyridines with alkynes or by thermal cyclization of disubstituted azirines. Subsequent palladium-catalyzed introduction of pyridines or de novo synthesis of pyrimidines affords inhibitors of p38 kinase.
Organic Letters 11/2005; 7(21):4753-6. · 5.86 Impact Factor
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ABSTRACT: The discovery, synthesis, potential binding mode, and in vitro kinase profile of several pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines as potent kinase inhibitors are discussed.
Bioorganic & Medicinal Chemistry Letters 09/2005; 15(16):3778-81. · 2.55 Impact Factor
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Mark J Bamford, Michael J Alberti,
Nicholas Bailey,
Susannah Davies,
David K Dean,
Alessandra Gaiba,
Stephen Garland,
John D Harling,
David K Jung,
Terence A Panchal,
Christopher A Parr,
Jon G Steadman,
Andrew K Takle,
James T Townsend,
David M Wilson,
Jason Witherington
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ABSTRACT: A novel series of imidazo[4,5-c]pyridines bearing a 1,2,5-oxadiazol-3-ylamine functionality has been developed. These are potent inhibitors of mitogen and stress-activated protein kinase-1.
Bioorganic & Medicinal Chemistry Letters 08/2005; 15(14):3402-6. · 2.55 Impact Factor