- Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles
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We have previously reported the discovery and initial SAR of the [1,7]naphthyridine-3-carbonitriles and quinoline-3-carbonitriles as Tumor Progression Loci-2 (Tpl2) kinase inhibitors. In this paper, we report new SAR efforts which have led to the identifi
- Kaila, Neelu,Green, Neal,Li, Huan-Qiu,Hu, Yonghan,Janz, Kristin,Gavrin, Lori Krim,Thomason, Jennifer,Tam, Steve,Powell, Dennis,Cuozzo, John,Hall, J. Perry,Telliez, Jean-Baptiste,Hsu, Sang,Nickerson-Nutter, Cheryl,Wang, Qin,Lin, Lih-Ling
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p. 6425 - 6442
(2008/04/05)
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- 4, 6-DIAMINO-[1,7] NAPHTHYRIDINE-3-CARBONITRILE INHIBITORS OF TPL2 KINASE AND METHODS OF MAKING AND USING THE SAME
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The present invention provides compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, m and n are defined as described herein. The inventio
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Page/Page column 18; 38-39
(2010/11/25)
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- Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationships
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The synthesis and structure-activity studies of a series of 6-substituted-4-anilino-[1,7]-naphthyridine-3-carbonitriles as inhibitors of Tpl2 kinase are described. The early exploratory work described here may lead to the discovery of compounds with signi
- Gavrin, Lori Krim,Green, Neal,Hu, Yonghan,Janz, Kristin,Kaila, Neelu,Li, Huan-Qiu,Tam, Steve Y.,Thomason, Jennifer R.,Gopalsamy, Ariamala,Ciszewski, Greg,Cuozzo, John W.,Hall, J. Perry,Hsu, Sang,Telliez, Jean-Baptiste,Lin, Lih-Ling
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p. 5288 - 5292
(2007/10/03)
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- Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles
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The syntheses and EGFR kinase inhibitory activity of a series of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles are described. Both reversible and irreversible binding inhibitors were prepared. These series were compared with each other and with the corresponding 4-anilinoquinoline-3-carbonitriles. Compounds having a 1,7-naphthyridine core structure can retain high potency while those with a 1,8-naphthyridine core are significantly less active. These results are consistent with molecular modeling observations.
- Wissner, Allan,Hamann, Philip R.,Nilakantan, Ramaswamy,Greenberger, Lee M.,Ye, Fei,Rapuano, Timothy A.,Loganzo, Frank
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p. 1411 - 1416
(2007/10/03)
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- SUBSTITUTED-3-CYANO-[1.7],[1.5], AND [1.8]-NAPHTHYRIDINE INHIBITORS OF TYROSINE KINASES
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This invention provides compounds of formula (I) having structure (a) wherein A'' is a diavalent moiety selected from the group (a, b, c) which are useful as inhibitors of protein tyrosine kinase.
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