- 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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- Inhibition of Tpl2 kinase and TNFα production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis
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The synthesis and structure-activity studies of a series of quinoline-3-carbonitriles as inhibitors of Tpl2 kinase are described. Potent inhibitors of Tpl2 kinase with selectivity against a panel of selected kinases in enzymatic assays and specificity in cell-based phosphorylation assays in LPS-treated human monocytes were identified. Selected inhibitors with moderate activity in human whole blood assay effectively inhibited LPS/D-Gal induced TNFα release when administered intraperitoneally in mice.
- Hu, Yonghan,Green, Neal,Gavrin, Lori K.,Janz, Kristin,Kaila, Neelu,Li, Huan-Qiu,Thomason, Jennifer R.,Cuozzo, John W.,Hall, J. Perry,Hsu, Sang,Nickerson-Nutter, Cheryl,Telliez, Jean-Baptiste,Lin, Lih-Ling,Tam, Steve
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p. 6067 - 6072
(2007/10/03)
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- USE OF CYANOQUINOLINES FOR TREATING OR INHIBITING COLONIC POLYPS
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This invention provides a method of treating or inhibiting colonic polyps which comprises providing a compound of formula (1); wherein R1, R2, R3, R4, X, Y, and n are defined hereinbefore, or a pharmaceutically acceptable salt thereof.
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- SUBSTITUTED 3-CYANOQUINOLINES AS PROTEIN TYROSINE KINASES INHIBITORS
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This invention provides compounds of formula (1) wherein R1, G1, G2, R4, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof, which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
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- Method of treating or inhibiting colonic polyps
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This invention provides a method of treating or inhibiting colonic polyps which comprises providing a compound of formula 1 wherein:R1, R2, R3, R4, X, Y, and n are as defined hereinbefore, or a pharmaceutically acceptable salt thereof.
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- Substituted 3-cyanoquinolines
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This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
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