136117-70-9Relevant articles and documents
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition
Reich, Siegfried H.,Sprengeler, Paul A.,Chiang, Gary G.,Appleman, James R.,Chen, Joan,Clarine, Jeff,Eam, Boreth,Ernst, Justin T.,Han, Qing,Goel, Vikas K.,Han, Edward Z. R.,Huang, Vera,Hung, Ivy N. J.,Jemison, Adrianna,Jessen, Katti A.,Molter, Jolene,Murphy, Douglas,Neal, Melissa,Parker, Gregory S.,Shaghafi, Michael,Sperry, Samuel,Staunton, Jocelyn,Stumpf, Craig R.,Thompson, Peggy A.,Tran, Chinh,Webber, Stephen E.,Wegerski, Christopher J.,Zheng, Hong,Webster, Kevin R.
, p. 3516 - 3540 (2018/05/01)
Dysregulated translation of mRNA plays a major role in tumorigenesis. Mitogen-activated protein kinase interacting kinases (MNK)1/2 are key regulators of mRNA translation integrating signals from oncogenic and immune signaling pathways through phosphoryla
INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
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Page/Page column 90, (2014/02/15)
Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
4,6-DIAMINONICOTINAMIDE COMPOUND
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Page/Page column 43, (2011/09/20)
[Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.
PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
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Page/Page column 41-42, (2012/01/13)
Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.
Prokineticin 1 receptor antagonists
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Page/Page column 42, (2008/12/04)
The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
PROKINETICIN 2 RECEPTOR ANTAGONISTS
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Page/Page column 113, (2010/11/28)
The present invention relates to certain novel compounds of Formula (I): and methods for the treatment of prokineticin 2 or prokinetin 2 receptor mediated disorders.
Imidazo[1,2-a]pyridines. Synthesis and inotropic activity of new 5-imidazo[1,2-a]pyridinyl-2(1H)-pyridinone derivatives
Yamanaka,Miyake,Suda,Ohhara,Ogawa
, p. 1556 - 1567 (2007/10/02)
A series of 1,2-dihydro-5-imidazo[1,2-a]pyridinyl-2(1H)-pyridinones was synthesized and evaluated for positive inotropic activity. 1,2-Dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-3- pyridinecarbonitrile (11a) hydrochloride monohydrate (E-1020) was found to be a potent and selective inhibitor of phosphodiesterase III and a long-acting, potent, orally active positive inotropic agent. Additional imidazo[1,2-a]pyridin-2-yl (3a), -3-yl (16), -7-yl (20) and -8-yl (24a) compounds were also prepared. Altering the pyridine substitution from the 2-position to the 6-position produced a 2-fold increase in the i.v. cardiotonic potency (ED50) from 52 to 23 μg/kg, while substitution at the 3-, 7- or 8-position reduced potency. In the 2-positional isomers, introduction of halogen groups enhanced the activity and 3-chloro-1,2-dihydro-5-(6-fluoroimidazo[1,2-a]pyridin-2-yl)-6-methyl-2(1H)- pyridinone (3a) was the most potent (i.v. ED50 11 μg/kg) in this seris. E-1020 is presently under development for the treatment of congestive heart failure.