155269-60-6Relevant articles and documents
Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCθ inhibitors
Boschelli, Diane H.,Subrath, Joan,Niu, Chuansheng,Wu, Biqi,Wang, Yan,Lee, Julie,Brennan, Agnes,Ho, Melisa,Deng, Bijia,Yang, Xiaoke,Xu, Xin,Leung, Louis,Wang, Jianyao,Atherton, James,Chaudhary, Divya
, p. 1965 - 1968 (2010)
Analog 8, a 3-pyridinecarbonitrile with an (E)-2-{6-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl}vinyl group at C-5, had an IC50 value of 1.1 nM for the inhibition of PKCθ and potently blocked the production of IL-2 in both stimulated murine T cells (IC50 = 34 nM) and human whole blood (IC50 = 500 nM).
PYRIDINE DERIVATIVE AND MEDICINE
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, (2015/07/15)
The main purpose of the invention is to provide a novel pyridine derivative or a pharmaceutically acceptable salt thereof. Examples of the invention include a pyridine derivative represented by general formula [1], and a pharmaceutically acceptable salt thereof. This compound or a pharmaceutically acceptable salt thereof exhibits mGluR5 inhibitory activity, and can therefore be used as an agent for the prevention or treatment of, e.g., pain (for example, acute pain, chronic pain, inflammatory pain, neuropathic pain, hyperalgesia, thermal hyperalgesia, allodynia, pain due to noxious thermal stimulation, pain due to noxious mechanical stimulation, pain in the lower urinary tract or reproductive organs, or migraine), pruritus, lower urinary tract symptoms or lower urinary tract dysfunctions, gastroesophageal reflux disease (GERD), gastroesophageal reflux associated with transient lower esophageal sphincter relaxation (TLESR), and diseases of the central nervous system.
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors
Boschelli, Diane H.,Wang, Daniel,Wang, Yan,Wu, Biqi,Honores, Erick E.,Barrios Sosa, Ana Carolina,Chaudhary, Inder,Golas, Jennifer,Lucas, Judy,Boschelli, Frank
scheme or table, p. 2924 - 2927 (2010/07/04)
The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC50 values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study.
5-ALKYL/ALKENYL-3-CYANOPYRIDINES AS KINASE INHIBITORS
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Page/Page column 167, (2009/07/17)
Described herein are compounds of formula I: wherein G is and pharmaceutically acceptable salts thereof, wherein J, X, R1, R2, R11, R12' and p are as defined herein. Also provided herein are methods of making the compounds of formula I, and methods of using these compounds for inhibiting or treating a pathological condition or disorder linked to or mediated by a protein kinase in a mammal.
Branch-selective reductive coupling of 2-vinyl pyridines and imines via rhodium catalyzed C-C bond forming hydrogenation
Komanduri, Venukrishnan,Grant, Christopher D.,Krische, Michael J.
supporting information; experimental part, p. 12592 - 12593 (2009/05/08)
Hydrogenation of 2-vinyl azines 1a-1e in the presence of N-arylsulfonyl imines 2a-2l at ambient temperature and pressure employing cationic rhodium catalysts ligated by tri-2-furylphosphine results in regioselective reductive coupling to furnish branched