- FUSED PYRAZINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON TAK1
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A compound selected from pyrazine fused-ring derivatives of a chemical formula 1 or pharmaceutically acceptable salts thereof has excellent inhibition activity with respect to TAK1 kinase. A pharmaceutical composition comprising the same is capable of increasing activity of anticancer drugs with respect to cancer or tumor by inhibiting activation of TAK1 kinase, with excellent effects as a prevention agent or a therapeutic agent of cancer or tumor. In the chemical formula 1, A, X, Y, W, Z, E, R^1, and m are the same as defined in the specification.COPYRIGHT KIPO 2016
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Paragraph 0127-0130
(2016/11/02)
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- Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis
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MAPKAPK5 has been proposed to play a role in regulation of matrix metalloprotease expression and so to be a potential target for intervention in rheumatoid arthritis. We present here the identification of a series of compounds against this target which are effective in both biochemical and cell assays. The expansion of the series is described, along with early SAR and pharmacokinetics for some representative compounds.
- Andrews, Martin J.I.,Andrew Clase,Bar, Gregory,Tricarico, Giovanni,Edwards, Paul J.,Brys, Reginald,Chambers, Mark,Schmidt, Wolfgang,MacLeod, Angus,Hirst, Kim,Allen, Vivienne,Birault, Veronique,Le, Joelle,Harris, John,Self, Andrew,Nash, Kevin,Dixon, Graham
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scheme or table
p. 2266 - 2270
(2012/05/04)
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- FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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Novel[1.2.4]triazolo[1,5-a]pyrazine and imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.
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Page/Page column 27
(2009/12/05)
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- IMIDAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula ( I ) represented by the following:The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.
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Page/Page column 47 - 48
(2008/06/13)
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