352705-03-4Relevant academic research and scientific papers
BICYCLIC PYRIMIDONE COMPOUNDS AS INHIBITORS OF LP-PLA2
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, (2014/08/07)
The present invention relates to novel pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator
Frederickson, Martyn,Callaghan, Owen,Chessari, Gianni,Congreve, Miles,Cowan, Suzanna R.,Matthews, Julia E.,McMenamin, Rachel,Smith, Donna-Michelle,Vinkovic, Mladen,Wallis, Nicola G.
, p. 183 - 186 (2008/09/19)
Fragment-based lead discovery has been applied to urokinase-type plasminogen activator (uPA). The (R)-enantiomer of the orally active drug mexiletine 5 (a fragment hit from X-ray crystallographic screening) was the chemical starting point. Structure-aided
THERAPEUTIC COMPOUNDS
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Page/Page column 61, (2010/11/27)
This invention relates to a novel class of substituted amino-ethoxy benzene derivatives of formula (I) which are inhibitors of serine proteases and to their use in treating aberrant serine protease activity in a mammal, contraception, anti-coagulant methods and methods for treating aberrant cell proliferation, tumours, cancer, angiogenesis, angiogenesis-based retinopathies, autoimmummune disease, inflammation, skin disease, arthritis, rheutmatoid arthritis, asthma, osteoarthritis and multiple sclerosis. (I), Wherein Rm, Rn, Rp, Rq, V, W, X, Y and R8 are as defined in the claims.
Cannabimimetic lipid amides as useful medications
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Page/Page column 3-4, (2010/11/25)
Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor aff
