942999-53-3Relevant academic research and scientific papers
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 138, (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.
