862094-56-2Relevant academic research and scientific papers
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase
Greco, Michael N.,Hawkins, Michael J.,Powell, Eugene T.,Almond Jr., Harold R.,De Garavilla, Lawrence,Hall, Jeffrey,Minor, Lisa K.,Wang, Yuanping,Corcoran, Thomas W.,Di Cera, Enrico,Cantwell, Angelene M.,Savvides, Savvas N.,Damiano, Bruce P.,Maryanoff, Bruce E.
, p. 1727 - 1730 (2008/02/02)
A series of β-carboxamido-phosphon(in)ic acids (2) was identified as a new structural motif for obtaining potent inhibitors of human mast cell chymase. For example, 1-naphthyl derivative 5f had an IC50 value of 29 nM and (E)-styryl derivative 6
Novel inhibitors of chymase
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Page/Page column 62, (2008/06/13)
The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
