Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase
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
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)
Novel inhibitors of chymase
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.
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Page/Page column 53
(2008/06/13)
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