The discovery of setileuton, a potent and selective 5-lipoxygenase inhibitor
The discovery of novel and selective inhibitors of human 5-lipoxygenase (5-LO) is described. These compounds are potent, orally bioavailable, and active at inhibiting leukotriene biosynthesis in vivo in a dog PK/PD model. A major focus of the optimization
Ducharme, Yves,Blouin, Marc,Brideau, Christine,Chateauneuf, Anne,Gareau, Yves,Grimm, Erich L.,Juteau, Helene,Laliberte, Sebastien,MacKay, Bruce,Masse, Frederic,Ouellet, Marc,Salem, Myriam,Styhler, Angela,Friesen, Richard W.
scheme or table
p. 170 - 174
(2010/10/21)
α-TRIFLUOROMETHYL-α-HYDROXY CARBOXYLIC ACIDS
The methyl esters of α-trifluoromethyl-α-hydroxy carboxylic acids were obtained by the reaction of methyl trifluoropyruvate with organometallic reagents (Cd, Mg, Zn).The characteristic features of the reactions in relation to the nature of the alkylating agent were demonstrated.
Soloshonok, V. A.,Gerus, I. I.,Yagupol'skii, Yu. L.,Kukhar', V. P.
p. 1298 - 1303
(2007/10/02)
Amide derivatives
The disclosure relates to novel 3,4-disubstituted-branched-chain-fluorinated-acylanilides, processes for their manufacture and pharmaceutical compositions containing them. The compounds possess antiandrogenic activity. Representative of the compounds disclosed is 4-nitro-3-trifluoromethyl-(2-hydroxy-2-trifluoromethylpropionyl)anilide.
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(2008/06/13)
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