Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: Discovery of 2-[4-(3-{(R)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]- N, N -dimethyl-acetamide (BI 665915)
The synthesis, structure-activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. The use of structure-guided drug design techniques provided compounds that demonstrated excellent FLAP binding potency (IC50 4 synthesis in human whole blood (IC50 4 production.
Takahashi, Hidenori,Riether, Doris,Bartolozzi, Alessandra,Bosanac, Todd,Berger, Valentina,Binetti, Ralph,Broadwater, John,Chen, Zhidong,Crux, Rebecca,De Lombaert, Stéphane,Dave, Rajvee,Dines, Jonathon A.,Fadra-Khan, Tazmeen,Flegg, Adam,Garrigou, Michael,Hao, Ming-Hong,Huber, John,Hutzler, J. Matthew,Kerr, Steven,Kotey, Adrian,Liu, Weimin,Lo, Ho Yin,Loke, Pui Leng,Mahaney, Paige E.,Morwick, Tina M.,Napier, Spencer,Olague, Alan,Pack, Edward,Padyana, Anil K.,Thomson, David S.,Tye, Heather,Wu, Lifen,Zindell, Renee M.,Abeywardane, Asitha,Simpson, Thomas
p. 1669 - 1690
(2015/04/21)
OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
The present invention relates to compound of formula (I) and pharmaceutically acceptable salt thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 128; 197
(2012/03/26)
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