RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS
The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of
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Page/Page column 40
(2019/04/26)
Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis
Darapladib is one of the most potent Lp-PLA2 (Lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 0.25 nM. We demonstrate that a crucial step of Darapladib synthesis was not correctly described in the litera
Selective inhibitors and tailored activity probes for lipoprotein- associated phospholipase A2
Lipoprotein-associated phospholipase A2 (Lp-PLA2 or PLA2G7) binds to low-density lipoprotein (LDL) particles, where it is thought to hydrolyze oxidatively truncated phospholipids. Lp-PLA2 has also been implicate
Nagano, Joseph M.G.,Hsu, Ku-Lung,Whitby, Landon R.,Niphakis, Micah J.,Speers, Anna E.,Brown, Steven J.,Spicer, Timothy,Fernandez-Vega, Virneliz,Ferguson, Jill,Hodder, Peter,Srinivasan, Prabhavathi,Gonzalez, Tara D.,Rosen, Hugh,Bahnson, Brian J.,Cravatt, Benjamin F.
p. 839 - 843
(2013/02/25)
NOVEL PROCESSES
This invention relates to methods of making a compound of formula (I) and intermediates for same. The compounds of formula (I) being useful for treating cardiovascular and inflammatory diseases such as atherosclerosis.
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(2011/12/04)
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