304694-40-4Relevant academic research and scientific papers
Oxazolidinone compound as well as preparation method, application and pharmaceutical composition thereof
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, (2020/11/05)
The invention relates to an oxazolidinone compound used as an Lp-PLA2 covalent inhibitor and a pharmaceutical composition of the oxazolidinone compound, the structure of the oxazolidinone compound isshown as a general formula I, and R1, R2 and R3 are defined as the specification and claims. The compound shown in the general formula I or the stereoisomer or the pharmaceutically acceptable salt thereof can be used as the Lp-PLA2 covalent inhibitor to prevent and/or treat and/or improve diseases related to Lp-PLA2 enzyme activity. Meanwhile, the stereoisomer or the pharmaceutically acceptable salt of the compound shown in the general formula I can be used as an Lp-PLA2 specific molecular probe.
RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS
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, (2019/04/26)
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
Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis
Guibbal, Florian,Bénard, Sébastien,Patché, Jessica,Meneyrol, Vincent,Couprie, Jo?l,Yong-Sang, Jennyfer,Meilhac, Olivier,Jestin, Emmanuelle
, p. 787 - 792 (2018/01/17)
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
PROCESSES FOR THE PREPARATION OF DARAPLADIB AND ITS INTERMEDIATES
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Paragraph 17, (2015/06/25)
The present invention provides a process for the preparation of ethyl {2-[(4- fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl}acetate of Formula 4, {2-[(4-fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta [d]pyri
Selective inhibitors and tailored activity probes for lipoprotein- associated phospholipase A2
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.
supporting information, p. 839 - 843 (2013/02/25)
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
NOVEL PROCESSES
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Page/Page column 9-10, (2011/12/04)
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.
3-BENZYLTHIO-1,2,4-TRIAZINE-5 (2H)-ONE AS PAF-AH INHIBITORS
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Page/Page column 28, (2010/11/08)
The invention relates to 3-benzylthio-1,2,4-triazine-5 (2H)-one of formula I, methods for the production thereof, and the use thereof for producing medicaments that are used for the treatment and/or prevention of diseases, especially chronic inflammatory diseases, such as diseases of the rheumatic type, and cardiovascular diseases, e.g. dyslipidemia, arteriosclerosis, and coronary heart diseases.
SUBSTITUTED 1,2,4-TRIAZIN-5(2H)-ONES
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Page/Page column 31, (2010/11/08)
The invention relates to substituted 1,2,4-triazin-5(2H)-ones, to a method for the production thereof, and to their use for producing medicaments for treating and/or preventing diseases, particularly chronic inflammatory diseases, for example, rheumatoid
3-CYCLOALKYL-1,2,4-TRIAZIN-5(2H)-ONES
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Page/Page column 24-25, (2010/11/08)
The invention relates to 3-cycloalkyl-1,2,4-triazin-5(2H)-ones, to a method for the production thereof, and to their use for producing medicaments for treating and/or preventing diseases, particularly chronic inflammatory diseases, for example, rheumatoid
