- RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS
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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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- Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis
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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
- Guibbal, Florian,Bénard, Sébastien,Patché, Jessica,Meneyrol, Vincent,Couprie, Jo?l,Yong-Sang, Jennyfer,Meilhac, Olivier,Jestin, Emmanuelle
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p. 787 - 792
(2018/01/17)
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- AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
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The present invention relates to the filed of pharmarcutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) amd a preparation method thereof, a pharmarcutical composition with the compounds as active components, and a use of the azole compounds and the pharmarcutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as deinfed in the specifictaion.
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Paragraph 0154
(2014/05/20)
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- AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
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The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.
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Paragraph 0500
(2014/06/25)
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- Design and synthesis of novel pyrazole-based Lp-PLA2 inhibitors
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A series of novel pyrazole-based lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitors have been designed and synthetized by a variety of acetophenones via a 10-step convergent approach. The synthetic approach is carefully opt
- Wang, Yi,Xu, Weiren,Shao, Hua,Xie, Yafei,Wang, Jianwu
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experimental part
p. 2039 - 2048
(2012/03/26)
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- The identification of clinical candidate SB-480848: A potent inhibitor of lipoprotein-associated phospholipase A2
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Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A2 with sub-nanomolar potency. Cyclopentyl fused derivative 21, SB-480848, showed an enhanced in vitro and in vivo profile versus SB-435495 and has been selected for progression to man.
- Blackie, Josie A.,Bloomer, Jackie C.,Brown, Murray J. B.,Cheng, Hung-Yuan,Hammond, Beverley,Hickey, Deirdre M. B.,Ife, Robert J.,Leach, Colin A.,Lewis, V. Ann,Macphee, Colin H.,Milliner, Kevin J.,Moores, Kitty E.,Pinto, Ivan L.,Smith, Stephen A.,Stansfield, Ian G.,Stanway, Steven J.,Taylor, Maxine A.,Theobald, Colin J.
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p. 1067 - 1070
(2007/10/03)
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