1380429-48-0Relevant academic research and scientific papers
Discovery of Potent and Orally Active Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors as a Potential Therapy for Diabetic Macular Edema
Chen, Xinde,Wang, Kai,Xu, Wenwei,Ma, Quanxin,Chen, Minli,Du, Lili,Mo, Mingguang,Wang, Yiping,Shen, Jianhua
, p. 2674 - 2687 (2016)
Lipoprotein-associated phospholipase A2 (Lp-PLA2) is considered to be a promising therapeutic target for several inflammation-associated diseases. Herein, we describe the discovery of a series of pyrimidone derivatives as Lp-PLA2 inhibitors. Systematic structural modifications led to the identification of several pyrimidone compounds with promising in vitro inhibitory potency and pharmacokinetic properties. Compound 14c, selected for in vivo evaluation, demonstrated decent pharmacokinetic profiles and robust inhibitory potency against Lp-PLA2 in Sprague-Dawley (SD) rats. Furthermore, 14c significantly inhibited retinal thickening in STZ-induced diabetic SD rats as a model of diabetic macular edema (DME) after oral dosing for 4 weeks. Taken together, these results suggested that 14c can serve as a valuable lead in the search for new Lp-PLA2 inhibitors for prevention and/or treatment of DME.
Tricyclic pyrimidone compounds, preparation methods thereof, compositions thereof and uses
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Paragraph 0197-0201, (2022/01/08)
A tricyclic pyrimidone compound shown in formula (I) or its tautomer, racemic racemate, enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt thereof, having a structure shown in formula (I), is a brand new Lp-PLA2 inhibitor that can be used to treat neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis.
Tetracyclic pyrimidinone compound, preparation method, composition and application thereof
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Paragraph 0187-0191, (2021/03/31)
A tetracyclic pyrimidinone compound represented by a formula (I) or a pharmaceutically acceptable salt thereof has a structure represented by a formula (I), is a brand new Lp-PLA2 inhibitor, and can be used for treating neurodegenerative related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis and thelike.
PYRIMIDONE COMPOUNDS USED AS LP-PLA2 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Paragraph 0119; 0120, (2017/11/18)
The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, Rs
PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASES OR CONDITIONS MEDIATED BY LP - PLA2
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Page/Page column 41, (2012/06/30)
The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema (I).
