454464-38-1Relevant articles and documents
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
Synthesis and evaluation of an orally available “Y”-shaped biaryl peroxisome proliferator-activated receptor δ agonist
Kim, Dong-Su,Lee, Jaehwan,Londhe, Ashwini M.,Kadayat, Tara Man,Joo, Jeongmin,Hwang, Hayoung,Kim, Kyung-Hee,Pae, Ae Nim,Chin, Jungwook,Cho, Sung Jin,Kang, Heonjoong
, p. 4382 - 4389 (2018/07/30)
In this study, we designed and synthesized several novel “Y”-shaped biaryl PPARδ agonists. Structure-activity relationship (SAR) studies demonstrated that compound 3a was the most active agonist with an EC50 of 2.6 nM. We also synthesized and evaluated enantiospecific R and S isomers of compound 3a to confirm that R isomer (EC50 = 0.7 nM) shows much more potent activity than S isomer (EC50 = 6.1 nM). Molecular docking studies between the PPAR ligand binding domain and enantiospecific R and S isomers of compound 3a were performed. In vitro absorption, distribution, metabolism, excretion, and toxicity (ADMET) and in vivo PK profiles show that compound 3a possesses superior drug-like properties including good bioavailability. Our overall results clearly demonstrate that this orally administrable PPARδ agonist 3a is a viable drug candidate for the treatment of various PPARδ-related disorders.
Tetrazole Derivatives and Their Use for the Treatment of Cardiovascular Diseases
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, (2009/09/07)
The present application relates to novel tetrazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especial