- Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists
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A novel series of 1,3-bistrifluoromethylcarbinol derivatives that act as liver X receptor (LXR) β-selective agonists was discovered. Structure-activity relationship studies led to the identification of molecule 62, which was more effective (Emax) and selective toward LXRβ than T0901317 and GW3965. Furthermore, 62 decreased LDL-C without elevating the plasma TG level and significantly suppressed the lipid-accumulation area in the aortic arch in a Bio F1B hamster fed a diet high in fat and cholesterol. We demonstrated that our LXRβ agonist would be potentially useful as a hypolipidemic and anti-atherosclerotic agent. In this manuscript, we report the design, synthesis and pharmacology of 1,3-bistrifluoromethylcarbinol derivatives.
- Koura, Minoru,Matsuda, Takayuki,Okuda, Ayumu,Watanabe, Yuichiro,Yamaguchi, Yuki,Kurobuchi, Sayaka,Matsumoto, Yuuki,Shibuya, Kimiyuki
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p. 2668 - 2674
(2015/06/08)
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- CARBINOL DERIVATIVES HAVING CYCLIC LINKER
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[Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.
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Page/Page column 14
(2010/03/31)
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- SUBSTITUTED CARBINOL COMPOUND
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There is provided a novel LXRβ agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caus
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Page/Page column 15-16
(2009/09/26)
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- Ester composition
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The invention relates to a method for preparing an ester composition in which at least one activated phenolic ether group of a molecule is reacted with at least one haloformyl group of another molecule.
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