- A simple debenzylation of O-substituted phenol ethers using hydrobromic acid in presence of phase transfer catalyst
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A simple methodology for the debenzylation of ortho substituted phenol ethers in two phase system with aqueous hydrobromic acid in the presence of tetrabutylammonium bromide as a phase transfer catalyst is described.
- Bhalerao,Raju,Neelakantan
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- Photolytic cleavage and condensation reactions of cyclohexa-2,4-dienones with diamines
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Cyclohexa-2,4-diene-1-one sulfone derivative undergoes ring cleavage to afford bis-amides containing a diene moiety on irradiation with visible light in the presence of various diamines.
- Kim, Young Mee,Song, Suk Jin,Kwon, Tae Woo,Chung, Sung Kee
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- Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3- yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a highly selective thyroid hormone receptor β agonist in clinical trials for the treatment of dyslipidemia
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The beneficial effects of thyroid hormone (TH) on lipid levels are primarily due to its action at the thyroid hormone receptor β (THR-β) in the liver, while adverse effects, including cardiac effects, are mediated by thyroid hormone receptor α (THR-α). A pyridazinone series has been identified that is significantly more THR-β selective than earlier analogues. Optimization of this series by the addition of a cyanoazauracil substituent improved both the potency and selectivity and led to MGL-3196 (53), which is 28-fold selective for THR-β over THR-α in a functional assay. Compound 53 showed outstanding safety in a rat heart model and was efficacious in a preclinical model at doses that showed no impact on the central thyroid axis. In reported studies in healthy volunteers, 53 exhibited an excellent safety profile and decreased LDL cholesterol (LDL-C) and triglycerides (TG) at once daily oral doses of 50 mg or higher given for 2 weeks.
- Kelly, Martha J.,Pietranico-Cole, Sherrie,Larigan, J. Douglas,Haynes, Nancy-Ellen,Reynolds, Charles H.,Scott, Nathan,Vermeulen, John,Dvorozniak, Mark,Conde-Knape, Karin,Huang, Kuo-Sen,So, Sung-Sau,Thakkar, Kshitij,Qian, Yimin,Banner, Bruce,Mennona, Frank,Danzi, Sara,Klein, Irwin,Taub, Rebecca,Tilley, Jefferson
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p. 3912 - 3923
(2014/06/09)
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- P-Hydroxyphenacyl photoremovable protecting groups Robust photochemistry despite substituent diversity
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A broadly based investigation of the effects of a diverse array of substituents on the photochemical rearrangement of p-hydroxyphenacyl esters has demonstrated that common substituents such as F, MeO, CN, CO2R, CONH2, and CH3 have little effect on the rate and quantum efficiencies for the photo-Favorskii rearrangement and the release of the acid leaving group or on the lifetimes of the reactive triplet state. A decrease in the quantum yields across all substituents was observed for the release and rearrangement when the photolyses were carried out in buffered aqueous media at pHs that exceeded the ground-state pKa of the chromophore where the conjugate base is the predominant form. Otherwise, substituents have only a very modest effect on the photoreaction of these robust chromophores.
- Givens, Richard S.,Stensrud, Kenneth,Conrad, Peter G.,Yousef, Abraham L.,Perera, Chamani,Senadheera, Sanjeewa N.,Heger, Dominik,Wirz, Jakob
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scheme or table
p. 364 - 384
(2011/06/22)
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- PYRIDAZINONE DERIVATIVES AS THYROID HORMONE RECEPTOR AGONISTS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.
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Page/Page column 62-63
(2008/06/13)
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- Substituted compounds derived from N-(benzyl)phenylacetamide, preparation and uses
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This invention relates to poly-substituted derivatives of the N-(benzyl)phenylacetamide type, pharmaceutical compositions comprising same, therapeutic uses thereof, more particularly in the fields of human and animal health. This invention also relates to a process for the preparation of such derivatives.
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Page/Page column 46
(2010/10/20)
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