- SUBSTITUTED PIPERAZINES
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Disclosed herein are substituted piperazine late Na+ channel modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 32
(2009/01/24)
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- SUBSTITUTED PYRIMIDINES
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Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 38
(2008/12/07)
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- DEUTERATED PIPERAZINE DERIVATIVES AS ANTI-ANGINAL COMPOUNDS
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This invention relates to novel compounds of formula A that partially inhibit fatty acid oxidation and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel compounds that are derivatives of ranolazine. This invention also provides compositions comprising one or more compound of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by partial fatty acid oxidation inhibitors, such as ranolazine. (Formula A), wherein at least one of Y or R comprises a deuterium atom.
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Page/Page column 23-24
(2008/12/08)
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- Determination of 4-hydroxy-3-methoxyphenylethylene glycol 4-sulfate in human urine using liquid chromatography-tandem mass spectrometry
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A major metabolite of norepinephrine (NE) in brain is 4-hydroxy-3-methoxyphenylethylene glycol (MHPG). In many species, a large fraction of MHPG formed in brain is converted to the sulfate conjugate. Consequently, MHPG sulfate has been proposed as a bioma
- Jacob III, Peyton,Wilson, Margaret,Yu, Lisa,Mendelson, John,Jones, Reese T.
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p. 5290 - 5296
(2007/10/03)
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- Preparation of synthetic lignins with superior NMR characteristics via isotopically labeled monolignols
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Synthetic lignins are particularly valuable for studying aspects of lignification, plant cell wall cross-linking, and lignin structure. If they are not too highly polymeric, they are soluble in normal lignin solvents and amenable to solution-state NMR studies. However, in the application of inverse-detected correlation experiments, particularly the popular HMQC and HMBC experiments, the spectra have annoying T1-noise ridges. These artifacts make it difficult to locate correlation peaks that are near the methoxy signal in the proton dimension. One solution is to use gradient-enhanced NMR but that requires additional hardware that is not yet ubiquitous. An alternative is to produce monolignols in which the atoms of the methoxy group are NMR-invisible. We have accomplished this by preparing coniferyl and sinapyl alcohols using 13C-depleted deuterated methyl iodide (12C2H3I). The methods, which incorporate steps simpler than have been used previously for labeled monolignols, are sufficiently low cost and straight-forward that these monomers can be utilized for any synthetic lignins destined for NMR studies. The NMR spectra of lignins derived from these 'methoxy-less' monomers are markedly superior to their normal-monomer counterparts. Several popular NMR experiments are illustrated for synthetic lignins derived from normal vs. isotopically labeled coniferyl alcohol, along with some useful experiments that have not been seen in lignin-related publications to date.
- Ralph, John,Zhang, Yingsheng,Ede, Richard M.
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p. 2609 - 2613
(2007/10/03)
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- Mechanistic Studies of Selective Catechol Formation from o-Methoxyphenols using a Copper(II)-Ascorbic Acid-Dioxygen System
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Mechanistic details of selective conversion of o-methoxyphenols to the corresponding catechols using a Cu2+-ascorbic acid-O2 system, were studied. 2,5-Dimethoxyphenol was converted predominantly to the o-demethylated compound and partially to the m-demethylated one.Anisole with no phenolic hydroxy group was much less reactive.When guaiacol (1). guaiacol and 2-methoxy-6-methoxyphenol was used as substrates, moderate intermolecular and intramolecular kinetic isotope effects were observed (1.4-1.9). Catechol was derived from 1 in nine-fold excess over catechol when the reaction was run in an 18O2 atmosphere with natural water as a solvent, though no catechol was formed when using natural O2 and H218O.It was determined that the Cu2+-ascorbic acid-O2 system operates in a monooxygenase mode because the oxygen atom of dioxygen (not water) was incorporated into the products, and this oxidative conversion proceeded mainly via ipso-substitution at the methoxy position, probably with hydroxyl radical coordinated to the cupric ion as the active oxygen species.
- Aihara, Kazuhiro,Urano, Yasuteru,Higuchi, Tsunehiko,Hirobe, Masaaki
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p. 2165 - 2170
(2007/10/02)
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- A RAMAN SPECTROSCOPIC STUDY OF THE LOW-FREQUENCY VIBRATIONS OF o-DIMETHOXYBENZENE AND ITS METHYL DEUTERATED ANALOGUES
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The low-frequency (100-400 cm-1) Raman spectra of liquid (at 300 K) and solid (at 130 K) veratrole (o-dimethoxybenzene), and its methyl deuterated analogues, have been measured.The methyl and methoxyl torsional transitions have been identified, and the corresponding rotational barriers have been determined.The interpretation of the spectra points to a conformationally mixed situation for solid veratrole, in which both planar and non-planar conformers may co-exist.
- Konschin, Henrik,Tylli, Henrik,Westermark, Bertel
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p. 279 - 288
(2007/10/02)
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