61440-60-6Relevant academic research and scientific papers
DEUTERATED PITOLISANT
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Paragraph 131-132, (2020/05/28)
This invention also provides compound of Formula (I) including pharmaceutical compositions comprising a compound of Formula (I) and a pharmaceutically acceptable carrier. This invention also provides the use of such compounds and compositions in methods o
Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors
Terasaka, Tadashi,Kinoshita, Takayoshi,Kuno, Masako,Seki, Nobuo,Tanaka, Kohichiro,Nakanishi, Isao
, p. 3730 - 3743 (2007/10/03)
We disclose herein optimization efforts around the novel, highly potent non-nucleoside adenosine deaminase (ADA) inhibitor, 1-[(R)-1-hydroxy-4-(6-(3-(1- methylbenzimidazol-2-yl)propionylamino)indol-1-yl)-2-butyl]imidazole-4- carboxamide 1 (Ki =
A new series of estrogen receptor modulators that display selectivity for estrogen receptor β
Henke, Brad R.,Consler, Thomas G.,Go, Ning,Hale, Ron L.,Hohman, Dana R.,Jones, Stacey A.,Lu, Amy T.,Moore, Linda B.,Moore, John T.,Orband-Miller, Lisa A.,Robinett, R. Graham,Shearin, Jean,Spearing, Paul K.,Stewart, Eugene L.,Turnbull, Philip S.,Weaver, Susan L.,Williams, Shawn P.,Wisely, G. Bruce,Lambert, Millard H.
, p. 5492 - 5505 (2007/10/03)
A series of 1,3,5-triazine-based estrogen receptor (ER) modulators that are modestly selective for the ERβ subtype are reported. Compound 1, which displayed modest potency and selectivity for ERβ vs ERα, was identified via high-throughput screening utiliz
Reactions of γ-arylalkanols via aryl radical cation and alkoxyl radical intermediates. Part 3. Reactions of 3-arylprop-1-yl hydroperoxides with iron(II) in the presence of copper(II)
Goosen, Andre,Marais, Charles F.,McCleland, Cedric W.,Rinaldi, Fabrizio C.
, p. 1227 - 1236 (2007/10/02)
A strategy for comparing the 1,5- and 1,6-cyclisation reactions of 3-phenylpropan-1-oxyl radicals is described.Iron(II)-catalysed reduction of 3-(p-methylphenyl)prop-1-yl hydroperoxide and its para-chloro and para-methoxy-substituted analogues, carried out in the presence of copper(II), has been found to give in each case the appropriate para-substituted 3-phenylpropan-1-ol, 3-phenylpropanal and a low yield of a mixture of isomeric 6- and 7-substituted chromans.The alcohols are proposed to form via reduction of either the hydroperoxide or the resulting alkoxyl radical or its cyclised intermediates, and the aldehydes as a result of rearrangement of the alkoxyl radical to an α-hydroxy alkyl radical which subsequently undergoes oxidation.The 7-substituted chromans, which arise directly from 1,6-cyclisation of the alkoxyl radical, were found to dominate the 6-substituted isomers which result from rearrangement of 1,5-cyclised intermediates.This effect is attributed to inefficient interception of the 1,5-cyclised radical intermediate which permits equilibration to the thermodynamically more stable 1,6-cyclised radical isomer to occur.The effect of pH on the reactions has been investigated and although no products typical of the intermediacy of aryl radical cations were detected (even under highly acidic conditions), the formation of such intermediates cannot be excluded.Semiempirical MO calculations have been carried out (at the PM3 level of approximation) on a series of model compounds, yielding results which have clarified our understanding of the effect of substituents on the stabilities of the various intermediates arising from the cyclisation reactions of 3-phenylpropan-1-oxyl radicals.Furthermore, these calculations have supported our assumptions regarding the probability and specificity of rearrangements of the spirodienyl intermediates.
Arylalkylaminobenzoic acids
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, (2008/06/13)
This disclosure describes novel [Bis(phenyl or substituted phenyl)alkyl]amino benzoic acids, esters, and derivatives thereof. These compounds are useful pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial walls of mammals.
Antilipidemic para-[aryl(alkyl or alkenyl)amino]-benzoic acid derivatives
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, (2008/06/13)
Novel para-[aryl(alkyl or alkenyl)amino]benzoic acids, esters, pharmaceutically acceptable salts and pharmaceutical compositions thereof and a method of lowering serum lipid levels in mammals therewith.
