- PERIPHERAL ALKYL AND ALKENYL CHAINS EXTENDED BENZENE DERIVATIVES AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME
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The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX) / histone deacetylase (HD AC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.
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Paragraph 0063; 0460-0463
(2020/10/20)
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- Br?nsted acid/visible-light-promoted Markovnikov hydroamination of vinylarenes with arylamines
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A Br?nsted acid/visible-light-promoted Markovnikov hydroamination of vinylarenes with arylamines in the presence of TPT and CF3CO2H has been developed. This transformation provides a green approach to alpha-amino-substituted arylalkanes under metal-free conditions.
- Gui, Jiao,Xie, Haisheng,Chen, Fengjuan,Liu, Zhipeng,Zhang, Xiaoqi,Jiang, Fubin,Zeng, Wei
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supporting information
p. 956 - 963
(2020/02/15)
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- Silylative Kinetic Resolution of Racemic 1-Indanol Derivatives Catalyzed by Chiral Guanidine
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Efficient kinetic resolution of racemic 1-indanol derivatives was achieved using triphenylchlorosilane by asymmetric silylation in the presence of chiral guanidine catalysts. The chiral guanidine catalyst (R,R)-N-(1-(β-naphthyl)ethyl)benzoguanidine was found to be highly efficient as only 0.5 mol % catalyst loading was sufficient to catalyze the reaction of various substrates with appropriate conversion and high s-values (up to 89). This catalyst system was successfully applied to the gram-scale silylative kinetic resolution of racemic 1-indanol with high selectivity.
- Yoshimatsu, Shuhei,Yamada, Akira,Nakata, Kenya
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p. 452 - 458
(2018/02/19)
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- BICYCLICALLY SUBSTITUTED URACILS AND THE USE THEREOF
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The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
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Paragraph 0903; 0922; 0923; 0924; 0925
(2015/06/03)
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- SUBSTITUTED HETEROCYCLIC DERIVATIVES AS GPR AGONISTS AND USES THEREOF
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The present invention generally relates to substituted heterocyclic derivatives (the compounds of Formula (I)), processes for their preparation, pharmaceutical compositions containing said compounds, their use as G-protein coupled receptor (GPR) agonists, particularly as GPR40 agonists and methods of using these compounds in the treatment of GPR40 mediated diseases or conditions such as Type 2 diabetes, obesity, dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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- AMINOINDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY
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The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.
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- Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/- indanes and structurally modified derivatives: Potent and selective inhibitors of aldosterone synthase
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Elevated aldosterone levels are key effectors for the development and progression of congestive heart failure and myocardial fibrosis. Recently, we proposed inhibition of aldosterone synthase (CYP11B2) as an innovative strategy for the treatment of these
- Ulmschneider, Sarah,Müller-Vieira, Ursula,Klein, Christian D.,Antes, Iris,Lengauer, Thomas,Hartmann, Rolf W.
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p. 1563 - 1575
(2007/10/03)
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- Transition-state effects in acid-catalyzed aryl epoxide hydrolyses
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The hydronium ion-catalyzed hydrolyses of 5-methoxyindene 1,2-oxide and of 6-methoxy-1,2,3,4-tetrohydronaphthalene-1,2-epoxide were each found to yield 75-80% of cis diol and only 20-25% of trans diol as hydrolysis products. The relative stabilities of the cis and trans diols in each system were determined by treating either cis or trans diols with perchloric acid in water solutions and following the approach to an equilibrium cis/trans mixture as a function of time. These studies establish that the trans diol in each system is more stable than the corresponding cis diol. Thus, acid-catalyzed hydrolysis of each epoxide, which proceeds via a carbocation intermediate, yields the less stable cis diol as the major product. Transition-state effects, presumably of a hydrogen-bonding nature, selectively stabilize the transition state for attack of water on the intermediate 2-hydroxy-1-indanyl carbocation leading to the less stable cis diol in this system. Transition-state effects must also be responsible for formation of the less stable cis diol as the major product in the acid-catalyzed hydrolysis of 5-methoxy-1,2,3,4-tetrahydronaphthalene 1,2-epoxide. However, in this system steric effects at the transition state may be more important than hydrogen bonding in determining the cis/trans diol product ratio. The synthesis of 5-methoxyindene 1,2-oxide and a study of its rate of reaction as a function of pH in water and dioxane-water solutions are reported. Both an acid-catalyzed reaction leading to only diol products and a pH-independent reaction yielding 71% of 5-methoxy-2-indanone and 29% of diols are observed; the half-life of its pH-independent reaction in water is only 2.4 s.
- Sampson, Kyere,Paik, Augustine,Duvall, Bridget,Whalen, Dale L.
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p. 5204 - 5211
(2007/10/03)
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- Substituent Effect Behavior in the Antiaromatic Inden-1-yl Cation System
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Studies of the rate-accelerating effects in solvolysis produced by 5-methyl and 5-methoxy substituents on the benzene ring and a 3-methyl substituent on the double bond of the inden-1-yl 3,5-dinitrobenzolate system have been carried out.In both 80percent aqueous acetone and in 2,2,2-trifluoroethanol, the rate accelerations observed in the inden-1-yl system were approximately the same as those found in model cyclopenten-3-yl and indan-1-yl systems.From these results, it is concluded that delocalization of charge into both the benzene ring and double bond of the 8?-electron inden-1-yl carbocation is taking place and is apparently undiminished by antiaromatic effects.
- Friedrich, Edwin C.,Tam, Teresa M.
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p. 315 - 319
(2007/10/02)
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