1200-12-0Relevant academic research and scientific papers
Synthesis of α-arylthioacetones using TEMPO as the: C 3 synthon via a reaction cascade of sequential oxidation, skeletal rearrangement and C-S bond formation
Zou, Jiao-Xia,Jiang, Yi,Lei, Shuai,Yin, Gao-Feng,Hu, Xiao-Ling,Zhao, Quan-Yi,Wang, Zhen
supporting information, p. 2341 - 2345 (2019/03/07)
Here, we present an unprecedented pathway to α-sulfenylated carbonyl compounds from commercially available thiols and universally employed TEMPO and its analogues, which act as C3 synthons through skeletal rearrangement under simple and metal-f
A sulfur-containing amino acid amide carbamate derivative and application thereof
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Paragraph 0033-0034; 0042-0043, (2017/08/09)
The invention belongs to the field of plant fungicides, and relates to sulfur-containing amino acid amide carbamate derivatives of which the general formulas I are shown in the description and pharmaceutically acceptable salts of the sulfur-containing amino acid amide carbamate derivatives. In the general formulas I, substituent groups R1, R2 and n are defined in the description. The invention further relates to preparation methods of compounds related to the general formulas I, special intermediates developed for the preparation of the compounds, and application of the compounds to prevention and control of plant diseases.
GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 00313-00314, (2016/07/05)
The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
α-Arylchalcogenation of acetone with diaryl dichalcogenide via metal-free oxidative C(sp3)-H bond functionalization
Yan, Guobing,Borah, Arun Jyoti,Wang, Lianggui,Pan, Zhangjin,Chen, Shuangshuang,Shen, Xuqian,Wu, Xiangmei
supporting information, p. 4305 - 4307 (2015/06/22)
Direct α-arylchalcogenation of acetone with diaryl dichalcogenides has been achieved by using a mixture of TBHP and DTBP oxidants at 120 °C without transition-metal catalyst via oxidative C(sp3)-H bond functionalization. The method exhibits good functional group tolerance and products were isolated in moderate to high yields.
17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
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Page/Page column 56, (2012/11/13)
The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C17,20-lyase inhibitors.
NEW COMPOUNDS
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Page/Page column 49, (2012/04/04)
A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
Preparation and pharmacological evaluation of a novel series of 2-(phenylthio)benzo[b]thiophenes as selective MT2 receptor ligands
Mésangeau, Christophe,Fraise, Mika?l,Delagrange, Philippe,Caignard, Daniel Henri,Boutin, Jean Albert,Berthelot, Pascal,Yous, Sa?d
scheme or table, p. 1835 - 1840 (2011/05/06)
A series of N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl) ethyl)acylamides was synthesized and evaluated for binding affinity and intrinsic activity at melatonin receptors. The affinity of each compound for the melatonin receptors was determined by binding studies on cloned human MT 1 and MT2 receptors expressed in CHO cells. Agonist and antagonist potency was measured on the [35S]GTPγS binding assay for the most interesting compounds. The new derivatives 8-14 showed modest to high selectivity (between 4 and 220) for MT2 receptors. The most selective compound, N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl) ethyl)but-3-enamide (14), an MT2 ligand with affinity for the MT 2 receptor similar to that of melatonin and a 220-fold preference over MT1 receptors, acts as a partial agonist. In addition, N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl)ethyl)propionamide (9), a nanomolar MT2 ligand with a good selectivity ratio (MT 1/MT2 = 51) shows antagonist activity on both melatonin receptors.
Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma
Davis, Robert L.,Kahraman, Mehmet,Prins, Thomas J.,Beaver, Yan,Cook, Travis G.,Cramp, Jessica,Cayanan, Charmagne S.,Gardiner, Elisabeth M.M.,McLaughlin, Marsha A.,Clark, Abbot F.,Hellberg, Mark R.,Shiau, Andrew K.,Noble, Stewart A.,Borchardt, Allen J.
scheme or table, p. 3361 - 3366 (2010/08/07)
We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intr
HYDANTOIN DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS
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Page/Page column 74, (2008/06/13)
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
