- Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis
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Sepsis, a systemic inflammatory response, caused by pathogenic factors including microorganisms, has high mortality and limited therapeutic approaches. Herein, a new soluble epoxide hydrolase (sEH) inhibitor series comprising a phenyl ring connected to a
- Bao, Xuefei,Chen, Guoliang,Du, Fangyu,Hammock, Bruce D.,Liu, Qiu,Liu, Zhongbo,Morisseau, Christophe,Sun, Wenjiao,Wang, Chao,Xiao, Wei,Yang, Hao,Zhang, Tan,Zhou, Jun
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- PGDH INHIBITORS AND METHODS OF MAKING AND USING
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Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.
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Paragraph 0271; 0278; 0281; 0376; 0378
(2021/07/31)
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- Indole-2-ketone derivative, preparation method and application thereof
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The invention belongs to the field of medicines, particularly relates to an indole-2-ketone derivative, a preparation method and application thereof, and provides a compound represented by the following formula (I), a stereoisomer, a racemate, a tautomer,
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Paragraph 0240; 0631; 0634-0635
(2020/07/06)
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- sEH inhibitor and preparation method and application thereof
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The invention provides an sEH inhibitor and a preparation method and application thereof, and relates to the technical field of endogenous active substance regulation and control. The sEH inhibitor provided by the invention has a structure as shown in a f
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Paragraph 0234; 0236
(2020/07/28)
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- Tuneable Copper Catalysed Transfer Hydrogenation of Nitrobenzenes to Aniline or Azo Derivatives
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A highly versatile and flexible copper nanoparticle (Cu(0) NPs) catalytic system has been developed for the controlled and selective transfer hydrogenation of nitroarene. Interestingly, the final catalytic product is strongly dependent on the nature of the hydrogen donor source. The yield of nitrobenzene reduction to aniline increased from 20% to an almost quantitative yield over a range of alcohols, diols and aminoalcohols. In glycerol at 130 °C aniline was isolated in 93% yield. In ethanolamine, the reaction was conveniently performed at a lower temperature (55 °C) and gave selectively substituted azobenzene (92% yield). Experimental studies provide support for a reaction pathway in which the Cu(0) NPs catalysed transfer hydrogenation of nitrobenzene to aniline proceeds via the condensation route. The high chemoselectivity of both protocols has been proved in experiments on a panel of variously substituted nitroarenes. Enabling technologies, microwaves and ultrasound, used both separately and in combination, have successfully increased the reaction rate and reaction yield. (Figure presented.).
- Moran, Maria Jesus,Martina, Katia,Baricco, Francesca,Tagliapietra, Silvia,Manzoli, Maela,Cravotto, Giancarlo
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supporting information
p. 2689 - 2700
(2020/05/18)
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- Enhanced catalytic activity of natural hematite-supported ppm levels of Pd in nitroarenes reduction
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In this work, Pd NPs supported on amine-modified natural hematite have been prepared and characterized. Using this simple catalyst, nitroaromatic compounds as a major cause of industrial pollution were reduced to corresponding amines with ppm levels of Pd in the presence of designer surfactant TPGS-750-M and NaBH4 at room temperature in aqueous media. Synergistic effect between hematite and Pd is responsible for the observed enhanced catalytic activity. This catalyst was recycled for at least four times with a small decrease in the activity.
- Gholinejad, Mohammad,Shojafar, Mohammad,Sansano, José M.
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p. 2033 - 2043
(2020/04/07)
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- Synergistic Effects of ppm Levels of Palladium on Natural Clinochlore for Reduction of Nitroarenes
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Augmenting the modified naturally occurring clay clinochlore with ppm amounts of palladium leads to a new and very effective reagent for the reduction of numerous aromatic nitro species. When palladium nanoparticles are supported on pyridyltriazole-modified clinochlore, iron within clinochlore acts synergistically with palladium to catalyze the reduction of a wide variety of nitroarenes at room temperature in aqueous media. Based on E-factor calculations, the catalyst system is found to be in line with green chemistry standards and can be recycled up to five times.
- Gholinejad, Mohammad,Oftadeh, Erfan,Shojafar, Mohammad,Sansano, José M.,Lipshutz, Bruce H.
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p. 4240 - 4248
(2019/09/06)
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- Starch functionalized creatine for stabilization of gold nanoparticles: Efficient heterogeneous catalyst for the reduction of nitroarenes
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Selective reduction of nitroaromatic pollutants into amines with recoverable and reusable heterogeneous catalysts is highly desirable. Herein, we prepared and characterized an efficient novel catalyst comprising 4 nm size Au nanoparticles supported on creatine modified starch. Using this catalyst, efficient reduction of nitroarenes into amines at room temperature in aqueous media was achieved. The presence of creatine in the structure of the catalyst plays important role in amount of Au loading, efficiency of the catalyst, recycling times, and leaching of Au compared to starch supported Au without creatine.
- Gholinejad, Mohammad,Dasvarz, Neda,Shojafar, Mohammad,Sansano, José M.
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- Environmentally benign selective hydrogenation of α,β-unsaturated aldehydes and reduction of aromatic nitro compounds using Cu based bimetallic nanoparticles supported on multiwalled carbon nanotubes and mesoporous carbon
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Bimetallic catalysts of Cu with Fe, Co, Ni, Zn or Ru supported on multiwalled carbon nanotubes (MWCNT) and mesoporous carbon (MC) were prepared by in situ reduction of CuCl2 and the metal chlorides using NaBH4. The catalytic activity of these materials was investigated in the hydrogenation of α,β-unsaturated aldehydes and reduction of aromatic nitro compounds using different hydrogen sources. Cu-Ni and Cu-Ru supported on MWCNT catalysts were found to be better than MC supported catalysts in terms of yield of the expected product and recyclability. Among the different hydrogen sources used, molecular H2 was found to be the best for the hydrogenation of α,β-unsaturated aldehydes to corresponding alcohols (conversion 83-86%, selectivity 72-78%), whereas NaBH4 was the best for the reduction of aromatic nitro compounds to corresponding amines (conversion 100%, selectivity 98%). The reaction conditions were optimised for good yield and selectivity of the product. Generality of the catalysts was also investigated in the reduction of different α,β-unsaturated aldehydes and aromatic nitro compounds. The relationship between catalytic activity and physico-chemical properties was investigated by characterising the catalytic materials using powder X-ray diffraction (powder XRD), X-ray photoelectron spectroscopy (XPS), Brunauer-Emmett-Teller (BET) surface area, scanning electron microscopy (SEM)-energy dispersive X-ray spectroscopy (EDS) and transmission electron microscopy (TEM).
- Hareesh,Minchitha,Venkatesh,Nagaraju,Kathyayini
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p. 82359 - 82369
(2016/09/09)
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- Metal–Organic Framework Based on Copper and Carboxylate-Imidazole as Robust and Effective Catalyst in the Oxidative Amidation of Carboxylic Acids and Formamides
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A metal–organic framework (MOF) based on copper and 1,3-bis(carboxymethyl)imidazole (bcmim) was prepared on a gram scale by using a precipitation method at room temperature. The Cu(bcmim)2MOF was shown to be an efficient catalyst for the preparation of amides through an oxidative coupling between carboxylic acids and formamides in the presence of an oxidant, such as tert-butyl hydroperoxide (TBHP). The method for the preparation of the amides is robust regardless of the carboxylic acid and gives good conversions with good selectivity. The heterogeneous catalyst was recovered unaltered after the reaction, was easily separated from the reaction mixture, and subsequently reactivated by suitable treatment. Moreover, the coupling reaction was scaled up to a gram scale, which allowed for the preparation of valuable products, such as fatty acid amides (i.e., 1-palmitoylpiperidine).
- Albert-Soriano, María,Pastor, Isidro M.
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supporting information
p. 5180 - 5188
(2016/10/26)
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- Assembly of Primary (Hetero)Arylamines via CuI/Oxalic Diamide-Catalyzed Coupling of Aryl Chlorides and Ammonia
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A general and practical catalytic system for aryl amination of aryl chlorides with aqueous or gaseous ammonia has been developed, with CuI as the catalyst and bisaryl oxalic diamides as the ligands. The reaction proceeds at 105-120°C to provide a diverse set of primary (hetero)aryl amines in high yields with various functional groups.
- Fan, Mengyang,Zhou, Wei,Jiang, Yongwen,Ma, Dawei
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supporting information
p. 5934 - 5937
(2015/12/11)
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- Visible-light-promoted radical C-H trifluoromethylation of free anilines
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The trifluoromethyl-substituted anilines are biologically active compounds and useful building blocks. In this communication, we have developed the first visible-light-induced radical trifluoromethylation of free anilines with the commercially available and easily handled Togni reagent at room temperature. The resulting products were successfully transformed into a variety of valuable fluorine-containing molecules and heterocyclic compounds. This protocol provides an economical and powerful route to trifluoromethylated free anilines.
- Xie, Jin,Yuan, Xiangai,Abdukader, Ablimit,Zhu, Chengjian,Ma, Jing
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supporting information
p. 1768 - 1771
(2014/04/17)
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- Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts
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A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.
- Cheung, Chi Wai,Surry, David S.,Buchwald, Stephen L.
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supporting information
p. 3734 - 3737
(2013/08/23)
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- Compounds and compositions as inhibitors of receptor tyrosine kinase activity
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The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with cSRC, Lck, FGFR3, Flt3, TrkB, Bmx, and/or PFGFRα kinase
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Page/Page column 9
(2010/02/11)
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- Perhydroquinolylbenzamides as novel inhibitors of 11β-hydroxysteroid dehydrogenase type 1
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High-throughput screening identified 5 as a weak inhibitor of 11β-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some with low nanomolar inhibitory potency. A tertiary benzamide is required for biological activity and substitution of the terminal benzamide with either electron-donating or -withdrawing groups is tolerated. The majority of the compounds show selectivity of >20 to > 700-fold over 11β-HSD2. Analogues which showed >50% inhibition of 11β-HSD1 at 1 μM in an cellular assay were screened in an ADX mouse model. A maximal response of >70% reduction of liver corticosterone levels was observed for three compounds; 9m, 25 and 49.
- Coppola, Gary M.,Kukkola, Paivi J.,Stanton, James L.,Neubert, Alan D.,Marcopulos, Nicholas,Bilci, Natalie A.,Wang, Hua,Tomaselli, Hollis C.,Tan, Jenny,Aicher, Thomas D.,Knorr, Douglas C.,Jeng, Arco Y.,Dardik, Beatriz,Chatelain, Ricardo E.
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p. 6696 - 6712
(2007/10/03)
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- Method of suppressing body odor with aminobenzoic acid amides
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This invention is directed to a cosmetic deodorant composition comprising: (a) from about 0.1 to 5 percent by weight, based on the weight of the total composition, of aminobenzoic acid amides of the formula STR1 wherein R1 and R2, which may be the same or different, each represent hydrogen, an alkyl of from 1 to 12 carbon atoms; a hydroxyalkyl of from 2 to 4 carbon atoms; an aryl; an aralkyl or carboxyalkyl with from 1 to 3 carbon atoms in the alkyl moiety; or an alkoxyalkyl with from 1 to 8 carbon atoms in the alkoxy moiety and from 1 to 3 carbon atoms in the alkyl moiety, or R1 and R2 together with the amide nitrogen form an optionally substituted heterocyclic ring; and (b) the remainder conventional cosmetic deodorant composition compounds.
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