cas 5434-20-8, 3-AMINOPHTHALIC ACID | Articles data

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A dicopper complex chemiluminescence probe for the determination of thiols in the extracts of murine P388 lymphocytic leukemia cell
A chemiluminescence (CL) probe of peroxidase-like dicopper complex (Cu 2L2) for the determination of glutathione (GSH) and related cellular thiols was developed for the first time.
Zhang, Xiaoru,Zhou, Huanran,Ding, Caifeng,Zhang, Shusheng
p. 5624 - 5626
(2009)
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Chemiluminescence determination of trimetazidine via inducing the aggregation of gold nanoparticles
A simple, rapid and sensitive chemiluminescence (CL) method combined with flow injection analysis was developed for the determination of trimetazidine. Trimetazidine was found to significantly increase the CL signal arising from N-bromosuccinimide-luminol reaction in the presence of gold nanoparticles. The enhanced CL intensity was proportional to trimetazidine concentration in the range of 0.01-5.0 μg/mL, with a limit of detection (3sb) of 6.7 ng/mL. The relative standard deviation was 2.8% for 11 repetitive measurements of 0.1 μg/mL trimetazidine solution. The practicality of the method was evaluated by determining trimetazidine in pharmaceutical formulations and in spiked human serum samples. Moreover, the possible CL reaction mechanism was also discussed.
Li, Jiao,Quan, Jie,Du, Jianxiu,Liu, Mei
p. 33 - 37
(2013)
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Mesoporous material-based manipulation of the enzyme-like activity of CoFe2O4 nanoparticles
Mesoporous material supported CoFe2O4 magnetic nanoparticles possess unique peroxidase/oxidase-like activity, and react with luminol to yield a novel chemiluminescence without the need of H 2O2. Their oxidase-like activity shows pH and support dependence, and could be reversibly controlled by their pH. This offers a new method for manipulating the enzyme-like activity of nanoparticles.
Fan, Yingwei,Shi, Wenbing,Zhang, Xiaodan,Huang, Yuming
p. 2482 - 2486
(2014)
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Enzyme-Loaded Hemin/G-Quadruplex-Modified ZIF-90 Metal–Organic Framework Nanoparticles: Bioreactor Nanozymes for the Cascaded Oxidation of N-hydroxy-l-arginine and Sensing Applications
Biocatalytic cascades are challenging to operate in homogeneous solution, where diffusional mass transport hinders efficient communication between the reactive components. There is great interest in developing devices to perform such transformations in co
Chen, Chaochao,O'Hagan, Michael P.,Ouyang, Yu,Vázquez-González, Margarita,Wang, Zhanhui,Willner, Itamar
(2022/01/19)

ISOINDOLE DERIVATIVE
Disclosed is a compound of formula (I) and a stereoisomer thereof: wherein R1, R2, R3 and R4 are as defined in the present disclosure.
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Paragraph 0226

(2021/02/25)

Visible-Light-Mediated Dearomatisation of Indoles and Pyrroles to Pharmaceuticals and Pesticides
Dearomatisation of indole derivatives to the corresponding isatin derivatives has been achieved with the aid of visible light and oxygen. It should be noted that isatin derivatives are highly important for the synthesis of pharmaceuticals and bioactive compounds. Notably, this chemistry works excellently with N-protected and protection-free indoles. Additionally, this methodology can also be applied to dearomatise pyrrole derivatives to generate cyclic imides in a single step. Later this methodology was applied for the synthesis of four pharmaceuticals and a pesticide called dianthalexin B. Detailed mechanistic studies revealed the actual role of oxygen and photocatalyst.
Schilling, Waldemar,Zhang, Yu,Riemer, Daniel,Das, Shoubhik
supporting information
p. 390 - 395
(2019/12/15)

Synthesis method of methyl 2-acetyl-6-aminobenzoate
The invention provides a synthesis method of methyl 2-acetyl-6-aminobenzoate. The target product methyl 2-acetyl-6-aminobenzoate is prepared from cheap and easily available 3-nitrophthalic acid through a six-step reaction. The synthesis method has the characteristics of easily available raw materials, short route, high yield, easiness in operation, small environmental pollution and the like, and is suitable for large-scale industrial production.
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Paragraph 0055; 0057; 0058; 0069; 0071; 0072

(2020/05/01)

Palladium Supported on Carbon Nanoglobules as a Promising Catalyst for Selective Hydrogenation of Nitroarenes
The catalysts 1?wt% palladium supported on carbon nanoglobules (CNGs) were shown to be highly active in the liquid-phase hydrogenation of various nitroarenes and provided nearly 100% selectivity to aromatic amines at complete conversion under mild conditions (323?K, 0.5?MPa, 1?h). The catalytic activity (in terms of turnover frequency and substrate conversion) and selectivity depend on the kind of CNGs support, catalyst preparation method and the reaction conditions (solvent nature). The Pd/CNGs catalyst can be repeatedly used while maintaining the same catalytic performance. The excellent performances of Pd/CNGs catalysts can be due to the globular morphology of the supports as well as the absence of micropores and pronounced surface defects. Graphic Abstract: [Figure not available: see fulltext.]
Mironenko,Belskaya,Stepanova,Gulyaeva,Trenikhin,Likholobov
p. 888 - 900
(2019/11/11)

METHODS FOR THE TREATMENT OF OBESITY USING APREMILAST
Methods of treating, managing or preventing obesity and overweight are disclosed. Specific methods encompass the administration of apremilast, alone or in combination with additional active agents or treatment regimens.
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Paragraph 0079

(2019/05/22)

APREMILAST FOR THE TREATMENT OF A LIVER DISEASE OR A LIVER FUNCTION ABNORMALITY
Methods of treating, managing or preventing liver disease are disclosed. Specific methods encompass the administration of apremilast, alone or in combination with additional active agents or treatment regimens.
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Paragraph 0098

(2019/09/15)

NOVEL PROCESS TO PREPARE N-[2-[(1S)-1-(3-ETHOXY-4-METHOXYPHENYL)-2-(METHYLSULPHONYL) ETHYL]-1, 3-DIOXO-2,3-DIHYDRO-1H-ISOINDOL-4-YL]ACETAMIDE
An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.
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Page/Page column 11; 12

(2018/12/03)

NOVEL PROCESS FOR PREPARATION OF APREMILAST
The present invention related to a novel compound of Formula II, its enantiomers or acid addition salts thereof and process for its preparation. The compound of Formula II can be used for preparation of N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2- (methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide also known as apremilast.
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Page/Page column 16

(2018/02/03)

Visible-light photocatalytic activity of chitosan/polyaniline/CdS nanocomposite: Kinetic studies and artificial neural network modeling
Chitosan/polyaniline (CS/PAni), chitosan/CdS (CS/CdS) and chitosan/polyaniline/CdS nanocomposite were synthesized and characterized using X-ray diffraction pattern analysis, FT-IR spectroscopy and scanning electronic microscopy. The adsorption performance and photocatalytic activity of CS/PAni/CdS was compared with CS/PAni and CS/CdS in the removal of Reactive Blue 19 (RB19) dye. After five cycles of experiments under visible light irradiation, CS/PAni/CdS retained high photocatalytic activity which confirmed good stability of nanocomposite. Moreover, the kinetics of decolorization was investigated and novel equation rate for dye removal was established by considering two parallel mechanisms including adsorption and surface photocatalytic degradation of dye by CS/PAni/CdS. Artificial neural network was employed to develop a model for predicting the decolorization efficiency and determining the relative importance of operational parameters. A 3-layer perceptron network with optimized 5:10:1 topology could provide adequate predictive performance (R2 = 0.983). Moreover, the photocatalytic degradation of RB19 was monitored by measuring the total organic carbon (TOC) and GC-MS analysis, enabling the evaluating the mineralization and identifying the intermediates. During 120 min of experiment, more than 80% of TOC was removed.
Rasoulifard,Seyed Dorraji,Amani-Ghadim,Keshavarz-Babaeinezhad
p. 60 - 70
(2016/02/03)

Preparation method for 3-aminophthalic acid and derivative thereof
The invention discloses a preparation method for an apremilast intermediate, i.e., 3-aminophthalic acid, and a derivative thereof. The preparation method comprises a step of reducing 3-nitrophthalic acid or a derivative thereof in the presence of a reducing agent selected from a group consisting of elemental sulfur, sulfide and a mixture of elemental sulfur and sulfide. The method has the advantages of high yield, simple operation, environmental protection and suitability for industrial production.
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Paragraph 0019

(2017/04/11)

DOSAGE TITRATION OF APREMILAST FOR THE TREATMENT OF DISEASES AMELIORATED BY PDE4 INHIBITION
Administration of apremilast in a specific dosage titration schedule, alone or in combination with a second active agent for use in methods of treating, managing or preventing diseases ameliorated by inhibiting PDE4 such as psoriasis, ankylosing spondylitis, Behcet's disease, rheumatoid arthritis, atopic dermatitis, Crohn's disease, and ulcerative colitis.
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Paragraph 0094

(2016/02/29)

Methods and compositions using PDE4 inhibitors for the treatment and management of autoimmune and inflammatory diseases
Methods of treating, preventing, or managing autoimmune inflammatory diseases and disorders including but not limited to spondylitis, juvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, osteoarthritis, ankylosing spondylitis, and rheumatoid arthritis by the administration of phosphodiesterase 4 (PDE4) inhibitors in combination with other therapeutics are disclosed. Pharmaceutical compositions, dosage forms, and kits suitable for use in methods of the invention are also disclosed.
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Page/Page column 22-23

(2016/05/02)

CONTROLLED RELEASE ORAL DOSAGE FORMS OF POORLY SOLUBLE DRUGS AND USES THEREOF
Provided herein are controlled release oral dosage forms of poorly soluble drugs, methods of making the dosage forms, and methods of their use for the treatment of various diseases and/or disorders.
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Paragraph 0214

(2016/06/06)

Methods for treating diseases using isoindoline compounds
Methods of treating a disease selected from dermatomyositis, prurigo nodularis, pyoderma gangrenosum, alopecia areata, hidradenitis suppurtiva, rosacea, lichen planus, giant cell arteritis, Sjogren's syndrome, gout, chronic prostatitis, posterior uveitis, vulvodynia and interstitial cystitis in a human are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, cyclopropyl {2-[(15)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindolin-4-yl}carboxamide or a combination thereof, or a pharmaceutically acceptable prodrug, metabolite, polymorph, salt, solvate or clathrate thereof.
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Paragraph 27

(2016/08/17)

Preparation method of 3-acetyl aminophthalimide
The invention relates to a preparation method of 3-acetyl aminophthalimide, comprising the following steps: dissolving 3-nitro phthalic acid in sodium hydroxide aqueous solution, then adding a reducer and a catalyst, heating to 70 to 80 DEG C, stirring and reacting for 1 to 20 hours, and recrystallizing to obtain 3-amino phthalic acid; stirring with acetic anhydride and performing reflux reaction for 1 to 10 hours to obtain N-(1,3-Dioxo-1,3-dihydro-2-benzofuran-4-yl)acetamide; dissolving the N-(1,3-Dioxo-1,3-dihydro-2-benzofuran-4-yl)acetamide in an organic solvent, adding an amino donor, and stirring and refluxing for 1 to 10 hours, thus obtaining the 3-acetyl aminophthalimide. The method is simple in operation, high in yield, short in reaction route, less in the three wastes (waste gas industrial residue), and easy for industrial production.
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Paragraph 0033; 0034

(2016/10/07)

PROCESS FOR THE ENANTIOMERIC RESOLUTION OF APREMILAST INTERMEDIATES
A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.
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Page/Page column 11

(2016/11/17)

Industrial method for preparing apremilast and intermediate thereof
The invention discloses an industrial method for preparing high-purity apremilast (described in formula I) and an intermediate thereof. With 3-nitrophthalic acid (compound II) adopted as the starting raw material, and organic acid or acid anhydride adopted as the solvent, the method comprises the following steps: preparing high-purity 3-acetamido phthalic anhydride (compound IV) through different intermediates; directly enabling the obtained undried product to react with (S)-1-(3-oxethyl-4-methoxy phenyl)-2-mesyl) ethylamine (compound V) or the salt during reflux in glacial acetic acid, so as to obtain the apremilast. The preparation method is easy to operate, low in energy consumption, high in yield, and applicable to industrial production.
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Paragraph 0026; 0027

(2017/03/14)

Preparation of 2-phenyl-3-hydroxyquinoline-4(1H)-one-5-carboxamides as potential anticancer and fluorescence agents
The synthesis of 3-hydroxyquinoline-4(1H)-one derivatives bearing substituted phenyl in position 2 and variously substituted carboxamide group in position 5 is described, with use of 3-nitrophthalic anhydride, α-haloketones and primary amines as the starting materials. The synthetic approach was inspired by the preparation of analogous derivatives reported previously. However, a different strategy had to be developed with the corresponding bis(phenacyl)-3-aminophthalates as the key intermediates. Synthesized hydroxyquinolinones, as well as their intermediates, were tested for their cytotoxic activity towards various cancer and non-malignant cell lines. The fluorescent properties of these compounds have also been evaluated. In both fields, interesting data were obtained and compared to isomeric compounds that have been studied in the past.
Funk, Petr,Motyka, Kamil,D?ubák, Petr,Znojek, Pawel,Gurská, Soňa,Kusz, Joachim,McMaster, Claire,Hajdúch, Marián,Soural, Miroslav
p. 48861 - 48867
(2015/06/16)

Chemiluminescence properties of luminol related quinoxaline analogs: Experimental and DFT based approach to photophysical properties
Novel luminol and isoluminol related compounds containing a quinoxaline moiety were synthesized by the reaction of various 1,2-diketones with dimethyl-4,5-diaminophthalate (5) and dimethyl-3,4-diaminophthalate (5′). The UV-Vis absorption and emission spectra of the dyes were studied in solvents of differing polarity and the compounds show solvatofluorism properties. The chemiluminescent properties of the isoluminol and luminol based quinoxaline derivatives were examined and compared with isoluminol and luminol. These compounds produced chemiluminescence by reaction with hydrogen peroxide in the presence of potassium hexacyanoferrate(III) in sodium hydroxide solution. The chemiluminescence intensities of these chemiluminophores were affected by the concentrations of hydrogen peroxide, potassium hexacyanoferrate(III) and sodium hydroxide. These quinoxaline derivatives were found to produce chemiluminescence in the range of 3.2-7.3 and it is 0.57-1.7 times more intensely than isoluminol and luminol, respectively. Density Functional Theory computations have been used for in-depth understanding of structural, molecular, electronic and photophysical parameters of the compounds.
Deshmukh, Mininath S.,Sekar, Nagaiyan
p. 49 - 60
(2015/03/04)

USE OF PDE4 INHIBITORS AND COMBINATIONS THEREOF FOR THE TREATMENT OF CYSTIC FIBROSIS
Methods of treating cystic fibrosis by administering a PDE4 inhibitor in combination with one or more cystic fibrosis transmembrane conductance regulator (CFTR) potentiators, including ivacaftor, and/or one or more CFTR correctors, including lumacaftor. Pharmaceutical compositions, dosage forms, and kits suitable for use in methods of the invention are also disclosed.
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Paragraph 0111

(2016/02/16)

COMPOSITIONS AND METHODS FOR THE TREATMENT OF ATHEROSCLEROTIC CARDIOVASCULAR DISEASES WITH PDE4 MODULATORS
Provided herein are methods of treating, preventing or managing atherosclerosis by administering a PDE4 modulator. Pharmaceutical compositions, dosage forms, and kits suitable for use in methods are also provided.
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Paragraph 0186

(2016/04/26)

Determination of cysteine and glutathione based on the inhibition of the dinuclear Cu(II)-catalyzed luminol-H2O2 chemiluminescence reaction
The catalyzed luminol chemiluminescent reaction has received a great amount of attention because of its high sensitivity and low background signal which make the reaction an attractive analytical chemistry tool. The present study, introduces the beneficial catalytic effects of dinuclear Cu(II) complex [Cu 2L2(TAE)]X2, where TAE = tetraacetylethane; L = N,N'-dibenzylethylenediamine and X = ClO4 on the luminol chemiluminescent reaction as a novel probe for the determination of glutathione (GSH) and L-cysteine (CySH) in human serum and urine. The [Cu2L 2(TAE)]X2 has exhibited highly efficient catalytic activity of luminol CL as an artificial peroxidase model at pH as low as 7.5 in water in the presence of H2O2×GSH and CySH can induce a sharp decrease in CL intensity from the [Cu2L 2(TAE)]X2-catalyzed luminol system. Under the selected experimental conditions, a linear relationship was obtained between the CL intensity and the concentrations of GSH and CySH in the range of 1.0 × 10-7-1.0 × 10-4 M, with detection limits (S/N = 3) of 2.7 × 10-8 and 6.8 × 10-8 M and RSD 4.2% (n = 7) for GSH and CySH, respectively.
Chaichi, Mohammad Javad,Ehsani, Mahjoobeh,Khajvand, Tahereh,Golchoubian, Hamid,Rezaee, Ehsan
p. 405 - 410
(2014/01/06)

METHODS FOR THE TREATMENT OF BONE LOSS
Provided herein are methods of treating, preventing and/or managing bone loss using (+)-2- [ 1 -(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-4-acetylaminoisoindolin- 1,3-dione, alone or in combination with other therapeutics.
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Page/Page column 20

(2014/05/24)

TREATMENT OF PSORIATIC ARTHRITIS USING APREMILAST
Methods of treating, managing or preventing psoriatic arthritis are disclosed. Specific methods encompass the administration of apremilast, alone or in combination with a second active agent.
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Paragraph 0072

(2014/10/04)

Synthesis, insecticidal activities and SAR of novel phthalamides targeting calcium channel
In order to find novel and environmental friendly insecticides targeting the ryanodine receptor, three series of novel phthalamides containing heptafluoroisopropyl group, low fluorine atoms group and non-fluorine group were designed and synthesized. 35 novel structures of three series were obtained. Insecticidal activities of title compounds against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of title compounds showed moderate to high activities at the tested concentration. The structure-activity relationship (SAR) was discussed in detail. During synthesizing title compounds B8, C7, D1, D9 and D12, their corresponding positional isomers (B8′, C7′, D1′, D9′ and D12′) were afforded, and their structures were confirmed by 2D NMR. The calcium-imaging technique was also applied to investigate the effects of compounds B2, B10, C4 and C5 on the intracellular calcium ion concentration ([Ca2+]i), which indicated that they released stored calcium ions from endoplasmic reticulum, which denoted that some compounds are potential modulators of the insect ryanodine receptor (RyR).
Chen, Youwei,Li, Yuxin,Pan, Li,Liu, Jingbo,Wan, Yingying,Chen, Wei,Xiong, Lixia,Yang, Na,Song, Haibin,Li, Zhengming
p. 6366 - 6379
(2015/01/09)

Design, synthesis and in-vitro cytotoxicity of novel platinum (II) complexes with phthalate as the leaving group
Three platinum (II) complexes (6-8) with phthalate as the leaving group were synthesized and characterized by FTIR, 1H NMR, 13C NMR, mass spectrometry and elemental analysis. In-vitro cytotoxicity of all three complexes was evaluated using COLO 205 (human colon cancer cell line) against the parent drug "oxaliplatin". The compound 4-amino-(transcyclohexane-1,2-diamine) platinum(II) (8) showed potent cytotoxicity with IC50 = 0.12 μM as compared to oxaliplatin (IC50 = 0.19 μM) and its aqueous solubility was found to be 16 mg/mL which is higher than oxaliplatin (8 mg/mL). The acute toxicity showed that the platinum complex (8) was less toxic than oxaliplatin. Molecular oxaliplatin-DNA complex structure indicates that the diaminocyclohexane (DACH) and Pt (II) showed interactions with N7 and O6 of GG base pairs of DNA helix. In this present study, it is interesting to note that all three platinum based anticancer agents with phthalate as the leaving group exhibited great cytotoxicity, less toxicity, good lipophilicity as well as better aqueous solubility. 2013 Bentham Science Publishers.
Sharma, Rajiv,Rawal, Ravindra K.,Malhotra, Manav,Gaba, Tripti,Sharma,Bhardwaj
p. 872 - 878
(2013/12/04)

METHODS AND COMPOSITIONS USING PDE4 INHIBITORS FOR THE TREATMENT AND MANAGEMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES
Methods of treating, preventing, or managing autoimmune inflammatory diseases and disorders including but not limited to spondylitis, juvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, osteoarthritis, ankylosing spondylitis, and rheumatoid arthritis by the administration of phosphodiesterase 4 (PDE4) inhibitors in combination with other therapeutics are disclosed. Pharmaceutical compositions, dosage forms, and kits suitable for use in methods of the invention are also disclosed.
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(2012/11/08)

Methods for treating cutaneous lupus using aminoisoindoline compounds
Methods of treating cutaneous lupus in a human are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, 4-(amino)-2-(2,6-dioxo(3-piperidyl))-isoindoline-1,3-dione (ACTIMID?), 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (REVLIMID?), or cyclopropyl 2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindolin-4-yl}carboxamide, alone or alternatively, in combination with a second active agent.
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Page/Page column 14

(2010/11/27)

Hydrogenation of ortho-substituted nitrobenzenes over palladium catalysts
Hydrogenation of o-nitrobenzenes, under mild conditions (1 atm of hydrogen, 20-40°C, organic solvents) over a Pd/C catalyst and the palladium-containing anion exchangers AN-1 and AV-17-8 proceeds without the formation of intermediate products. The yield of primary amines varies from 25 to 100%. It was shown that the palladium-containing anion exchangers are superior to Pd/C in selectivity and stability in the hydrogenation of o-nitrobenzenes. Based on quantum-chemical calculations of substrate molecules, a two-parameter correlation was proposed to describe the electronic and steric effects of the substituent on the hydrogenation rate.
Klyuev,Volkova,Abdullaev
p. 30 - 33
(2007/10/03)

Hydrogenation of ortho-Substituted Nitrobenzenes over AV-17-8 Palladium-Containing Anion Exchanger
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Abdullaev,Nasibulin,Klyuev
p. 1676 - 1677
(2007/10/03)

Disazo dyestuffs
Disazo dyestuffs have been found which, in the form of the free acid, correspond to the formula (I) STR1 represents H or an optionally substituted aliphatic or aromatic radical and R1 to R6 and A have the meaning given in the description, which are outstandingly suitable for inkjet printing.
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(2008/06/13)

CARBOXY AND SUBSTITUTED CARBOXY AROLY PEPTIDES
Peptides of the formula STR1 wherein X is various amino or imino acids or esters are useful as hypotensive agents.
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(2008/06/13)