- Novel organotin complexes with phenol and imidazole moieties for optimized antitumor properties
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A series of novel imidazole-containing ligands and their organotin complexes were synthesized and characterized by NMR, IR, MALDI and elemental analysis. Redox behavior was studied by cyclic voltammetry (CV). Antioxidant properties were estimated in model
- Antonets, A. A.,Dubova, L. G.,Gontcharenko, V. E.,Gracheva, Yu A.,Kazak, A. A.,Lyssenko, K. A.,Milaeva, E. R.,Mironova, E. M.,Nikitin, E. A.,Pavlyukov, M. S.,Shamraeva, M. A.,Shevtsov, P. N.,Shevtsova, E. F.,Shpakovsky, D. B.,Shtil, A. A.,Tyurin, V. Yu,Vasilichin, V. A.
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- METHOD
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The present invention relates to a method of treating pain in a patient in need of such treatment, said method comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt o
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Paragraph 0221; 0222
(2018/06/04)
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- Novel diphenylsulfimide antioxidants containing 2,6-di-tert-butylphenol moieties
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New diphenylsulfimide derivatives containing substituents with the 2,6-di-tert-butylphenol moiety at the nitrogen atom were synthesized. Their molecular structures were established by X-ray diffraction. Antioxidant activity was experimentally evaluated by spectrophotometry based on hydrogen transfer to the stable radicals, namely, 2,2-diphenyl-1-picrylhydrazyl and the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation (ABTS·+), and using in vitro lipid peroxidation in rat brain and liver homogenates. The presence of phenol and diphenylsulfimide moieties in one molecule leads to a significant enhancement of antioxidant activity. The new compounds exhibit moderate inhibitory activity against enzymes involved in carbohydrate and lipid metabolism. The evaluation of antiglycation activity showed that the new sulfimides taken at a concentration of 100 μmol L–1 have activity comparable with that of aminoguanidine.
- Milaeva,Shpakovsky,Maklakova,Rufanov,Neganova,Shevtsova,Churakov,Babkova,Babkov,Kosolapov,Spasov
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p. 2025 - 2034
(2019/01/08)
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- DEVELOPING POTENT URATE TRANSPORTER INHIBITORS: COMPOUNDS DESIGNED FOR THEIR URICOSURIC ACTION
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A compound represented by the general Formula (I): a pharmaceutically acceptable salt or ester thereof, a solvate thereof, a chelate thereof, a non-covalent complex thereof, a pro-drug thereof, a deuterated radio-labeled analog thereof, and mixtures of any of the foregoing, wherein: A - K are individually selected from carbon or nitrogen; X = -O, -NR1,or -S; R1-11 are individually selected from the group consisting of-H, C1-C6 alkyl, C6-C aryl, substituted C6-C14 aryl, C1-C14-alkoxy, halogen, hydroxyl, carboxy, cyano, C1-C6-alkanoyloxy, C1-C6-alkylthio, C1-C6-alkylsulfonyl, trifluoromethyl, hydroxy, C2-C6-alkoxycarbonyl, C2-C6-alkanoylamino, -O-R12, S-R12,-SO2-Ri2, -NHSO2R12 and -NHCO2R12, wherein R12 is phenyl, naphthyl, or phenyl or naphthly substituted with one to three groups selected from C1-C6-alkyl, C6-C10 aryl,C1-C6-alkoxy and halogen, and C4-C20 hydroxyheteroaryl wherein the heteroatoms are selected from the group consisting of sulfur, nitrogen, and oxygen.
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Page/Page column 41-42
(2012/04/23)
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- NOVEL GLUCOPYRANOSE DERIVATIVES, PREPARATION THEREOF, AND BIOLOGICAL USES THEREOF
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The invention relates to a novel ester, the 3,5-di-tertiobutyl-4-hydroxybenzoate of 3,4,5-trihydroxy-6-methoxytetrahydropyran-2-yl methyl defined by the following formula (I). The invention also relates to the method for preparing the compound of formula
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Page/Page column 3
(2011/06/24)
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- Synthesis of new functionalized mono-And bisphosphinates with 2,6-di-tert-butyl-4-methylphenol fragments
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Convenient procedures for the synthesis of functionalized mono- and bisphosphinates with 2,6-di-tert-butyl-4-methylphenol (ionol) fragments, starting from the available 3,5-di-tert-butyl-4-benzaldehyde and its derivatives, are proposed, and some propertie
- Prishchenko, Andrey A.,Livantsov, Mikhail V.,Novikova, Olga P.,Livantsova, Ludmila I.,Milaeva, Elena R.
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p. 562 - 568
(2008/12/22)
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- SKIN-WHITENING COSMETIC
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Disclosed are: a novel skin-whitening agent; and a skin-whitening cosmetic or quasi-drug which is highly effective for prevention/amelioration of melanopathy and is prepared using the skin-whitening agent. The cosmetic contains a compound represented by t
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Page/Page column 8
(2008/12/08)
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- 2-ARYLTHIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
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The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
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Page/Page column 75
(2010/11/28)
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- New analogues of butylated hydroxytoluene as anti-inflammatory and antioxidant agents
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Amine or amide derivatives bearing the 2,6-di-tert-butyl phenol moiety are synthesised. Almost all are antioxidants, reduce acute inflammation and inhibit COX-1 and lipoxygenase activity. The most potent anti-inflammatory, COX-1 inhibitor and antioxidant agent, with low toxicity, is 2,6-di-tert-butyl-4-thiomorpholin-4-ylmethyl-phenol.
- Ziakas, George N.,Rekka, Eleni A.,Gavalas, Antonios M.,Eleftheriou, Phaedra T.,Kourounakis, Panos N.
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p. 5616 - 5624
(2007/10/03)
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- Substituted Azetidine compounds, their preparation and use as medicaments
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The present invention relates to substituted Azetidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals
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Page/Page column 9
(2010/02/13)
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- NO-mediated aromatic nitration during decomposition of phenolic S-nitrosothiols in non-aqueous aerobic medium
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Five novel S-nitrosothiol compounds (6-10) derived from L-cysteine were generated in solution and their decomposition rate was followed by UV spectroscopy. In acetonitrile, compounds 9 and 10 were the most stable of this series with a half-life of 24 h. T
- Petit,Bernardes-Genisson,Hoffmann,Souchard,Labidalle
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p. 1634 - 1638
(2007/10/03)
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- POLY(OXYALKYLENE) HYDROXYAROMATIC ESTERS AND FUEL COMPOSITIONS CONTAINING THE SAME
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Poly(oxyalkylene) hydroxyaromatic esters having the formula: (I) or a fuel-soluble salt thereof; where R1 and R2 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; R3 and R
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- Dual inhibition of human leukocyte elastase and lipid peroxidation: In vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives
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A series of potent and selective human leukocyte elastase (HLE) inhibitors of the Val-Pro-Val type has been developed. Initially, the central proline residue was replaced by nonnatural amino acids Phi ((2S,3aS,7aS)- perhydroindole-2-carboxylic acid) and A
- Portevin, Bernard,Lonchampt, Michel,Canet, Emmanuel,De Nanteuil, Guillaume
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p. 1906 - 1918
(2007/10/03)
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- Antioxidant grafted polysaccharides
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Grafted polysaccharide compositions comprising polysaccharides grafted with antioxidants on at least one hydroxyl group of the polysaccharide. The use of antioxidant grafted polysaccharides or antioxidant grafted crosslinked polysaccharides as a treatment
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- 1-arylpyrimidine derivatives and pharmaceutical use thereof
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The present invention relates to 1-arylpyrimidine derivatives represented by general formula (I): STR1 wherein R1 is H, alkyl or aralkyl; Ar is 1-naphthyl, or a substituted or unsubstituted phenyl group; R4 is a substituted phenyl, a substituted styryl, 1-methylcyclohexyl, 4-methylcyclohexyl, 4-oxo-4H-pyran-2-yl or 2-oxo-2H-pyran-5-yl group; R5 and R6 are each independently H or alkyl; R3 is H, and R7 and R8 are combined together to be oxo, or else R3 and R7 are combined together to be another direct bond, and R5 and R8 are combined together to be a direct bond, or pharmaceutically acceptable salts thereof; and methods for treating allergic diseases with such compounds.
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- N-(carbonyl, carbonimidoyl, carbonothioyl)sulfonamide charge control agents and toners and developers
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An electrophotographic toner having polymeric binder and a charge control agent selected from the group consisting of sulfonamides having the general structure: STR1 and metal salts thereof. T1 is independently selected from H, alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. R1 is O, S, N--H, N--R5, or N--L--R5 ; where L is a linking group selected from: STR2 and R5 is independently selected from alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. L1 and L2 are each independently a direct link or divalent alkyl or fluoroalkyl having from 1 to 20 carbons. Ra and Rb are each independently selected from the group consisting of H, F and ring systems having a solitary ring or from 2 to 3 fused or linked rings, said ring system having from 3 to 34 carbons, including carbons of substituent groups. If L1 is a direct link, Ra is a ring system and if L2 is a direct link, Rb is a ring system.
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- Medicinal use of 3',5'-di-tert.-butyl-4'-hydroxy flavones
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Compounds of the general formula (I): STR1 in which R represents: a hydrogen atom, or a radical --OR' in which R' is as defined in the description.
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- Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions
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Bi-aromatic esters have the formula STR1 wherein R1 represents H, OH, --CH3, --CH2 OH, --CH(OH)CH3, --COOR9, STR2 or SO2 R10 ; R9 represents H, C1 -C6
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- Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, - 1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents
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To discover dual inhibitors of 5-lipoxygenase (LO) and cyclooxygenase (CO) with improved pharmacokinetic properties, we have designed and synthesized series of 1,2,4-triazole, 1,3,4-oxadiazole, and 1,3,4-thiadiazole di-tert- butylphenol derivatives which
- Mullican,Wilson,Connor,Kostlan,Schrier,Dyer
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p. 1090 - 1099
(2007/10/02)
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- SYNTHESIS OF STERICALLY HINDERED PHENOLS OF THE DIARYLAMIDINE SERIES AND THE PROPERTIES OF RADICALS BASED ON THEM
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The stereodynamics and 1,3-migrations of various groups in free phenoxyl radicals containing a diarylamidine fragment at the para position of the phenoxyl ring were studied by the dynamic ESR method.The reversible Z,E-isomerization process was detected in
- Ivakhnenko, E. P.,Shif, A. I.,Prokof'ev, A. I.,Olekhnovich, L. P.,Minkin, V. I.
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p. 319 - 328
(2007/10/02)
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- Novel anti-inflammatory agents, pharmaceutical compositions and methods for reducing inflammation
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The present invention relates to novel specifically-substituted phenyl compounds, especially substituted di-tert-butyl phenol derivatives, which are effective as anti-inflammatory, analgesic and/or antipyretic agents. These phenyl compounds are substituted with a low molecular weight alkyl chain which terminates in a specific unsaturated functional group. These unsaturated functionalities are --C CH, C=CH2, C=C=CH2, and aldehydes in the form of their acetals. The present invention further relates to pharmaceutical compositions which contain an anti-inflammatory agent of the present invention and a pharmaceutically-acceptable carrier. Finally, the present invention relates to methods for treating diseases characterized by inflammation, such as rheumatoid arthritis and osteoarthritis, in humans or lower animals. Such methods comprise administering to a human or lower animal in need of such treatment a safe and effective amount of an anti-inflammatory agent or composition of the present invention.
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- Ester of ω,ω-bis(dialkylhydroxyphenyl) alkanols as effective antioxidants
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This invention describes novel antioxidant compounds which are esters of ω,ω-bis(dialkylhydroxyphenyl) alkanols having the formula: STR1 wherein R1 is a tertiary alkyl group having 4-8 carbon atoms; R2 is alkyl having 1-4 carbon atom
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- Dual purpose stabilizer compounds and polymer compositions containing same
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Diesters of partially hindered mercaptophenols and 3,5-di-alkyl-4-hydroxybenzoic acid and its corresponding acid salt, wherein such diester corresponds to the following formula STR1 wherein R and R1 are the same and are selected from among the following STR2 with R6 and R7 being an aliphatic hydrocarbon radical of 3 to 10 carbon atoms; and y being 0-5; R2 is a tertiary aliphatic hydrocarbon radical having from 4 to 10 carbon atoms or an alicyclic hydrocarbon radical having from 4 to 10 carbon atoms, where the carbon atom of attachment to the aromatic ring is fully substituted; R3 is hydrogen, halogen, an aliphatic hydrocarbon radical having from 1 to 10 carbon atoms or an alicyclic hydrocarbon radical having from 3 to 10 carbon atoms; and R4 and R5 is STR3 where WHERE A and A' are independently selected from among hydrogen, an aliphatic hydrocarbon radical of 1 to 10 carbon atoms or an alicyclic hydrocarbon radical of 3 to 10 carbon atoms. The above diesters are highly effective stabilizers of polyolefins against oxidative degradation and also impart a modest degree of protection and such materials against UV degradation.
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- Benzoyloxybenzoates and compositions stabilized therewith
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Benzoyloxybenzoates having the formula STR1 wherein R1, R2, R3 and R4 are lower alkyl or cycloalkyl, X is oxygen or sulfur, and R5 is alkyl, aryl, alkaryl or hydrogen Are useful as stabilizers of orga
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