- SUBSTITUTED HYDROXYSTILBENE COMPOUNDS AND DERIVATIVES SYNTHESIS AND USES THEREOF
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The present disclosure relates to substituted hydroxystilbene compounds and derivatives, specifically 2-substituted hydroxystilbene compounds and derivatives, the synthesis of such compounds and their use in therapy.
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Page/Page column 170
(2021/07/02)
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- BICYCLIC COMPOUND
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Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.
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Paragraph 0921
(2017/12/28)
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- Conjugatable and Bioreduction Cleavable Linker for the 5′-Functionalization of Oligonucleotides
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An efficient conjugatable and bioreduction cleavable linker was designed and synthesized for the 5′-terminal ends of oligonucleotides. A phosphoramidite reagent bearing this linker was successfully applied to solid phase synthesis and incorporated at the 5′-terminal ends of oligonucleotides. The controlled pore glass (CPG)-supported oligonucleotides were subsequently conjugated to a diverse range of functional molecules using a CuAAC reaction. The synthesized oligonucleotide conjugates were then cleaved using a nitroreductase/NADH bioreduction system to release the naked oligonucleotides.
- Saneyoshi, Hisao,Yamamoto, Yuta,Kondo, Kazuhiko,Hiyoshi, Yuki,Ono, Akira
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p. 1796 - 1802
(2017/02/10)
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- Diphenylpolyene-cholesterol conjugates as fluorescent probes for microheterogeneous media
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Extrinsically conjugated fluorescent diphenylpolyene cholesterol derivatives are synthesized and spectroscopic investigations in homogeneous and aqueous micellar solutions are described. The emission of these cholesterol conjugates reveals characteristic
- Palakollu, Veerabhadraiah,Kanvah, Sriram
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- Thermally robust Au99(SPh)42 nanoclusters for chemoselective hydrogenation of nitrobenzaldehyde derivatives in water
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We report the synthesis and catalytic application of thermally robust gold nanoclusters formulated as Au99(SPh)42. The formula was determined by electrospray ionization and matrix-assisted laser desorption ionization mass spectrometry in conjunction with thermogravimetric analysis. The optical spectrum of Au99(SPh)42 nanoclusters shows absorption peaks at ～920 nm (1.35 eV), 730 nm (1.70 eV), 600 nm (2.07 eV), 490 nm (2.53 eV), and 400 nm (3.1 eV) in contrast to conventional gold nanoparticles, which exhibit a plasmon resonance band at 520 nm (for spherical particles). The ceria-supported Au99(SPh)42 nanoclusters were utilized as a catalyst for chemoselective hydrogenation of nitrobenzaldehyde to nitrobenzyl alcohol in water using H2 gas as the hydrogen source. The selective hydrogenation of the aldehyde group catalyzed by nanoclusters is a surprise because conventional nanogold catalysts instead give rise to the product resulting from reduction of the nitro group. The Au 99(SPh)42/CeO2 catalyst gives high catalytic activity for a range of nitrobenzaldehyde derivatives and also shows excellent recyclability due to its thermal robustness. We further tested the size-dependent catalytic performance of Au25(SPh)18 and Au36(SPh)24 nanoclusters, and on the basis of their crystal structures we propose a molecular adsorption site for nitrobenzaldehyde. The nanocluster material is expected to find wide application in catalytic reactions.
- Li, Gao,Zeng, Chenjie,Jin, Rongchao
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p. 3673 - 3679
(2014/03/21)
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- Benzimidazole Thiophene Compounds
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The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
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Page/Page column 54
(2009/01/20)
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- Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1
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A regioselective synthesis of novel 1-(2-thienyl)-benzimidazole inhibitors of polo-like kinase 1 is described. Amination of substituted 2-iodo or -bromo nitrobenzenes with a 2-aminothiophene derivative catalyzed by Pd2dba3 and XANTPH
- Hornberger, Keith R.,Badiang, Jennifer G.,Salovich, James M.,Kuntz, Kevin W.,Emmitte, Kyle A.,Cheung, Mui
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supporting information; body text
p. 6348 - 6351
(2009/04/07)
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- BENZIMIDAZOLE THIOPHENE COMPOUNDS
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The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
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Page/Page column 43
(2010/11/26)
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- REGIOSELECTIVE PROCESS FOR PREPARING BENZIMIDAZOLE THIOPHENES
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The present invention provides a process for preparing benzimidazole thiophene compounds of formula I. Intermediates used in the process are also claimed.
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Page/Page column 70-71
(2010/11/26)
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- BENZIMIDAZOLE THIOPHENE COMPOUNDS
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The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
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Page/Page column 125
(2008/06/13)
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- 2-(Amino or substituted amino)-5-(substituted oxymethyl)-phenol compounds, dyeing compositions containing them, and use thereof
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Disclosed are 2-(amino or substituted amino)-5-(substituted oxymethyl)-phenol compounds according to the Formula (I), as defined herein. Also, compositions for the oxidative dyeing of keratin fibers, comprising a medium suitable for dyeing and a compound of the Formula (II), as defined herein. The substituents of both formulae may themselves be substituted or unsubstituted. Further, methods for oxidative dyeing of keratin fibers, comprising applying such compositions in the presence of an oxidizing agent, for a period which is sufficient to develop the desired coloration.
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- Tricyclic indole-2-carboxylic acids: Highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor
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A series of tricyclic indole-2-carboxylic acid derivatives were synthesized and evaluated by the radioligand binding assay and the anticonvulsant effects in the mouse NMDA-induced seizure model. Among them, derivatives of 3S-(-)-4 such as 3a, 3f, and 3g which had certain zwitterionic anilides showed high affinity to the NMDA-glycine binding site. The absolute configuration of 3S-(-)-4 was confirmed by X-ray crystallographic analysis. In particular, 3g (SM-31900) was found to be a highly active glycine antagonist for both in vitro and in vivo assays (Ki = 1.0 ± 0.1 nM, ED50 = 2.3 mg/kg, iv) and also showed high selectivity for the glycine site. In addition, 3g was soluble enough in aqueous media (> 10 mg/mL at pH 7.4) to use for medications by intravenous injection.
- Katayama, Seiji,Ae, Nobuyuki,Kodo, Toru,Masumoto, Shuji,Hourai, Shinji,Tamamura, Chika,Tanaka, Hiroyasu,Nagata, Ryu
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p. 691 - 701
(2007/10/03)
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- Synthesis of anti-rheumatic agent epoxyquinomicin B
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Anti-rheumatic agent (±)-epoxyquinomicin B was synthesized for a 22% overall yield in eight steps from commercially available 3-hydroxy-4- nitrobenzaldehyde via the intermediate quinone 6 prepared by selective phenol oxidation of 5 by use of Fremy's salt as the key step.
- Matsumoto, Naoki,Iinuma, Hironobu,Sawa, Tsutomu,Takeuchi, Tomio
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p. 2945 - 2948
(2007/10/03)
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- Selective detection of the carbohydrate-bound state of concanavalin A at the single molecule level
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The labeling of molecules with charge-transfer dyes, such as 5-(dimethylamino)-1-napthalenesulfonyl (dansyl) chloride, is a powerful tool for examining the solvent shell of attached substances. This investigation describes the synthesis and application of
- La Clair, James J.
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p. 7676 - 7684
(2007/10/03)
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- Synthesis of 5-(tert-Butoxycarbonylaminoacetoxymethyl)-2-nitrophenoxyacetic Acid
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5-(tert-Butoxycarbonylaminoacetoxymethyl)-2-nitrophenoxyacetic acid was synthesized in seven steps starting from 5-methyl-2-nitrophenol. Its phenyl ester was selectively hydrolyzed with triethylamine in aqueous dioxane. 5-Hydroxymethyl-2-nitrophenoxyacetic acid was formed as by-product. Its formation was proved by independent synthesis from 1-acetoxy-5-bromomethyl-2-nitrobenzene. Experimental difficulties that arise along other routes to the target compound are discussed.
- Selivanov,Kulikov,Ginak
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p. 394 - 400
(2007/10/03)
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- Potential photoaffinity labels for tubulin. Synthesis and evaluation of diazocyclohexadienone and azide analogs of colchicine, combretastatin, and 3,4,5-trimethoxybiphenyl
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Analogs of tubulin assembly inhibitors such as colchicine, combretastatin, and 3,4,5-trimethoxybiphenyl which incorporate a 6-diazo-2,4-cyclohexadienone (o-quinone diazide) ring have been synthesized and characterized. The compounds synthesized include 6-diazo-4-(2',3',4'-trimethoxyphenyl)cyclohexa-2,4-dien-1-one and its 3-methyl and 3-ethyl analogs (1a-c), 6-diazo-3-(2,3,4-trimethoxyphenyl)-2,4-cyclohexadien-1-one and its 4-methyl and 4-ethyl derivatives (2a-c), 4-[Z-2-(3',4',5'-trimethoxyphenyl)ethenyl]-6-diazocyclohexa-2,4-dienon e (3), 3-[Z-2-(3',4',5'-trimethoxyphenyl)ethenyl]-6-diazocyclohexa-2,4-dien-1 -one (4), the corresponding dihydro derivatives (5, 6) and two isomeric diazocyclohexadienones derived from N-acetylcolchinol (7, 8). Compounds in which the cyclohexadienone oxygen is approximately isostructural with carbonyl or hydroxy functions of the parent compounds exhibit good activity in the tubulin assembly inhibition assay. 2'-Alkyl-4'azido-3,4,5-trimethoxy-1,1'-biphenyls also show good activity as tubulin assembly inhibitors.
- Olszewski,Marshalla,Sabat,Sundberg
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p. 4285 - 4296
(2007/10/02)
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- Ester derivatives and pharmaceutical compositions containing them
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The invention concerns ester derivatives of the formula I wherein Ar is phenyl, naphthyl, indenyl, indanyl, a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from
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