- GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
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Paragraph 00974-00976; 001478; 001479
(2021/01/22)
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- A Ni-Mg-Al layered triple hydroxide-supported Pd catalyst for heterogeneous acceptorless dehydrogenative aromatization
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In the presence of a Ni-Mg-Al layered triple hydroxide-supported Pd catalyst, the acceptorless dehydrogenative aromatization of a wide range of cyclohexanols/cyclohexanones and cyclohexylamines efficiently proceeded to give the corresponding phenols and anilines, respectively, in moderate to high yields with the liberation of molecular hydrogen.
- Jin, Xiongjie,Taniguchi, Kento,Yamaguchi, Kazuya,Nozaki, Kyoko,Mizuno, Noritaka
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supporting information
p. 5267 - 5270
(2017/07/10)
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- Au-Pd alloy nanoparticles supported on layered double hydroxide for heterogeneously catalyzed aerobic oxidative dehydrogenation of cyclohexanols and cyclohexanones to phenols
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Phenol, an important industrial chemical, is widely produced using the well-developed cumene process. However, demand for the development of a novel alternative method for synthesizing phenol from benzene has been increasing. Herein, we report a novel system for the synthesis of phenols through aerobic oxidative dehydrogenation of cyclohexanols and cyclohexanones, including ketone-alcohol (KA) oil, catalyzed by Mg-Al-layered double hydroxide (LDH)-supported Au-Pd alloy nanoparticles (Au-Pd/LDH). Alloying of Au and Pd and basicity of LDH are key factors in achieving the present transformation. Although monometallic Au/LDH, Pd/LDH, and their physical mixture showed almost no catalytic activity, Au-Pd/LDH exhibited markedly high catalytic activity for the dehydrogenative phenol production. Mechanistic studies showed that β-H elimination from Pd-enolate species is accelerated by Au species, likely via electronic ligand effects. Moreover, the effect of supports was critical; despite the high catalytic performance of Au-Pd/LDH, Au-Pd bimetallic nanoparticles supported on Al2O3, TiO2, MgO, and CeO2 were ineffective. Thus, the basicity of LDH plays a deterministic role in the present dehydrogenation possibly through its assistance in the deprotonation steps. The synthetic scope of the Au-Pd/LDH-catalyzed system was very broad; various substituted cyclohexanols and cyclohexanones were efficiently converted into the corresponding phenols, and N-substituted anilines were synthesized from cyclohexanones and amines. In addition, the observed catalysis was truly heterogeneous, and Au-Pd/LDH could be reused without substantial loss of its high performance. The present transformation is scalable, utilizes O2 in air as the terminal oxidant, and generates water as the only by-product, highlighting the potential practical utility and environmentally benign nature of the present transformation. Dehydrogenative aromatization of cyclohexanols proceeds through (1) oxidation of cyclohexanols to cyclohexanones; (2) dehydrogenation of cyclohexanones to cyclohexenones; and (3) disproportionation of cyclohexenones to afford the desired phenols. In the present Au-Pd/LDH-catalyzed transformation, the oxidation of the Pd-H species is included in the rate-determining step.
- Jin, Xiongjie,Taniguchi, Kento,Yamaguchi, Kazuya,Mizuno, Noritaka
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p. 5371 - 5383
(2016/07/29)
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- Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
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A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
- Zhang, Xuqing,Hufnagel, Heather,Markotan, Thomas,Lanter, James,Cai, Chaozhong,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Sui, Zhihua
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supporting information; experimental part
p. 5577 - 5582
(2011/10/09)
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- Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides
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Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His 6 with phenyl-containing rigid templates in achieving good hMC4R agonist potency and selectivity against hMC1R in linear pentapeptides.
- Chu, Xin-Jie,Bartkovitz, David,Danho, Waleed,Swistok, Joseph,Cheung, Adrian Wai-Hing,Kurylko, Grazyna,Rowan, Karen,Yeon, Mitch,Franco, Lucia,Qi, Lida,Chen, Li,Yagaloff, Keith
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p. 4910 - 4914
(2007/10/03)
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- Alkenylcyclohexane liquid crystalline compounds
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Compounds of the formula STR1 wherein Z1 denotes a single covalent bond or --CH2 Ch2 --; ring A1 represents 1,4-phenylene, pyrimidine-2,5-diyl, pyridine-2,5-diyl or, when Z1 stands for --CH2 CH2 --, also trans-1,4-cyclohexylene; X1 stands for fluorine or chlorine; X2 signifies fluorine, chlorine or hydrogen, with the proviso that X2 only signifies hydrogen when X1 is chlorine or when ring A1 signifies pyridine-2,5-diyl and Z1 signifies --CH2 CH2 --; and R1 signifies 1E-alkenyl with 2 to 12 carbon atoms, their manufacture, liquid crystalline mixtures which contain these compounds and their use for electro-optical purposes.
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- Regioselective Photocycloadditions of Benzoquinones to Alkylidenecyclohexanes: A New Synthetic Resource
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Benzoquinones add regioselectively to alkylidenecyclohexanes.The photoadducts are converted into useful building blocks in good yield.
- Ciufolini, Marco A.,Rivera-Fortin, M. Angelica,Byrne, Norman E.
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p. 3505 - 3508
(2007/10/02)
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