- Amide compounds and uses thereof
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Provided herein are novel amide compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein the definition of each symbol is as described in the description.
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Page/Page column 62
(2021/10/11)
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- AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF CONDITIONS RELATED TO THE MODULATION OF IL-12, IL-23 AND/OR IFN-ALPHA
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Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-2
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Page/Page column 208-209
(2020/05/29)
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- Synthesis of a Water-Soluble, Soft N-Donor BTzBP Ligand Containing only CHON
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A hydrophilic ligand that contains only C, H, O, and N substituents and uses a 6,6′-bis(1 H -1,2,3-triazol-4-yl)-2,2′-bipyridine (BTzBP) structural core has been synthesized. The effect of adding water-soluble groups onto extractant ligands has been extensively studied to facilitate the efficient partitioning of 4f and transuranic 5f elements for the treatment of spent nuclear fuel. Soft, N-donor ligands exhibit greater binding affinities for the trivalent actinides over the trivalent lanthanides, making BTzBP ligands an ideal candidate in the search for extractants to be used on an industrial scale. To date, hydrophobic BTzBPs have been shown to exhibit physical and chemical properties that might be conducive to nuclear waste processing conditions. However, hydrophilic BTzBPs have yet to be reported. Herein, we show the synthesis of a hydrophilic BTzBP ligand featuring cationic water solubilizing groups attached to the bipyridal rings.
- Albright, Savannah G.,Ali, Bakr,Chapman, Hayley A.,Cheng, Yijie,Cusic, Rachel M.,Friese, Seth J.,Hartlove, Nathan B.,Labb, Samantha A.,Marr, Alissa N.,Masteran, Conner J.,Timmons, Miranda
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supporting information
p. 1384 - 1388
(2020/08/03)
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- DIHYDROPYRROLOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER
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The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 has any of the meanings hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and t
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Page/Page column 68
(2017/05/28)
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- Preparation method of 1-subtituted-1H-1,2,3-triazole-4-carboxylic acid
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The invention provides a preparation method of 1-subtituted-1H-1,2,3-triazole-4-carboxylic acid. The preparation method includes the following steps: 1-substituted-4,5-dibromo-1H-1,2,3-triazole is added to an isopropylmagnesium chloride, such that 1-substituted-4-bromo-1H-1,2,3-triazole is obtained through a reaction; an isopropylmagnesium chloride-lithium chloride complex is added directly, such that a mixture of 1-substituted-1H-1,2,3-triazole-4-carboxylic acid and 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylic acid is obtained; a base and iodomethane are added to the mixture, such that methyl 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylare is obtained through a reaction; the aqueous layer is adjusted with hydrochloric acid until a pH value is 1-5; extraction is carried out with an organic solvent, and drying and concentration crystallization are carried out, such that 1-substituted-1H-1,2,3-triazole-4-carboxylic acid is obtained. The method is suitable for industrial production, and has a great application value.
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Paragraph 0041; 0042; 0043
(2016/10/09)
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- BROMODOMAIN INHIBITORS AND USES THEREOF
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The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
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Page/Page column 151
(2012/11/14)
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- General solution to the synthesis of N-2-substituted 1,2,3-triazoles
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The regioselective N-alkylation of 1,2,3-triazoles 1 - 6 was studied. Good to excellent N-2 selectivity and high chemical yields for N-2-substituted 4,5-dibromotriazoles 7 were obtained with 4,5-dibromo- and 4-bromo-5- trimethylsilyl-1,2,3-triazoles. These building blocks can be readily converted to 2-mono-, 2,4-di-, and 2,4,5-polysubstituted triazoles 10 - 15, providing a general, protective, group-free method for the synthesis of N-2-substituted triazoles. Observed regioselectivities can be rationalized by a combination of Frontier Molecular Orbital, steric, and electrostatic directing effects on the heterocyclic scaffolds.
- Wang, Xiao-Jun,Zhang, Li,Krishnamurthy, Dhileepkumar,Senanayake, Chris H.,Wipf, Peter
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scheme or table
p. 4632 - 4635
(2010/12/18)
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- NOVEL HERBICIDES
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Compounds of formula I: wherein R1, R2, R3, R4, m, R5, R6, n and Y are as defined in claim 1; or N-oxides, salts and optical isomers thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising them and to methods of using them to control plants or to inhibit plant growth.
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Page/Page column 112
(2008/06/13)
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- HERBICIDAL ISOXAZOLINE COMPOUNDS
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Novel compounds of formula (I): wherein R1, R2, R3, R4, m, R5, R6, n and Y are as defined in claim 1; or N-oxides, salts and optical isomers thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising them and to methods of using them to control plants or to inhibit plant growth.
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- Towards the total synthesis of cyclo[n] carbons and the generation of cyclo[6]carbon
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We describe efforts towards the synthesis of some allotropes of carbon, the cyclo[n]carbons where n = 18, 24 and 30. The key intermediate 11 is hexa-1,3,5-triyne with the central triple bond masked as a 1-amino-1,2,3-triazole derivative. Cyclo-oligomerisation of this by oxidative coupling gives macrocyclic precursors of C18, C24 and C30. C30 is a proposed intermediate in the formation of C60 and we also describe some attempts at the synthesis of C60 via the chemical generation of benzotriyne, cyclo[6]carbon.
- Adamson, George A.,Rees, Charles W.
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p. 1535 - 1543
(2007/10/03)
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