- A class of 4, 5 - disubstituted imidazole derivatives and its preparation and use (by machine translation)
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The invention relates to a compound of general formula I indicated by the 4, 5 - disubstituted imidazole compound, or its pharmaceutically acceptable salt, pharmaceutical composition containing the same and its preparation and use, the compounds can be used as a xanthine oxidase (Xanthine oxidase, XO) inhibitor, used for the treatment of uric acid crystallization at the joints to the deposition of Gout and its complications. (by machine translation)
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Paragraph 0135-0137
(2017/07/22)
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- The effects of ring substituents and leaving groups on the kinetics of SNAr reactions of 1-halogeno- and 1-phenoxy-nitrobenzenes with aliphatic amines in acetonitrile
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Rate constants are reported for the reactions of a series of 1-chloro-, 1-fluoro- and 1-phenoxy-nitrobenzenes activated by CF3 or CN groups or by ring-nitrogen with n-butylamine, pyrrolidine or piperidine in acetonitrile. The results are compar
- Crampton, Michael R.,Emokpae, Thomas A.,Isanbor, Chukwuemeka
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p. 1378 - 1383
(2008/09/18)
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- Substituted compounds derived from N-(benzyl)phenylacetamide, preparation and uses
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This invention relates to poly-substituted derivatives of the N-(benzyl)phenylacetamide type, pharmaceutical compositions comprising same, therapeutic uses thereof, more particularly in the fields of human and animal health. This invention also relates to a process for the preparation of such derivatives.
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Page/Page column 38
(2010/10/20)
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- Fused bicyclic amide compounds and medicinal use thereof
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The present invention provides a compound represented by the formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine or a derivative thereof, imidazole or a derivative thereof and the like, ring B is benzene, cyclohexane, pyrrole or a derivative thereof, furan, thiophene and the like, R1, R2 and R3 are each hydrogen, alkyl, halogen, hydroxyl group, alkoxy and the like, W is hydrogen, alkyl or hydroxycarbonylalkyl, X is halogen, cyano, nitro and the like, X′ is hydrogen, halogen and the like, and Y is alkyl, hydroxyalkyl, hydroxycarbonylalkyl, aminoalkyl and the like, a salt thereof, and a pharmaceutical agent containing the compound. The compound of the present invention shows a superior inhibitory effect on the proliferation of activated lymphocyte and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
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- AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
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- Role of lactam vs. lactim tautomers in 2(1H)-pyridone catalysis of aromatic nucleophilic substitution
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3-Ethylaminocarbonyl-2(1H)-pyridone 1 and 3-ethoxycarbonyl-2(1H)-pyridone 2 have been synthesised and tested as catalysts for the aromatic nucleophilic substitution of fluoride by piperidine in 2-fluoro-5-nitrobenzonitrile 3. A kinetic model which takes into account the dimerisation of the catalysts has been developed, which allows a quantitative analysis of measured data. 3-Ethylaminocarbonyl-2(1H)-pyridone 1 exists exclusively as a lactam tautomer, either monomeric or dimeric but 3-ethoxycarbonyl-2(1H)-pyridone 2 exists as a lactim monomer, whereas its dimer exists in the lactam form. Despite such differences, these two compounds exhibit similar catalytic efficiencies for the reaction studied, suggesting that lactim and lactam tautomers have comparable efficiencies in tautomeric catalysis.
- Loppinet-Serani, Anne,Charbonnier, Florence,Rolando, Christian,Huc, Ivan
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p. 937 - 942
(2007/10/03)
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- The Origins of the Dichotomy of Amine Effects in Aromatic Nucleophilic Substitution Reactions
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The reactions of 2-trifluoromethyl- amd 2-cyano-4-nitrofluoro-benzenes with piperidine, n-butylamine and benzylamine in acetonitrile are not base catalysed, but the reactions with morpholine are catalysed.In benzene, the reactions of the 2-cyano-substrate
- Akpojivi, Raymond E.,Emokpae, Thomas A.,Hirst, Jack
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p. 443 - 450
(2007/10/02)
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