- HIV reverse transcriptase/integrase double target inhibitors 6-benzoyl-substituted uracils preparation and application
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The invention relates to application of a novel HIV retrovirus/intergrase double-target inhibitor 6-benzoyl substituted uracil compounds and pharmaceutical compositions containing the compounds to AIDS-treating medicines and antiviral medicines. The invention also relates to a preparation method of the compounds. The compounds are shown as a general formula I, and all groups in the general formula I are defined in right claim, R1=H, CH2OH, CHO, COOH, COOCH3, COOCH2CH3, CONHCH3, CONHCH2CH3, and R=CH3, H, F.
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Paragraph 0018; 0019; 0020
(2016/10/08)
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- Novel HIV reverse transcriptase inhibitors
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The invention is related to compounds of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
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Page/Page column 99-100
(2008/06/13)
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- PYRIMIDINE SUBSTITUTED MACROCYCLIC HCV INHIBITORS
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Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
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Page/Page column 93
(2008/12/08)
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- Dimethoxypyrimidines as Novel Herbicides. Part 1. Synthesis and Herbicidal Activity of Dimethoxyphenoxypyrimidines and Analogues
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A number of 6-(4-phenoxyphenoxy)pyrimidines and triazines were synthesized and their herbicidal activity was measured. Compounds with the methoxy groups at the 2- and 4-positions on the pyrimidine and triazine rings exhibited high herbicidal activity. Introduction of a substituent into the 5-position of the pyrimidine ring diminished the activity. In the phenoxyphenoxy substructure at the 6-position, the central ether bond can be replaced by a methylene group without loss of activity. The optimum substituent on the terminal phenyl ring was 3-trifluoromethyl. The compounds showed a strong Hill reaction inhibition, but unfortunately showed poor selectivity between weeds and crops. - Keywords: phenoxyphenoxypyrimidines; phenoxyphenoxy-s-triazines; Hill reaction inhibitors; 2,6-dimethoxy-4-pyrimidine; 2,6-dimethoxy-4--s-triazine; herbicides
- Nezu, Yukio,Miyazaki, Masahiro,Sugiyama, Kazuhiko,Kajiwara, Ikuo
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p. 103 - 114
(2007/10/03)
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- Reactions of 4a-Peroxides and 4a-Pseudobases of N10- and N5-Phenethylflavins
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A number of N5,N10-dialkylisoalloxazines have been synthesized in which either the N5 or the N10 substituent is a meta-substituted phenethyl group.Some of these compounds have been subjected to experiments in order to determine whether an intramolecular transfer of oxygen can occur between the flavin and the phenethyl group (a model of monooxygenase).When in the 1,5-dihydro reduced state, N5-alkyl-substituted isoalloxazines react with molecular oxygen to dive 4a-hydroperoxy derivatives.The hydroperoxides of the N5-ethyl-N10-phenethylflavins provide 4a-pseudobases on spontaneous decomposition.These in turn undergo ring contraction in base to yield 10a-spirohydantoins (Scheme V).The structure of 10a-spirohydantoin (28b) is as established by X-ray crystallographic technique.Spontaneous decomposition of 4a-hydroperoxides is not accompanied by intramolecular oxygen transfer to the phenethyl substituent groups at N10 or N5 (eq.4) 10a-Spirohydantoins may also be obtained by base treatment of 4a-pseudobases that have been prepared separately from the oxidized isoalloxazine (i.e., flavinium cation). 4a-(Allylperoxy)flavin derivatives, obtained by addition of alkyl peroxides to flavinium cations, undergo both spontaneous and photochemocal conversion to 10a-spirohydantoin.These findings are discissed in therms of proposals which have been made for the mechanism of action of flavoenzyme monooxygenases.
- Iwata, Masaki,Bruice, Thomas C.,Carrell, H. L.,Glusker, Jenny P,
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p. 5036 - 5044
(2007/10/02)
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