15870-78-7Relevant academic research and scientific papers
DERIVATIVES OF TRIAZINES AND URACILS, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPEUTICS
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Page/Page column 17-18, (2010/04/03)
The present invention relates to derivatives of general formula I wherein : - W represents nitrogen, - R1 represents: ? a hydrogen or a linear or branched C1-C5 alkyl radical or, ? a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, ? a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, ? a C6 2-oxocycloalkyl radical - R2 represents a methyl or heptyl, - m, n are equal to 1, - V represents CH2, - X-Y represents -N- (C=O) -, -CH-O-, - Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.
1,2,4-Triazine Derivatives, Preparation and Use Thereof in Human Therapy
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Page/Page column 7, (2008/12/06)
The invention concerns 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a branched or linear C1-C7 alkyl or alkenyl radical, a C1/s
Cyclohexane derivatives difunctionalised in 1,4 as ligands of 5T H1A receptors
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, (2008/06/13)
The invention concerns novel cyclohexane derivatives difunctionalised in 1.4 of general formula (1) in which A represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl or pyrimidinyl optionally substituted by one
3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT1A ligands
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, (2008/06/13)
A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I STR1 in which: R1 and R2, which are identical or different, represent hydrogen or C1 -C6 alkyl, n is 2 to 6, inclusive, A represents aryl piperazino II STR2 the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C1 -C3 alkyl, C1 -C3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino STR3 in which R represents hydrogen or C1 -C3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT1A receptor agonist therewith.
Anticoccidial derivatives of 6 azauracil. I. Enhancement of activity by benzylation of nitrogen 1. Observations on the design of nucleotide analogues in chemotherapy
Mylari,Miller,Howes Jr.,Figdor,Lynch,Koch
, p. 475 - 483 (2007/10/09)
Benzylation of 6-azauracil at N-1 (which corresponds to the point of attachment of the ribose phosphate unit in pyrimidine nucleotides) has been found to augment its anticoccidial activity fourfold. The high potency of 1-benzyl-6-azauracil is ascribed to a combination of intrinsic activity, efficient oral absorption, and a moderate rate of excretion. Metabolism experiments using 1-benzyl-6-azauracil labeled with 14C in the heterocycle and (separately) in the side chain showed that, in the drug accounted for, no cleavage had occurred. Additional activity increases were achieved by introducing small, electron-withdrawing substituents in the meta and/or para position(s) of the benzyl group. One of the most active derivatives, 1-(3-cyanobenzyl)-6-azauracil, is about 16 times as potent as 6-azauracil.
