214633-89-3Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AND THEIR USE FOR THE TREATMENT OF NEURODEGENERATIVE TAUOPATHIES
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, (2014/04/04)
The present invention is directed to triazolopyrimidine, phenylpyrimidine, pyridopyridazine, and pyridotriazine compounds and their use in the treatment of neurodegenerative disorders.
USE OF HYDROPHOBIN AS A SPREADING AGENT
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, (2012/01/12)
The present invention relates to the use of hydrophobin as a spreading agent, in particular in cosmetic or pharmaceutical compositions. The invention further relates to compositions for treating surfaces, in particular cosmetic or pharmaceutical compositions for topical use, that contain hydrophobin as a spreading agent.
Synthesis and SAR of [1,2,4]triazolo[1,5-a]pyrimidines, a class of anticancer agents with a unique mechanism of tubulin inhibition
Zhang, Nan,Ayral-Kaloustian, Semiramis,Nguyen, Thai,Afragola, Jay,Hernandez, Richard,Lucas, Judy,Gibbons, James,Beyer, Carl
, p. 319 - 327 (2007/10/03)
The synthesis and SAR of a series of triazolopyrimidines as anticancer agents are described. Treatment of 5-chloro-6-(trifluorophenyl)-N-fluoroalkyl[1, 2,4]triazolo[1,5-a]pyrimidin-7-amine with an alcohol, a thiol, or an alkylamine provided the corresponding final compounds. A clear SAR requirement has been established for optimal activity. A (1S)-2,2,2-trifluoro-1-methylethylamino group or an achiral 2,2,2-trifluoroethylamino group is required at the 5-position to achieve high potency. On the phenyl ring, both fluoro atoms, at the positions ortho to the triazolopyrimidine core, are needed for optimal activity. At the position para to the triazolopyrimidine core, on the phenyl ring, the best activity is achieved with an oxygen linkage followed by a three-methylene unit, and an alkylamino or a hydroxy group. The mechanism of action for this series of triazolopyrimidines was shown to be unique in that they promoted tubulin polymerization in vitro, but did not bind competitively with paclitaxel. Instead, they inhibit the binding of vincas to tubulin. Selected compounds were studied further, and it was shown that these compounds were able to overcome resistance attributed to several multidrug resistance transporter proteins. Lead compounds were shown to inhibit tumor growth in several nude mouse xenograft models, with high potency and efficacy, when dosed either orally or intravenously.
5-arylpyrimidines as anticancer agents
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Page/Page column 34-35, (2008/06/13)
This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof, wherein said compounds are anti-cancer agents useful for
Fungicidal trifluorophenyl-triazolopyrimidines
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, (2008/06/13)
The novel compounds of formula I: (R1, R2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.
FUNGICIDAL TRIFLUOROPHENYL-TRIAZOLOPYRIMIDINES
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, (2008/06/13)
The novel compounds of formula (I) (R, R and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.
Fungicidal trifluorophenyl-triazolopyrimidines
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, (2008/06/13)
The novel compounds of formula I: (R1, R2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.
Fungicidal trifluoromethylalkylamino-triazolopyrimidines
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, (2008/06/13)
The novel compounds of formula I: STR1 wherein R1, R2, Hal and L1 through L5, are defined in the specification show selective fungicidal activity.
