849600-02-8

Upstream product

• 849600-51-7 4,6-dichloro-2-(pyrazin-2-yl)-5-(2,4,6-trifluorophenyl)pyrimidine 
• 753-90-2 trifluoroethylamine 
• 262609-07-4 diethyl (2,4,6-trifluoro-phenyl)-malonate 
• 200928-43-4 2-carbamidinopyrazine 
• 849600-52-8 2-pyrazin-2-yl-5-(2,4,6-trifluorophenyl)pyrimidine-4,6-diol 

Downstream Products

• 849600-38-0 6-chloro-5-(4-[2-(dimethylamino)ethoxy]-2,6-difluorophenyl)-2-pyrazin-2-yl-N-(2,2,2-trifluoroethyl)pyrimidin-4-amine 
• 849600-36-8 6-chloro-5-(4-[3-(dimethylamino)propoxy]-2,6-difluorophenyl)-2-pyrazin-2-yl-N-(2,2,2-trifluoroethyl)pyrimidin-4-amine 
• 849600-39-1 6-chloro-5-(4-[4-(dimethylamino)butoxy]-2,6-difluorophenyl)-2-pyrazin-2-yl-N-(2,2,2-trifluoroethyl)pyrimidin-4-amine 

Relevant academic research and scientific papers

Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies

Microtubule (MT) stabilizing drugs hold promise as potential treatments for Alzheimer's disease (AD) and related tauopathies. However, thus far epothilone D has been the only brain-penetrant MT-stabilizer to be evaluated in tau transgenic mice and in AD p

HETEROCYCLIC COMPOUNDS AND THEIR USE FOR THE TREATMENT OF NEURODEGENERATIVE TAUOPATHIES

The present invention is directed to triazolopyrimidine, phenylpyrimidine, pyridopyridazine, and pyridotriazine compounds and their use in the treatment of neurodegenerative disorders.

Synthesis and SAR of 6-chloro-4-fluoroalkylamino-2-heteroaryl-5-(substituted)phenylpyrimidines as anti-cancer agents

The synthesis and SAR of a series of 6-chloro-4-fluoroalkylamino-2-heteroaryl-5-(substituted)phenylpyrimidines as anti-cancer agents are described. This series of 2-heteroarylpyrimidines was developed by modifying a series of anti-tumor [1,2,4]triazolo[1,5-a]pyrimidines and 2-cyanoaminopyrimidines we reported earlier. For the 2-heteroaryl group, the best activity is obtained when the heteroaryl group has a nitrogen atom at the ortho-position to the pyrimidyl core. The structure-activity relationship for the rest of the molecule in this 2-heteroarylpyrimidine series mimics that of the [1,2,4]triazolo[1,5-a]pyrimidine series. Like triazolopyrimidines and 2-cyanoaminopyrimidines, the 2-heteroarylpyrimidines retain the capability to overcome multidrug resistance due to Pgp. Mechanism of action studies showed that the lead compounds behaved in the same manner as triazolopyrimidines and 2-cyanoaminopyrimidines. The lead compounds in this series are more potent than the corresponding triazolopyrimidines in vitro and in vivo. Compound 21 (PTI-868) showed tumor growth inhibition in several nude mouse xenograft models, and was selected to advance to preclinical development.

5-arylpyrimidines as anticancer agents

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