377729-82-3

Upstream product

• 377729-81-2 furan-2-carboxylic acid N-(6-amino-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-hydrazide 
• 377729-80-1 furan-2-carboxylic acid N-(2-amino-6-chloro-5-formylpyrimidin-4-yl)-hydrazide 
• 5604-46-6 2-amino-4,6-dichloropyrimidine-5-carboxaldehyde 
• 3326-71-4 2-furoic acid hydrazide 
• 6315-52-2 1,2-bis-tosyloxyethane 
• 162401-16-3 2-furan-2-yl-7H-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidin-5-yl amine 

Downstream Products

• 377727-26-9 SCH 412348 
• 377727-87-2 preladenant 

Relevant academic research and scientific papers

Nitrogen-containing fused tricyclic derivative and application thereof

The invention discloses a nitrogen-containing fused tricyclic derivative and application thereof, and particularly relates to a novel nitrogen-containing fused tricyclic derivative and a pharmaceutical composition containing the nitrogen-containing fused tricyclic derivative, and the nitrogen-containing fused tricyclic derivative can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition and application of the compound and the pharmaceutical composition in preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.

Potent, selective, and orally active adenosine A2A receptor antagonists: Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines

Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A2A antagonist SCH 58261 as a starting point, we identified the potent and selective (vs. A1) antagonist 11 h, orally active in the rat haloperidol-induced catalepsy model. We further optimized this lead to the methoxyethoxyethyl ether 12a (SCH 420814), which shows broad selectivity, good pharmacokinetic properties, and excellent in vivo activity.