162401-16-3

Upstream product

• 162401-15-2 5-amino-7-tert-butyl-2-(2-furyl)-pyrazolo[4,3-e]-1,2,4 triazolo-[1,5-c]pyrimidine 
• 3326-71-4 2-furoic acid hydrazide 
• 5604-46-6 2-amino-4,6-dichloropyrimidine-5-carboxaldehyde 
• 377729-80-1 furan-2-carboxylic acid N-(2-amino-6-chloro-5-formylpyrimidin-4-yl)-hydrazide 
• 377729-81-2 furan-2-carboxylic acid N-(6-amino-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-hydrazide 
• 1027398-48-6 Furan-2-carboxylic acid (1-tert-butyl-4-imino-1,4-dihydro-pyrazolo[3,4-d]pyrimidin-5-yl)-amide 
• 174648-59-0 7-tert-butyl-2-(2-furyl)pyrazolo<4,3-e>-1,2,4-triazolo<1,5-c>pyrimidine 
• 174648-67-0 5-amino-1-tert-butyl-4-<3-(2-furyl)-1,2,4-triazol-5-yl>pyrazole 

Downstream Products

• 396124-18-8 2-furan-2-yl-7-[3-(4-nitro-phenyl)-propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-ylamine 
• 396124-19-9 N-{4-[2-(5-amino-2-furan-2-yl-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-7-yl)-ethyl]-phenyl}-acetamide 
• 396124-24-6 {4-[2-(5-amino-2-furan-2-yl-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-7-yl)-ethyl]-phenoxy}-acetic acid ethyl ester 
• 646511-92-4 [2-furan-2-yl-5-(3-phenyl-ureido)-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-8-yl]-acetic acid tert-butyl ester 
• 377729-44-7 C₂₅H₂₁N₇O₂ 
• 377729-47-0 C₂₅H₁₈F₃N₇O₂ 
• 377729-42-5 C₂₃H₁₈N₈O 
• 377729-48-1 C₂₄H₂₀N₈O₂ 
• 1052713-93-5 C₂₄H₂₀N₈O 
• 377729-53-8 C₂₂H₁₇N₉O 
• 377729-51-6 C₂₃H₁₈N₈O 
• 377729-50-5 C₂₄H₁₉N₇O 
• 897025-47-7 8-(3-benzyloxypropyl)-2-(furan-2-yl)-8H-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidin-5-ylamine 

Relevant academic research and scientific papers

Heterobivalent Ligand for the Adenosine A2A-Dopamine D2Receptor Heteromer

A G protein-coupled receptor heteromer that fulfills the established criteria for its existence in vivo is the complex between adenosine A2A (A2AR) and dopamine D2 (D2R) receptors. Here, we have designed and synthesized heterobivalent ligands for the A2AR

PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST

Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.

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.

Nitrogen-containing fused tricyclic derivatives 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.

PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST

Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as an A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as an A2A receptor antagonist.

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.

Adenosine A3 receptor modulators

The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceu

Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists

Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.

New strategies for the synthesis of A3 adenosine receptor antagonists

New A3 adenosine receptor antagonists were synthesized and tested at human adenosine receptor subtypes. An advanced synthetic strategy permitted us to obtain a large amount of the key intermediate 5 that was then submitted to alkylation procedures in order to obtain the derivatives 6-8. These compounds were then functionalised into ureas at the 5-position (compounds 9-11, 18 and 19) to evaluate their affinity and selectivity versus hA3 adenosine receptor subtype; in particular, compounds 18 and 19 displayed a value of affinity of 4.9 and 1.3 nM, respectively. Starting from 5, the synthetic methodologies employed permitted us to perform a rapid and a convenient divergent synthesis. A further improvement allowed the regioselective preparation of the N8-substituted compound 7. This method could be used as an helpful general procedure for the design of novel A3 adenosine receptor antagonists without the difficulty of separating the N8-substituted pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines from the corresponding N 7-isomers.

Adenosine A3 receptor modulators

The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceu