960116-30-7

Upstream product

• 6863-73-6 3-chloropyrazin-2-amine 
• 937-20-2 p-chlorophenacyl chloride 
• 536-38-9 4-chlorobenzoylmethyl bromide 

Downstream Products

• 960116-31-8 C₂₂H₂₆ClN₅O₂ 
• 1169426-29-2 C₁₈H₁₃ClN₆O 
• 1169426-33-8 C₁₈H₁₉ClN₆O 
• 1432446-39-3 C₁₇H₁₁ClIN₅ 
• 1432446-40-6 C₁₇H₁₇ClIN₅ 
• 1432446-41-7 C₁₅H₁₅ClIN₅ 
• 1169426-39-4 C₁₆H₁₇ClN₆O 
• 1432446-48-4 C₁₈H₁₁ClN₆ 
• 1169426-93-0 C₁₈H₁₇ClN₆ 
• 1432446-49-5 C₁₆H₁₅ClN₆ 
• 1432446-30-4 C₁₇H₁₂ClN₅ 
• 1432446-31-5 C₁₇H₁₈ClN₅ 
• 1432446-32-6 C₁₅H₁₆ClN₅ 

Relevant academic research and scientific papers

Discovery of Imidazo[1,2- a]pyrazines and Pyrazolo[1,5- c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators

This report discloses the discovery and characterization of imidazo[1,2-a]pyrazines and pyrazolo[1,5-c]pyrimidines as selective negative modulators of α-amino-3-hydroxy-5-methylisoxazole-4-propionate receptors (AMPARs) associated with transmembrane AMPAR regulatory protein γ-8. Imidazopyrazine 5 was initially identified as a promising γ-8 selective high-throughput screening hit, and subsequent structure-activity relationship optimization yielded subnanomolar, brain penetrant leads. Replacement of the imidazopyrazine core with an isosteric pyrazolopyrimidine scaffold improved microsomal stability and efflux liabilities to provide 26, JNJ-61432059. Following oral administration, 26 exhibited time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, which resulted in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.

Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors

Chemistry has been developed to access both imidazo[1,2-a]pyrazines and imidazo[1,2-c]pyrimidines. Small structural modifications in both series led to a switch of potency between two kinases involved in mediating cell cycle checkpoint control, CHK1 and MK2.

IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS

In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds of formula (I) as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.