1228588-20-2

Upstream product

• 1228588-19-9 ethyl-Nβ-[3-(pyrroldin-1′-ylmethyl)-benzyl]-β-alaninoate 
• 38136-96-8 6-chloro-2-(methylsulfanyl)-5-nitropyrimidin-4-amine 
• 884507-42-0 3-(pyrrolidin-1′-ylmethyl)-benzaldehyde 
• 1979-96-0 4,6-dichloro-2-(methylthio)-5-nitropyrimidine 
• 4244-84-2 ethyl β-alaninate hydrochloride 

Downstream Products

• 1228588-21-3 C₂₂H₃₀N₆O₆S 
• 1228588-22-4 ethyl-Nβ-[4-amino-2-n-butoxy-5-nitropyrimidin-6-yl],Nβ-[3′-(pyrrolidin-1″-ylmethyl)-benzyl]-β-alaninoate 
• 1228585-89-4 4-amino-2-n-butylamino-[9H]-9-[3′-(pyrrolidin-1′′-ylmethyl)-benzyl] pyrimido[6,5:b]-5,6,7,8-tetrahydro[1,4]diazepin-6-one 

Relevant academic research and scientific papers

Identification and optimization of pteridinone toll-like receptor 7 (TLR7) agonists for the oral treatment of viral hepatitis

Pteridinone-based Toll-like receptor 7 (TLR7) agonists were identified as potent and selective alternatives to the previously reported adenine-based agonists, leading to the discovery of GS-9620. Analogues were optimized for the immunomodulatory activity and selectivity versus other TLRs, based on differential induction of key cytokines including interferon α (IFN-α) and tumor necrosis factor α (TNF-α). In addition, physicochemical properties were adjusted to achieve desirable in vivo pharmacokinetic and pharmacodynamic properties. GS-9620 is currently in clinical evaluation for the treatment of chronic hepatitis B (HBV) infection.

MODULATORS OF TOLL-LIKE RECEPTORS

Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.