200292-54-2

Upstream product

• 539-82-2 ethyl n-valerate 
• 60598-48-3 5-amino-1-benzyl-1H-imidazole-4-carbonitrile 
• 640274-67-5 9-benzyl-2-butylhypoxanthine 
• 3815-69-8 5-amino-1-(phenylmethyl)-1H-imidazole-4-carboxamide 
• 870656-49-8 9-benzyl-2-butyl-6-chloropurine 

Downstream Products

• 200291-67-4 N-(9-benzyl-2-n-butyl-9H-purin-6-yl)-N-(3,4,5-trimethoxybenzoyl)-3,4,5-trimethoxybenzamide 
• 640274-68-6 9-benzyl-8-bromo-2-butyladenine 

Relevant academic research and scientific papers

Synthesis and structure-activity relationships of 2-substituted-8-hydroxyadenine derivatives as orally available interferon inducers without emetic side effects

Recently we reported the adenine derivatives (2-4) as new interferon (IFN) inducers. In the present study, we conducted a detailed structure and activity relationship study of 4 and its related derivatives on IFN inducing activity. From this study, we found that compound 4 exhibited the most potent IFN inducing activity in vitro with a minimum effective concentration of 0.01 μM, and 4 also showed strong IFN-inducing activity at doses of more than 0.3 mg/kg by oral administration in mice. This potency was 10-fold stronger than that of Imiquimod. Moreover, 4 did not cause emesis in ferrets even at doses as high as 10 mg/kg, whereas, 80% of animals were emetic when orally administered with the same dose of Imiquimod. These results indicate that compound 4 is superior to Imiquimod with respect to efficacy and safety.

Amide derivatives

PCT No. PCT/JP97/01875 Sec. 371 Date Dec. 2, 1998 Sec. 102(e) Date Dec. 2, 1998 PCT Filed Jun. 2, 1997 PCT Pub. No. WO97/46560 PCT Pub. Date Nov. 12, 1997The invention provides amide derivatives which are useful as analgesics, anti-inflammatory agents, an