1029-52-3Relevant articles and documents
Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists
McGowan, David C.,Herschke, Florence,Khamlichi, Mourad D.,Rosauro, Mari Luz,Benedicto, Sara M. Pérez,Pauwels, Frederik,Stoops, Bart,Pande, Vineet,Scholliers, Annick,Van Schoubroeck, Bertrand,Mostmans, Wendy,Van Dijck, Kris,Thoné, Tine,Horton, Helen,Fanning, Gregory,Jonckers, Tim H.M.,Raboisson, Pierre
supporting information, p. 3216 - 3221 (2018/08/24)
In a continuing effort to discover novel TLR agonists, herein we report on the discovery and structure–activity relationship of novel tetrahydropyridopyrimidine TLR 7/8 agonists. Optimization of this series towards dual agonist activity and a high clearance profile resulted in the identification of compound 52a1. Evaluation in vivo revealed an interferon stimulated response (ISG) in mice with limited systemic exposure and demonstrated the potential in antiviral treatment or as a vaccine adjuvant.
PIPERIDINO-PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
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Page/Page column 10, (2013/08/28)
This invention relates to piperidino-pyhmidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
2-Amino-6-iodo-4-tosyloxypyrimidine: a versatile key intermediate for regioselective functionalization of 2-aminopyrimidines in 4- and 6-positions
Benderitter, Pascal,de Araújo Júnior, Jo?o Xavier,Schmitt, Martine,Bourguignon, Jean-Jacques
, p. 12465 - 12470 (2008/03/13)
2-Amino-6-iodo-4-tosyloxypyrimidine, easily prepared from commercially available material, is a key intermediate for the preparation of differentially substituted 2-aminopyrimidines by means of sequenced Suzuki and/or Sonogashira reactions.