08-03-2018 дата публикации
Номер: US20180064745A1
The present invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes), In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides induce human STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are 2′-fluoro substituted, bis-3′,5′CDNs, and most preferably one or more 2′,2″-diF-Rp,Rp, bis-3′,5′CDNs. 4. The compound according to claim 3 , wherein R21 and R22 are both adenine.5. The compound according to claim 3 , wherein R21 is adenine and R22 is guanine.8. The compound according to claim 1 , wherein the compound is the sodium claim 1 , potassium claim 1 , calcium claim 1 , magnesium claim 1 , zinc claim 1 , aluminum claim 1 , ammonium claim 1 , diethylamine claim 1 , olamine claim 1 , benzathine claim 1 , benethamine claim 1 , tromethamine (2-amino-2-(hydroxymethyl)propane-1 claim 1 ,3-diol) claim 1 , morpholine claim 1 , epolamine claim 1 , piperidine claim 1 , picoline claim 1 , dicyclohexylamine claim 1 , N claim 1 ,N′-dibenzylethylenediamine claim 1 , 2-hydroxyethylamine claim 1 , tri-(2-hydroxyethyl)amine claim 1 , chloroprocaine claim 1 , choline claim 1 , deanol claim 1 , imidazole claim 1 , diethanolamine claim 1 , ethylenediamine claim 1 , meglumine (N-methylglucamine) claim 1 , procaine claim 1 , dibenzylpiperidine claim 1 , dehydroabietylamine claim 1 , glucamine claim 1 , collidine claim 1 , quinine claim 1 , quinolone claim 1 , erbumine claim 1 , lysine or arginine salt thereof.9. The compound according to claim 1 , wherein the compound is the sodium salt thereof.10. A pharmaceutical composition comprising one or more compounds according to and a pharmaceutically acceptable excipient.11. A pharmaceutical composition comprising one or more compounds according to claim 1 , another ...
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