170871-87-1

Upstream product

• 40615-36-9 4,4'-dimethoxytrityl chloride 
• 129054-67-7 N-(9-((2R,3S,4S,5R)-4-fluoro-3-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-yl)benzamide 
• 1101107-81-6 (3S,4S,5R)-5-((benzyloxy)methyl)-4-fluoro-2-methoxytetrahydrofuran-3-ol 
• 1009818-08-9 (2R,3R,4R)-2-((benzyloxy)methyl)-5-methoxytetrahydrofuran-3,4-diol 
• 230632-62-9 ((2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-(benzoyloxy)-3-fluorotetrahydrofuran-2-yl)methyl benzoate 
• 123484-12-8 ((2R,3R,4S)-5-acetoxy-4-(benzoyloxy)-3-fluorotetrahydrofuran-2-yl)methyl benzoate 
• 1005482-73-4 (2R,3R,4R,5R)-5-(6-benzamido-9H-purin-9-yl)-2-((bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-4-((tert-butyldimethylsilyl)oxy)tetrahydrofuran-3-yl trifluoromethane-sulfonate 
• 129681-71-6 5'-O-dimethoxytrityl-2'-O-tert-butyldimethylsilyl-N₆-benzoyl adenosine 
• 222725-68-0 N-(9-((2R,3R,4S,5R)-5-((bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-3-((tert-butyldimethylsilyl)oxy)-4-hydroxytetrahydrofuran-2-yl)-9H-purin-6-yl)benzamide 
• 98-88-4 benzoyl chloride 
• 75059-22-2 (2R,3S,4S,5R)-2-(6-amino-9H-purine-9-yl)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-3-ol 

Relevant academic research and scientific papers

Bis 2′-5′-RR-(3′F-A)(3′F-A) cyclic dinucleotide compound and uses thereof

The present invention provides the cyclic dinucleotide compound 2′2′-RR-(3′F-A)(3′F-A) as a highly active immune stimulator that activates DCs via the cytoplasmic receptor known as STING (Stimulator of Interferon Genes), and compositions and uses thereof.

COMPOUNDS, COMPOSITIONS, AND METHODS FOR THE TREATMENT OF DISEASE

Disclosed are compounds and compositions for the activation or induction of expression of a pattern recognition receptor (e.g., STING, RIG-I, MDA5), and methods of use thereof.

NOVEL STING AGONISTS

The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z1, Z2, R1, R2, R3, R4 and R5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

DC-SIGN ANTIBODY CONJUGATES COMPRISING STING AGONISTS

Provided herein are immunoconjugates comprising an anti-DC-SiGN antibody conjugated to a STING agonist. Also disclosed are methods of making the immunoconjugates and methods of treating cancer using the immunoconjugates.

CYCLIC DINUCLEOTIDES AS STING AGONISTS

Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein B2,X2, R2a, R2b, R2c, Z-M-Y, Y1-M1Z1, B1, X1, R1a, R1b, R1c are as defined herein.

LOCKED NUCLEIC ACID CYCLIC DINUCLEOTIDE COMPOUNDS AND USES THEREOF

The present invention provides highly active locked nucleic acid cyclic-dinucleotide (LNA-CDN) immune stimulators that activate DCs via the cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the LNA-CDNs of the present in

COMPOSITIONS AND METHODS FOR ACTIVATING "STIMULATOR OF INTERFERON GENE"-DEPENDENT SIGNALLING

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 dinuclotides present in the composition are 2'- or 3'-mono-fluoro substituted, or 2'3'-di-fluoro substituted mixed linkage 2',5' - 3',5' CDNs.

Solid phase synthesis of 2',5'-oligoadenylates containing 3'-fluorinated ribose

2',5'-phosphodiester bond-linked oligoadenylate trimers with 3'-fluoro- 3'-deoxyadenosine residues incorporated at specific positions of the nucleotide sequence were synthesized by the solid phase phosphite triester (phosphoramidite) method. The syntheses were in the 2' to 5' direction and were performed manually using commercially available microcolumns. The oligonucleotides were 5'-end phosphorylated on the support before deprotection.