Composiciones y métodos para activar "estimulador de interferon gene" - señalización dependientes

• Main Authors: LEONG MEREDITH LAI LING, VANCE RUSSELL E, LEMMENS EDWARD EMILE, GLICKMAN LAURA HIX, KANNE DAVID B, DUBENSKY THOMAS W., JR
• Format: Patent
• Language: Spanish
• Published: 30.12.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

COMPOSICIÓN QUE COMPRENDE UNO O MÁS DINUCLEÓTIDOS DE PURINA CÍCLICOS; USO DE LA COMPOSICIÓN PARA INDUCIR RESPUESTA INMUNE EN UN SUJETO; USO PARA INDUCIR LA PRODUCCIÓN DE INTERFERÓN DEL TIPO I QUE DEPENDE DE STING; Y USO PARA TRATAR CÁNCER. The invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate dentritic cells via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the CDNs of the invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides that induce STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are substantially pure 2',5',3',5' CDNs, and preferably Rp,Rp stereoisomers.linked towherein R3 is a bond to the 5' carbon of (b), R4 is a bond to the 3' carbon of (b), R1 is a purine linked through its N9 nitrogen to the ribose ring of (a), R5 is a purine linked through its N9 nitrogen to the ribose ring of (b), each of X1 and X2 are S, and the 2' carbon of (b) is -O-R6.