# US 2017/0283454 A1 · Compositions comprising cyclic purine dinucleotides having defined stereochemistries and methods for their preparation and use

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- Number: US 2017/0283454 A1
- Document ID: US20170283454A1
- Status: Published application
- Kind: A1
- Application number: 15/630,741
- Filed: 2017-06-22
- Published: 2017-10-05
- Earliest claimed: 2012-12-13
- Assignees: Aduro Biotech, Inc.
- Applicants: Aduro Biotech, Inc.
- Inventors: Thomas W. Dubensky, JR.; David B. Kanne; Meredith Lai Ling Leong; Edward Emile Lemmens; Laura Hix Glickman
- Web page: https://patentgrep.com/patent/US20170283454A1

## CPC

- C07H 21/02: with ribosyl as saccharide radical
- A61K 31/7084: Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
- A61K 39/0005: {Vertebrate antigens (from snakes A61K39/38)}
- A61K 39/02: Bacterial antigens
- A61K 39/12: Viral antigens
- A61K 39/385: Haptens or antigens, bound to carriers
- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/04: Immunostimulants
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07H 19/213: containing cyclic phosphate
- C07H 21/00: Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
- C07H 21/04: with deoxyribosyl as saccharide radical
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

It is an object of the present invention to provide novel and highly active cyclic-di-nucleotide (CDN) immune stimulators that activates 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 that induce STING-dependent TBK1 activation, wherein the cyclic purine dinuclotides present in the composition are substantially pure Rp,Rp or Rp,Sp stereoisomers, and particularly substantially pure Rp,Rp, or RpSp CDN thiophosphate diastereomers.

## Claims

### Claim 1

A composition comprising:
one or more cyclic purine dinucleotides or prodrugs or pharmaceutically acceptable salts thereof which induce STING-dependent TBK1 activation, wherein the cyclic purine dinuclotides present in the composition are substantially pure Rp,Rp or Rp,Sp diastereomers, or prodrugs or pharmaceutically acceptable salts thereof, wherein said cyclic purine dinucleotides are preferably thiophposphate cyclic purine dinucleotides.