# US 10,117,873 B2 · 6-amino-purin-8-one compounds

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- Number: US 10,117,873 B2
- Document ID: US10117873B2
- Status: Granted
- Kind: B2
- Application number: 15/846,475
- Filed: 2017-12-19
- Published: 2018-05-03
- Granted: 2018-11-06
- Earliest claimed: 2008-08-11
- Assignees: GlaxoSmithKline LLC
- Applicants: GlaxoSmithKline LLC
- Inventors: Keith Biggadike; Diane Mary Coe; Xiao Qing Lewell; Charlotte Jane Mitchell; Stephen Allan Smith; Naimisha Trivedi
- Web page: https://patentgrep.com/patent/US10117873B2

## CPC

- A61K 31/522: having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
- A61K 9/0043: {Nose}
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- C07D 473/16: two nitrogen atoms
- C07D 473/18: one oxygen and one nitrogen atom, e.g. guanine
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

## Claims

### Claim 1

A method of treating or preventing a vaccine-treatable or vaccine-preventable disease in a human subject suffering from or susceptible to said disease, the method comprising administering to the human a vaccine composition comprising an antigen or antigen composition, and administering to the human a compound of formula (I):
wherein:
R1 is (1S)-1-methylbutyloxy;
m is an integer having a value of 4 to 6;
n is an integer having a value of 2 to 4;
or a salt thereof.

### Claim 2 (depends on 1)

The method according to claim 1 wherein the compound is selected from the group consisting of:
6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[4-(1-piperidinyl)butyl]-7,9-dihydro-8H-purin-8-one;
6-amino-9-[4-(hexahydro-1H-azepin-1-yl)butyl]-2-{[(1S)-1-methylbutyl]oxy}-7,9-dihydro-8H-purin-8-one;
6-amino-9-[5-(hexahydro-1H-azepin-1-yl)pentyl]-2-{[(1S)-1-methylbutyl]oxy}-7,9-dihydro-8H-purin-8-one; and
6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one.

### Claim 3 (depends on 1)

The method according to claim 1 wherein the salt is a pharmaceutically acceptable salt.

### Claim 4 (depends on 1)

The method according to claim 1 wherein the compound is a free base.

### Claim 5

A method of treating or preventing a vaccine-treatable or vaccine-preventable disease in a human subject suffering from or susceptible to said disease, the method comprising administering to the human a vaccine composition comprising an antigen or antigen composition, and administering to the human 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one, or a salt thereof.

### Claim 6 (depends on 5)

The method according to claim 5 wherein the salt is a pharmaceutically acceptable salt.

### Claim 7 (depends on 5)

The method according to claim 5 wherein the compound is a free base.