2-aminopyrimidine derivatives for the treatment of viral infections

Patent metadata

Field	Value
Publication number	US-9598378-B2
Application number	US-201414769773-A
Country	US
Kind code	B2
Filing date	Feb 20, 2014
Priority date	Feb 21, 2013
Publication date	Mar 21, 2017
Grant date	Mar 21, 2017

Abstract

This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

First claim

The invention claimed is:

1. A compound of formula (I)

or a pharmaceutically acceptable salt, tautomer(s), stereo-isomeric forms, or solvate thereof, wherein
X represents S, S═O or O═S═O;
R 1 is hydrogen, (C 1-6 )-alkyl, (C 1-6 )-alkoxy or aryl;
R 2 is (C 1-3 )-alkyl or (C 3-6 -cycloalkyl; and
n=1 or 2.

2. A pharmaceutical composition comprising a compound of claim 1 together with one or more pharmaceutically acceptable excipients, diluents or carriers.

3. A method of activating TLR7 and/or TLR8 to induce interferon-stimulated response elements in a subject in need thereof comprising administering to said subject at least one compound of claim 1 .

4. The compound of claim 1 , wherein
R 1 is hydrogen;
R 2 is methyl; and
n is 1.

5. The compound of claim 4 , wherein
X is S.

6. The compound of claim 4 , wherein
X is S═O.

7. The compound of claim 4 , wherein
X is O═S═O.

8. A compound selected from the group consisting of

Assignees

• Janssen Sciences Ireland Uc

Inventors

• Mcgowan David Craig
• Raboisson Pierre Jean-Marie Bernard
• Jonckers Tim Hugo Maria

Classifications

• A61P37/02

  Immunomodulators · CPC title

• A61P31/12

  Antivirals · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61K31/505

  Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim · CPC title

• C07D239/47 Primary

  One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine · CPC title