Substituted pyrimidines as toll-like receptor modulators

• US 9,284,304 B2
• Filed: 08/09/2013
• Issued: 03/15/2016
• Est. Priority Date: 08/10/2012
• Status: Active Grant

• Current Assignee: Janssen Sciences Ireland UC (Johnson & Johnson)
• Original Assignee: Janssen Sciences Ireland UC (Johnson & Johnson)
• Inventors: McGowan, David Craig, Jonckers, Tim Hugo Maria, Raboisson, Pierre Jean-Marie Bernard
• Primary Examiner(s): Willis, Douglas M
• Application Number:
  US14/420,066
• Publication Number:
  US 20150239872A1
• Time in Patent Office: 949 Days
• Field of Search: 514/275, 544/323, 546/181, 546/268.1, 549/59
• US Class Current: 1/1
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 239/48 Two nitrogen atoms
• CPC Class Codes: C07D 239/49 with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
• CPC Class Codes: C07D 401/06 linked by a carbon chain containing only aliphatic carbon atoms
• CPC Class Codes: C07D 409/06 linked by a carbon chain containing only aliphatic carbon atoms

Abstract

This invention relates to alkylpyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.

Claims

1. A compound of formula (I)

3. The compound as claimed in claim 1, wherein

R₁ is hydrogen, and

R₂ is optionally substituted by one or more substituents independently selected from halo, hydroxy, amino, cyano, carboxy, carboxy ester, amido, C_1-3 alkyl, C_1-3 alkoxy, or C_3-6 cycloalkyl.

4. A pharmaceutical composition comprising a compound as claimed in claim 1 or a pharmaceutically acceptable salt thereof together with one or more pharmaceutically acceptable excipients, diluents or carriers.

5. A method for modulating toll-like receptor 7 activity and/or toll-like receptor 8 activity in a human, comprising administering to said human a therapeutically effective amount of at least one compound as claimed in claim 1.

2. A compound of formula (I)

6. A compound selected from the group consisting of: