QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES

• US 20140073642A1
• Filed: 05/18/2012
• Published: 03/13/2014
• Est. Priority Date: 05/18/2011
• Status: Active Grant

• Current Assignee: Janssen Sciences Ireland UC (Johnson & Johnson)
• Original Assignee: Janssen R&D Ireland (Johnson & Johnson)
• Inventors: McGowan, David, Raboisson, Pierre Jean-Marie Bernard, Jonckers, Tim Hugo Maria, Last, Stefaan Julien, Embrechts, Werner, Pieters, Serge Maria Aloysius
• Granted Patent: US 8,916,575 B2
• Time in Patent Office: Days
• US Class Current: 514/234.5
• 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 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 239/95 with hetero atoms directly attached in positions 2 and 4
• CPC Class Codes: C07D 295/192 from aromatic carboxylic acids
• CPC Class Codes: C07D 401/06 linked by a carbon chain containing only aliphatic carbon atoms
• CPC Class Codes: C07D 403/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 491/056 with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Abstract

This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.

Claims

1. A compound of formula (I)

2. A compound of formula (I) according to claim 1 wherein R₁ is butyl, pentyl or 2-pentyl and wherein R₂, R₃, R₄ and R₅ are as specified above.

3. A compound of formula (I) according to claim 1 wherein R₁ is C_4-8alkyl substituted with a hydroxyl, and wherein R₂, R₃, R₄ and R₅ are as specified above.

4. A compound of formula (I) according to claim 3 wherein R₁, when being C_4-8alkyl substituted with hydroxyl, is one of the following:

5. A compound of formula (I) according to claim 1 wherein R₅ is preferably hydrogen or fluorine and R₁, R₂, R₃, and R₄ are as described above.

6. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt, solvate or polymorph thereof and one or more pharmaceutically acceptable excipients, diluents or carriers.

8. A method for the treatment of a subject having a disorder in which the modulation of TLR7 and/or TLR8 is involved, said method comprising administration of a compound claim 1 or a pharmaceutically acceptable salt, solvate or polymorph thereof, or a pharmaceutical composition according to claim 6 to the subject.

9. A compound of claim 1 having a structure shown in Table 1, or a pharmaceutically acceptable salt, solvate or polymorph thereof.

10. A compound of claim 1 having the structure:

7. (canceled)