ACYLAMINOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES

• US 20150274676A1
• Filed: 10/03/2013
• Published: 10/01/2015
• Est. Priority Date: 10/05/2012
• Status: Active Grant

• Current Assignee: Janssen Sciences Ireland UC (Johnson & Johnson)
• Original Assignee: Janssen Sciences Ireland UC (Johnson & Johnson)
• Inventors: Mc Gowan, David Craig, Embrechts, Werner, Last, Stefaan Julien, Jonckers, Tim Hugo Maria, Raboisson, Pierre Jean-Marie Bernard, Pieters, Serge Marie Aloysius
• Granted Patent: US 9,790,191 B2
• Time in Patent Office: Days
• US Class Current: 1/1
• 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 213/75 Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• CPC Class Codes: C07D 239/47 One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
• CPC Class Codes: C07D 239/48 Two nitrogen atoms

Abstract

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

Claims

1. A compound of formula (I)

2. A compound as claimed in claim 1 wherein R_1A is substituted or unsubstituted acyl, R₂ is C_1-6 alkyl and R₃ is C_1-8 alkyl substituted with an alkylester.

3. A compound as claimed in claim 1 wherein R_1A is isobutyryl, R₂ is —

CH₃, and R₃ is heptan-3-yl isobutyrate.

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

7. A method of treating a disorder in which the induction of interferon is involved, comprising the administration of a therapeutically effective amount of at least one compound as claimed in claim 1.

8. A compound as claimed in claim 1 wherein R_1B is substituted or unsubstituted acyl, R₂ is C_1-6 alkyl and R₃ is C_1-8 alkyl substituted with an alkylester.

9. A compound as claimed in claim 1 wherein R_1A and R_1B are substituted or unsubstituted acyl, R₂ is C_1-6 alkyl and R₃ is C_1-8 alkyl substituted with an alkylester.

10. A compound as claimed in claim 1 wherein R_1A is substituted or unsubstituted acyl, R₂ is —

CH₃ and R₃ is C_1-8 alkyl substituted with an alkylester.

11. A compound as claimed in claim 1 wherein R_1B is substituted or unsubstituted acyl, R₂ is —

CH₃ and R₃ is C_1-8 alkyl substituted with an alkylester.

12. A compound as claimed in claim 1 wherein R_1A and R_1B are substituted or unsubstituted acyl, R₂ is —

CH₃ and R₃ is C_1-8 alkyl substituted with an alkylester.

13. A compound as claimed in claim 1 wherein R_1B is isobutyryl, R₂ is —

CH₃, and R₃ is heptan-3-yl isobutyrate.

14. A compound as claimed in claim 1 wherein R_1A and R_1B are isobutyryl, R₂ is —

CH₃, and R₃ is heptan-3-yl isobutyrate.

4. (canceled)

6. (canceled)