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Last Updated: March 28, 2024

Details for Patent: 8,841,310


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Title:Combinations of a pyrimidine containing NNRTI with RT inhibitors
Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
Inventor(s): Stoffels; Paul (Hoogstraten, BE)
Assignee: Janssen R & D Ireland (Eastgate Village, Eastgate Little Island, Co. Cork, IE)
Filing Date:Oct 07, 2009
Application Number:12/574,881
Claims:1. A combination comprising (i) 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile, or a stereoisomeric form thereof; or a pharmaceutically acceptable salt thereof, and (ii) tenofovir or its prodrug tenofovir disoproxil fumarate, and (iii) emtricitabine; wherein the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile, or a stereoisomeric form thereof; or a pharmaceutically acceptable salt thereof; the tenofovir or its prodrug tenofovir disoproxil fumarate; and the emtricitabine are therapeutically effective HIV inhibitors at a dose that can be administered once daily.

2. The combination according to claim 1, wherein the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile, or a stereoisomeric form thereof; or a pharmaceutically acceptable salt thereof, is E-4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-am- ino]-benzonitrile.

3. The combination of claim 1, wherein the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile, or a stereoisomeric form thereof; or a pharmaceutically acceptable salt thereof, is E-4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-am- ino]-benzonitrile hydrochloride.

4. The combination of claim 1, wherein the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile, or a stereoisomeric form thereof; or a pharmaceutically acceptable salt thereof, is 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile hydrochloride.

5. The combination of claim 1, comprising tenofovir disoproxil fumarate.

6. The combination of claim 3, comprising tenofovir disoproxil fumarate.

7. The combination of claim 1 comprising between 10 mg and 500 mg of the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile or a stereoisomeric form thereof.

8. The combination of claim 1 comprising between 10 mg and 300 mg of the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile or a stereoisomeric form thereof.

9. The combination of claim 1 comprising about 25 mg of the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile or a stereoisomeric form thereof.

10. The combination of claim 1, wherein the 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amin- o]-benzonitrile, or a stereoisomeric form thereof; or a pharmaceutically acceptable salt thereof, tenofovir or its prodrug tenofovir disoproxil fumarate; and emtricitabine are together in a unitary pharmaceutically acceptable formulation.

11. The combination of claim 10, wherein the pharmaceutically acceptable formulation is selected from the group consisting of tablets, capsules, parenteral compositions, injectable solutions, and injectable suspensions.

12. The combination of claim 11, wherein the pharmaceutically acceptable formulation is a tablet.

13. The combination of claim 3, wherein the E-4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-am- ino]-benzonitrile hydrochloride, tenofovir or its prodrug tenofovir disoproxil fumarate, and emtricitabine are together in a unitary pharmaceutically acceptable formulation.

14. The combination of claim 13, wherein the pharmaceutically acceptable formulation is a tablet.

15. The combination of claim 6, wherein the E-4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-am- ino]-benzonitrile hydrochloride, tenofovir disoproxil fumarate, and emtricitabine are together in a unitary pharmaceutically acceptable formulation.

16. The combination of claim 15, wherein the pharmaceutically acceptable formulation is a tablet.

17. A method of treating HIV infection in a patient comprising administering to the patient the combination of claim 1 once daily.

18. A method of treating HIV infection in a patient comprising administering to the patient the combination of claim 10 once daily.

19. A method of treating HIV infection in a patient comprising administering to the patient the combination of claim 15 once daily.

20. A method of treating HIV infection in a patient comprising administering to the patient the combination of claim 16 once daily.

21. A pharmaceutical formulation comprising the combination of claim 1 and a pharmaceutically acceptable carrier.

22. The pharmaceutical formulation of claim 21, wherein the formulation is selected from the group consisting of tablets, capsules, parenteral compositions, injectable solutions, and injectable suspension.

23. The pharmaceutical formulation of claim 22, wherein the formulation is a tablet.

24. A pharmaceutical formulation comprising the combination of claim 3 and a pharmaceutically acceptable carrier.

25. The pharmaceutical formulation of claim 24, wherein the formulation is a tablet.

26. A pharmaceutical formulation comprising the combination of claim 6 and a pharmaceutically acceptable carrier.

27. The pharmaceutical formulation of claim 26, wherein the formulation is a tablet.

28. A method of treating HIV infection in a patient comprising administering to the patient the pharmaceutical formulation of claim 21 once daily.

29. A method of treating HIV infection in a patient comprising administering to the patient the pharmaceutical formulation of claim 26 once daily.

30. A method of treating HIV infection in a patient comprising administering to the patient the pharmaceutical formulation of claim 27 once daily.

31. A kit comprising the combination of claim 1 packaged with instructions for use.

32. A kit comprising the combination of claim 3 packaged with instructions for use.

33. A kit comprising the combination of claim 6 packaged with instructions for use.

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