Methods for the treatment and prophylaxis of HIV and AIDS
The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
1. A method for the prophylaxis of HIV infection in a subject which comprises orally administering to the subject an effective amount of a compound of structural formula:
or a pharmaceutically acceptable salt thereof, wherein the dosing regimen is once-weekly, and the dosage amount is from 1 mg to 20 mg at each administration.
2. The method of claim 1 wherein the subject is human.
3. The method of claim 2 wherein the HIV is HIV-1.
4. The method of claim 3 wherein the compound is
5. A method for the prophylaxis of HIV infection in a subject which comprises orally administering to the subject an effective amount of a compound of structural formula:
or a pharmaceutically acceptable salt thereof, wherein the dosing regimen is once-weekly, and the dosage amount is 1 mg, 2 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 9 mg or 10 mg at each administration.
6. The method of claim 5 wherein the subject is human.
7. The method of claim 6 wherein the HIV is HIV-1.
8. The method of claim 7 wherein the compound is
9. A method for the prophylaxis of HIV infection in a subject which comprises orally administering to the subject an effective amount of a compound of structural formula:
or a pharmaceutically acceptable salt thereof, wherein the dosing regimen is bi-weekly or twice monthly, and the dosage amount is from 2 mg to 40 mg at each administration.
10. The method of claim 9 wherein the subject is human.
11. The method of claim 10 wherein the HIV is HIV-1.
12. The method of claim 11 wherein the compound is
13. A method for the prophylaxis of HIV infection in a subject which comprises orally administering to the subject an effective amount of a compound of structural formula:
or a pharmaceutically acceptable salt thereof, wherein the dosing regimen is bi-weekly or twice monthly, and the dosage amount is 2 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 9 mg, 10 mg, 11 mg, 12 mg, 13 mg, 14 mg, 15 mg, 16 mg, 17 mg, 18 mg, 19 mg or 20 mg at each administration.
14. The method of claim 13 wherein the subject is human.
15. The method of claim 14 wherein the HIV is HIV-1.
16. The method of claim 15 wherein the compound is
17. A method for the prophylaxis of HIV infection in a subject which comprises orally administering to the subject an effective amount of a compound of structural formula:
or a pharmaceutically acceptable salt thereof, wherein the dosing regimen is once-monthly, and the dosage amount is from 4 mg to 80 mg at each administration.
18. The method of claim 17 wherein the subject is human.
19. The method of claim 18 wherein the HIV is HIV-1.
20. The method of claim 19 wherein the compound is
21. A method for the prophylaxis of HIV infection in a subject which comprises orally administering to the subject an effective amount of a compound of structural formula:
or a pharmaceutically acceptable salt thereof, wherein the dosing regimen is once-monthly and the dosage amount is 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 9 mg, 10 mg, 11 mg, 12 mg, 13 mg, 14 mg, 15 mg, 16 mg, 17 mg, 18 mg, 19 mg, 20 mg, 21 mg, 22 mg, 23 mg, 24 mg, 25 mg, 26 mg, 27 mg, 28 mg, 29 mg, 30 mg, 31 mg, 32 mg, 33 mg, 34 mg, 35 mg, 36 mg, 37 mg, 38 mg, 39 mg or 40 mg at each administration.
22. The method of claim 21 wherein the subject is human.
23. The method of claim 22 wherein the HIV is HIV-1.
24. The method of claim 23 wherein the compound is