Claims for Patent: 12,594,244

Summary for Patent: 12,594,244

Title:	Therapeutic compositions for treatment of human immunodeficiency virus
Abstract:	A solid oral dosage form is provided, comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.
Inventor(s):	Benjamin Micah Collman, Lei Hong, Joanna M. Koziara
Assignee:	Gilead Sciences Inc
Application Number:	US19/343,371
Patent Claims:	1. A tablet comprising from 6.5-11.0% w/w of a compound of Formula I: or a pharmaceutically acceptable salt thereof, 3.0-4.5% w/w tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and 25-30% w/w emtricitabine or a pharmaceutically acceptable salt thereof, where the weight percentages denote a proportion of the whole tablet. 2. A tablet comprising from 7.0-11.0% w/w of a compound of Formula II: 3.5-4.1% w/w tenofovir alafenamide hemifumarate, and 25-30% w/w emtricitabine, where the weight percentages denote a proportion of the whole tablet. 3. The tablet of claim 1, wherein the tablet does not contain lactose, crospovidone, or sodium stearyl fumarate. 4. The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium or magnesium stearate. 5. The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, or microcrystalline cellulose. 6. The tablet of claim 1, wherein the tablet releases at least about 50% of the compound of Formula I or the pharmaceutically acceptable salt thereof in about 20 minutes, measured using USP apparatus II, in 333 mL of fasted simulated intestinal fluid, pH 6.5, at 37° C. and paddle speed of 100 rpm. 7. The tablet of claim 6, wherein the tablet releases at least about 60% of the compound of Formula I or the pharmaceutically acceptable salt thereof in about 20 minutes. 8. The tablet of claim 6, wherein the tablet releases at least about 70% of the compound of Formula I or the pharmaceutically acceptable salt thereof in about 60 minutes. 9. A tablet comprising: (i) from about 6.4 w/w to about 8.5% w/w of a compound of Formula II (ii) about 25% w/w to about 32% w/w emtricitabine, (iii) about 3.5% w/w to about 4.5% w/w tenofovir alafenamide hemifumarate, (iv) about 46% w/w to about 57% w/w microcrystalline cellulose, (v) about 5.9% w/w to about 8.5% w/w croscarmellose sodium, and (vi) about 1.0-2.0% w/w magnesium stearate. 10. The tablet of claim 9, further comprising a film coating. 11. The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium and magnesium stearate. 12. The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, and microcrystalline cellulose. 13. The tablet of claim 1, wherein the tablet is a coated tablet. 14. The tablet of claim 1, wherein the tablet has a total weight of between about 250 and about 750 mg. 15. The tablet of claim 2, wherein the tablet does not contain lactose, crospovidone, or sodium stearyl fumarate. 16. The tablet of claim 2, wherein the tablet further comprises croscarmellose sodium or magnesium stearate. 17. The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium and magnesium stearate. 18. The tablet of claim 2, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, or microcrystalline cellulose. 19. The tablet of claim 2, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, and microcrystalline cellulose. 20. The tablet of claim 2, wherein the tablet is a coated tablet. 21. The tablet of claim 2, wherein the tablet has a total weight of between about 250 and about 750 mg. 22. The tablet of claim 2, wherein the tablet releases at least about 50% of the compound of Formula II in about 20 minutes, measured using USP apparatus II, in 333 mL of fasted simulated intestinal fluid, pH 6.5, at 37° C. and paddle speed of 100 rpm. 23. The tablet of claim 22, wherein the tablet releases at least about 60% of the compound of Formula II in about 20 minutes. 24. The tablet of claim 22, wherein the tablet releases at least about 70% of the compound of Formula II in about 60 minutes. 25. The tablet of claim 9, wherein the tablet releases at least about 50% of the compound of Formula II in about 20 minutes, measured using USP apparatus II, in 333 mL of fasted simulated intestinal fluid, pH 6.5, at 37° C. and paddle speed of 100 rpm. 26. The tablet of claim 25, wherein the tablet releases at least about 60% of the compound of Formula II in about 20 minutes. 27. The tablet of claim 25, wherein the tablet releases at least about 70% of the compound of Formula II in about 60 minutes. 28. The tablet of claim 9, wherein the tablet has a total weight of between about 250 and about 750 mg. 29. A method of therapeutic treatment of an HIV infection comprising administering to a subject a tablet comprising: (i) from about 6.4 w/w to about 8.5% w/w of the compound of Formula II (ii) about 25% w/w to about 32% w/w emtricitabine, (iii) about 3.5% w/w to about 4.5% w/w tenofovir alafenamide hemifumarate, (iv) about 46% w/w to about 57% w/w microcrystalline cellulose, (v) about 5.9% w/w to about 8.5% w/w croscarmellose sodium, and (vi) about 1.0-2.0% w/w magnesium stearate.