You're using a free limited version of DrugPatentWatch: Upgrade for Complete Access

Last Updated: December 22, 2024

Claims for Patent: 9,708,342


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 9,708,342
Title:Sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,- 5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2, 1-b][1, 3]oxazepin-8-olate
Abstract: The present invention relates to sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl) carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyraz- ino[2,1-b][1,3] oxazepin-8-olate Form I and the therapeutic uses thereof.
Inventor(s): Carra; Ernest A. (Foster City, CA), Chen; Irene (San Mateo, CA), Zia; Vahid (Palo Alto, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Application Number:14/744,915
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,708,342
Patent Claims: 1. A compound of Formula II: ##STR00004##

2. The compound of claim 1, characterized by being crystalline.

3. The compound of claim 2, characterized by an x-ray powder diffraction (XRPD) pattern having peaks at about 5.5.degree., 16.1.degree., and 23.3.degree. 2-.theta..+-.0.2.degree. 2-.theta..

4. The compound of claim 3, wherein the x-ray powder diffraction (XRPD) pattern has further peaks at about 22.1.degree., and 28.5.degree. 2-.theta..+-.0.2.degree. 2-.theta..

5. The compound of claim 4, wherein the x-ray powder diffraction (XRPD) pattern has further peaks at about 22.5 and 19.5.degree. 2-.theta..+-.0.2.degree. 2-.theta..

6. The compound of claim 5, wherein the x-ray powder diffraction (XRPD) pattern has further peaks at about 26.6.degree. and 17.9.degree. 2-.theta..+-.0.2.degree. 2-.theta..

7. The compound of claim 2, characterized by an x-ray powder diffraction (XRPD) pattern substantially as set forth in FIG. 1.

8. The compound of claim 2, characterized by differential scanning calorimetry (DSC) pattern substantially as set forth in FIG. 2.

9. The compound of claim 2, characterized by a dynamic vapor sorption (DVS) pattern substantially as set forth in FIG. 4.

10. The compound of any one of claims 1 to 9, characterized in being partially or fully hydrated.

11. The compound of any one of claims 1 to 9, characterized in being anhydrous or essentially anhydrous.

12. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of claims 1 to 9, and a pharmaceutically acceptable carrier or excipient.

13. The pharmaceutical composition of claim 12, further comprising one to three additional therapeutic agents.

14. The pharmaceutical composition of claim 13, wherein the additional therapeutic agents are each anti-HIV drugs.

15. The pharmaceutical composition of claim 13, wherein the additional therapeutic agents are each independently selected from the group consisting of HIV protease inhibitors, HIV non-nucleoside inhibitors of reverse transcriptase, HIV nucleoside inhibitors of reverse transcriptase, HIV nucleotide inhibitors of reverse transcriptase, pharmacokinetic enhancers and other drugs for treating HIV.

16. The pharmaceutical composition of claim 13, wherein one of the one to three additional therapeutic agents is an HIV nucleoside inhibitor of reverse transcriptase.

17. The pharmaceutical composition of claim 12, further comprising tenofovir disoproxil fumarate and emtricitabine.

18. The pharmaceutical composition of claim 12, further comprising tenofovir alafenamide and emtricitabine.

19. The pharmaceutical composition of claim 12, further comprising tenofovir alafenamide hemifumarate and emtricitabine.

20. The pharmaceutical composition of claim 12, wherein the pharmaceutical composition is in an oral unit dosage form.

21. The pharmaceutical composition of claim 20, wherein the unit dosage form is a tablet.

22. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of claims 1 to 9, and a pharmaceutically acceptable carrier or excipient, the composition further comprising one to three additional therapeutic agents, wherein each of the one to three additional therapeutic agents is independently an HIV nucleoside inhibitor of reverse transcriptase or an HIV nucleotide inhibitor of reverse transcriptase.

23. The pharmaceutical composition of claim 22, wherein the pharmaceutical composition is in an oral unit dosage form.

24. The pharmaceutical composition of claim 22, wherein the pharmaceutical composition is a tablet.

25. The pharmaceutical composition of claim 12, further comprising tenofovir alafenamide fumarate and emtricitabine.

26. The pharmaceutical composition of claim 12, further comprising tenofovir alafenamide hemifumarate and emtricitabine.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.