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Last Updated: March 29, 2024

Claims for Patent: 5,886,036


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Summary for Patent: 5,886,036
Title: Retroviral protease inhibiting compounds
Abstract:A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
Inventor(s): Kempf; Dale J. (Libertyville, IL), Norbeck; Daniel W. (Crystal Lake, IL), Sham; Hing Leung (Gurnee, IL), Zhao; Chen (Gurnee, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Application Number:08/822,071
Patent Claims: 1. A combination pharmaceutical agent for the treatment of an HIV infection comprising (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphen yl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and another HIV protease inhibiting compound.

2. The combination of claim 1 wherein the other HIV protease inhibiting compound is selected from the group consisting of Ro 31-8959, SC-52151, KNI-227 and KNI-272.

3. The combination of claim 1 wherein the other HIV protease inhibiting compound is Ro 31-8959.

4. The combination of claim 1 wherein (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphen yl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and the other HIV protease inhibiting compound are each formulated as separate compositions.

5. The combination of claim 4 wherein the formulation of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl) methyl)-amino)carbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxy-carbonyl) -amino)-1,6-diphenyl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and the formulation of the other HIV protease inhibiting compound are to be administered at the same time.

6. The combination of claim 4 wherein the formulation of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxy-carbonyl)-amino)-1,6-diphe nyl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and the formulation of the other HIV protease inhibiting compound are to be administered at different times.

7. A combination pharmaceutical agent for the treatment of an HIV infection comprising (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphen yl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and Ro 31-8959.

8. A combination of pharmaceutical agents for the treatment of an HIV infection comprising (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphen yl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and another HIV protease inhibiting compound.

9. The combination of claim 8 wherein the other HIV protease inhibiting compound is selected from the group consisting of Ro 31-8959, SC-52151, KNI-227 and KNI-272.

10. The combination of claim 8 wherein the other HIV protease inhibiting compound is Ro 31-8959.

11. The combination of claim 8 wherein (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphen yl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and the other HIV protease inhibiting compound are each formulated as separate compositions.

12. The combination of claim 11 wherein the formulation of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxy-carbonyl)-amino)-1,6-diphe nyl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and the formulation of the other HIV protease inhibiting compound are to be administered at the same time.

13. The combination of claim 11 wherein the formulation of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxy-carbonyl)-amino)-1,6-diphe nyl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and the formulation of the other HIV protease inhibiting compound are to be administered at different times.

14. A combination of pharmaceutical agents for the treatment of an HIV infection comprising (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphen yl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and Ro 31-8959.

15. (2S,3 S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)carbonyl )valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphenyl-3-h ydroxyhexane or a pharmaceutically acceptable salt thereof and another HIV protease inhibitor for concomitant administration for the treatment of an HIV infection.

16. (2S,3S,5S)- 5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)carbonyl)valin yl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphenyl-3-hydroxy hexane or a pharmaceutically acceptable salt thereof and Ro 31-8959 for concomitant administration for the treatment of an HIV infection.

17. A combination pharmaceutical agent for administration to a human for the treatment of an HIV infection comprising:

a) a first pharmaceutical composition comprising (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)-amino)-1,6-diphen yl-3-hydroxyhexane or a pharmaceutically acceptable salt thereof and

b) a second pharmaceutical composition comprising another HIV protease inhibiting compound.

18. The combination of claim 17 wherein the other HIV protease inhibiting compound is selected from the group consisting of Ro 31-8959, SC-52151, KNI-227 and KNI-272.

19. The combination of claim 17 wherein the other HIV protease inhibiting compound is Ro 31-8959.

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