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Claims for Patent: 5,484,801

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Claims for Patent: 5,484,801

Title: Pharmaceutical composition for inhibiting HIV protease
Abstract:A pharmaceutical composition is disclosed which comprises a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a mixture of (1) (a) a solvent selected from propylene glycol and polyethylene glycol or (b) a solvent selected from polyoxyethyleneglycerol triricinoleate, polyethylene glycol 40 hydrogenated castor oil, fractionated coconut oil, polyoxyethylene (20) sorbitan monooleate and 2-(2-ethoxyethoxy)ethanol or (c) a mixture thereof and (2) ethanol or propylene glycol.
Inventor(s): Al-Razzak; Laman A. (Libertyville, IL), Marsh; Kennan C. (Lake Forest, IL), Manning; Lourdes P. (Grayslake, IL), Kaul; Dilip (Waukegan, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Application Number:08/440,277
Patent Claims: 1. A pharmaceutical composition comprising a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a mixture of (1) (a) a solvent selected from propylene glycol and polyethylene glycol or (b) a solvent selected from polyoxyethyleneglycerol triricinoleate, polyethylene glycol 40 hydrogenated castor oil, fractionated coconut oil, polyoxyethylene (20) sorbitan monooleate and 2-(2-ethoxyethoxy)ethanol or (c) a mixture thereof and (2) ethanol or propylene glycol wherein the HIV protease Inhibiting compound is selected from the group consisting of:

N-(2(R)-hydroxy-1(S)-Indanyl)-2(R)-phenylmethyl-4(S)-hydroxy-5-(1-(4-(3-pyr idylmethyl)-2(S)-N'-(t-butylcarboxamido)-piperazinyl))-pentaneamide: N-tert-butyl-decahydro-2-(2(R)-hydroxy-4-phenyl-3(S)-((N-(2-quinolylcarbon yl)-L-asparaginyl)amino]butyl)-(4aS,8aS)-isoquinoline-3(S)-carboxamide; (1S-(1R*(R*),2S*)}-N.sup.1 (3-((((1,1-dimethylethyl)amino)carbonyl)(2-methylpropyl)amino)-2hydroxy-1- (phenylmethyl)propyl)-2-((2-quinolinylcarbonyl)amino)-butanediamide; and ##STR4##

2. The composition of claim 1 comprising a solution of the HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol or polyoxyethyleneglycerol triricinoleate or a mixture thereof and (2) ethanol.

3. The composition of claim 1 further comprising a pharmaceutically acceptable acid.

4. The composition of claim 1 further comprising water.

5. The composition of claim 1 further comprising one or more additives independently selected from pharmaceutically acceptable organic solvents, pharmaceutically acceptable oils, pharmaceutically acceptable sweetening agents, pharmaceutically acceptable flavoring agents, pharmaceutically acceptable surfactants and antioxidants.

6. The composition of claim 1 wherein the HIV protease inhibiting compound is N-(2(R)-hydroxy-1(S)-indanyl)-2(R)-phenylmethyl-4(S)-hydroxy-5-(1-(4-(3-py ridylmethyl)-2(S)-N'-(t-butylcarboxamido)-piperazinyl))-pentaneamide.

7. The composition of claim 1 wherein the HIV protease inhibiting compound is N-tert-butyl-decahydro-2-(2(R)-hydroxy-4-phenyl-3(S)-((N-(2-quinolylcarbon yl)-L-asparaginyl)amino]butyl)-(4aS,8aS)-isoquinoline-3(S)-carboxamide.

8. The composition of claim 1 wherein the HIV protease inhibiting compound is (1S-(1R*(R*),2S*)}-N.sup.1 (3-((((1,1-dimethylethyl)amino)carbonyl)(2-methylpropyl)amino)-2-hydroxy-1 -(phenylmethyl)propyl)-2-((2-quinolinylcarbonyl)amino)-butanediamide.

9. The composition of claim 1 wherein the HIV protease inhibiting compound is ##STR5##

10. A pharmaceutical composition comprising a solution of a compound of the formula: ##STR6## in a pharmaceutically acceptable organic solvent comprising a mixture of (1) (a) a solvent selected from propylene glycol and polyethylene glycol or (b) a solvent selected from polyoxyethyleneglycerol triricinoleate, polyethylene glycol 40 hydrogenated castor oil, fractionated coconut oil, polyoxyethylene (20) sorbitan monooleate and 2-(2-ethoxyethoxy)ethanol or (c) a mixture thereof and (2) ethanol or propylene glycol.

11. The composition of claim 10 comprising a solution of a compound of the formula: ##STR7## in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol or polyoxyethyleneglycerol triricinoleate or a mixture thereof and (2) ethanol.

12. The composition of claim 10 further comprising a pharmaceutically acceptable acid or a mixture of pharmaceutically acceptable acids.

13. The composition of claim 10 further comprising water.

14. The composition of claim 10 further comprising one or more additives independently selected from pharmaceutically acceptable organic solvents, pharmaceutically acceptable oils, pharmaceutically acceptable sweetening agents, pharmaceutically acceptable flavoring agents, pharmaceutically acceptable surfactants and antioxidants.

15. The composition of claim 10 comprising a solution of from about 1% to about 15% by weight of the total solution of a compound of the formula: ##STR8## in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of from about 10% to about 50% by weight of the total solution or polyoxyethyleneglycerol triricinoleate in the amount of from about 5% to about 35% by weight of the total solution or a mixture thereof and (2) ethanol in the amount of from about 5% to about 45% by weight of the total solution.

16. The composition of claim 15 further comprising a pharmaceutically acceptable acid in the amount of from about 0.2% to about 16% by weight of total solution.

17. The composition of claim 15 comprising a solution of from about 1% to about 15% by weight of the total solution of (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-dipheny l-3-hydroxyhexane in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of from about 10% to about 50% by weight of the total solution or polyoxyethyleneglycerol triricinoleate in the amount of from about 5% to about 35% by weight of the total solution or a mixture thereof and (2) ethanol in the amount of from about 5% to about 45% by weight of the total solution.

18. The composition of claim 17 further comprising a pharmaceutically acceptable acid in the amount of from about 0.2% to about 16% by weight of total solution.

19. The composition of claim 18 wherein the pharmaceutically acceptable acid is citric acid.

20. The composition of claim 19 comprising a solution of about 5% by weight of the total solution of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)car bonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl -3-hydroxyhexane and about 4% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of about 42% by weight of the total solution, (2) ethanol in the amount of about 32% by weight of the total solution and (3) water in the amount of about 17% by weight of the total solution.

21. The composition of claim 19 comprising a solution of about 12% by weight of the total solution of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)car bonyl)valinyl)amino-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl- 3-hydroxyhexane and from about 3% to about 4% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of about 32% by weight of the total solution, (2) ethanol in the amount of about 37% by weight of the total solution and (3) water in the amount of about 15% by weight of the total solution.

22. The composition of claim 19 comprising a solution of about 5% by weight of the total solution of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)car bonyl)valinyl)amino-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl- 3-hydroxyhexane and from about 5% to about 6% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of from about 44% to about 45% by weight of the total solution, (2) ethanol in the amount of about 24% by weight of the total solution and (3) polyoxyethyleneglycerol triricinoleate in the amount of about 20% by weight of the total solution.

23. The composition of claim 19 comprising a solution of about 10% by weight of the total solution of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)car bonyl)valinyl)amino-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl- 3-hydroxyhexane and from about 5% to about 6% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of from about 39% to about 40% by weight of the total solution, (2) ethanol in the amount of about 24% by weight of the total solution and (3) polyoxyethyleneglycerol triricinoleate in the amount of about 20% by weight of the total solution.

24. The composition of claim 19 comprising a solution of from about 2% to about 3% by weight of the total solution of (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-dipheny l-3-hydroxyhexane and about 4% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of about 43% by weight of the total solution, (2) ethanol in the amount of about 33% by weight of the total solution and (3) water in the amount of about 17% by weight of the total solution.

25. The composition of claim 19 comprising a solution of about 5% by weight of the total solution of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)car bonyl)valinyl)amino-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl- 3-hydroxyhexane and from about 0.3 to about 0.4% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of about 36% by weight of the total solution, (2) ethanol in the amount of about 36% by weight of the total solution and (3) water in the amount of about 19% by weight of the total solution.

26. The composition of claim 19 comprising a solution of about 8% by weight of the total solution of (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)car bonyl)valinyl)amino-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl- 3-hydroxyhexane and from about 0.3 to about 0.4% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propyleneglycol in the amount of about 35% by weight of the total solution, (2) ethanol in the amount of about 35% by weight of the total solution and (3) water in the amount of about 18% by weight of the total solution.

27. The composition of claim 19 comprising a solution of from about 7% to about 8% by weight of the total solution of (2S,3S,5S)-5-(N-(N-((N-MethyI-N-((2-isopropyl-4-thiazolyl)methyl)-amino)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-dipheny l-3-hydroxyhexane and about 0.5% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of from about 45% to about 46% by weight of the total solution, (2) ethanol in the amount of about 21% by weight of the total solution and (3) polyoxyethyleneglycerol triricinoleate in the amount of from about 24% to about 25% by weight of the total solution.

28. The composition of claim 19 comprising a solution of from about 7% to about 8% by weight of the total solution of (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-dipheny l-3-hydroxyhexane and from about 0.2% to about 0.3% by weight of the total solution of citric acid in a pharmaceutically acceptable organic solvent comprising a mixture of (1) propylene glycol in the amount of from about 31% to about 32% by weight of the total solution, (2) ethanol in the amount of about 32% by weight of the total solution, (3) polyoxyethyleneglycerol triricinoleate in the amount of from about 10% to about 11% by weight of the total solution and (4) water in the amount of from about 14% to about 15% by weight of the total solution.
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