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Details for Patent: 5,876,749

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Details for Patent: 5,876,749

Title: Pharmaceutical composition
Abstract:A pharmaceutical composition is disclosed which comprises a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a pharmaceutically acceptable alcohol. The composition can optionally comprise a pharmaceutically acceptable acid or a combination of pharmaceutically acceptable acids. The solution can optionally be encapsulated in hard gelatin capsules or soft elastic gelatin capsules. The solution can optionally be granulated with a pharmaceutically acceptable granulating agent.
Inventor(s): Al-Razzak; Laman A. (Libertyville, IL), Marsh; Kennan C. (Lake Forest, IL), Kaul; Dilip (Waukegan, IL), Manning; Lourdes P. (Grayslake, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Filing Date:May 04, 1995
Application Number:08/435,918
Claims:1. A pharmaceutical composition comprising a solution of (1) an HIV protease inhibiting compound 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-quinolylcarbony l)-L-asparaginyl)amino)butyl)-(4aS,8aS)-isoquinoline-3(S)-carboxamide;

5-(S)-Boc-amino-4(S)-hydroxy-6-phenyl-2(R)-phenylmethylhexanoyl-(L)-Val-(L) -Phe-morpholin-4-ylamide;

1-Naphthoxyacetyl-beta-methylthio-Ala-(2S,3S)-3-amino-2-hydroxy-4-butanoyl- 1,3-thiazolidine-4-t-butylamide;

5-isoquinolinoxyacetyl-beta-methylthio-Ala-(2S,3S)-3-amino-2-hydroxy-4-buta noyl-1,3-thiazolidine-4-t-butylamide;

(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; ##STR6## in the amount of from about 2% to about 30% by weight of the total solution and (2) a total of from about 0.2 to about 2 molar equivalents, based upon the amount of the compound of part (1), of (i) a pharmaceutically acceptable acid or (ii) a mixture of pharmaceutically acceptable acids, said HIV protease Inhibiting compound and pharmaceutically acceptable acid or acids being dissolved in a pharmaceutically acceptable organic solvent comprising a mixture of (a) a pharmaceutically acceptable alcohol or mixture of pharmaceutically acceptable alcohols in a total amount of from about 2% to about 50% by weight of the total solution, said alcohol or mixture of alcohols being a liquid at room temperature and (b) a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents in a total amount of from about 20% to about 60% by weight of the total solution, said solvent or mixture of solvents having a melting point between about 20.degree. C. and about 60.degree. C., said solvent or mixture of solvents being miscible with the alcohol or mixture of alcohols and providing a homogeneous mixture with the alcohol or mixture of alcohols, said homogeneous mixture being a solid or semi-solid at about 20.degree. C.

2. The composition of claim 1 wherein the HIV protease inhibitor 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.

3. The composition of claim 1 wherein the HIV protease inhibitor 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.

4. The composition of claim 1 wherein the HIV protease inhibitor is ##STR7##

5. The composition of claim 1 wherein the HIV protease inhibitor is ##STR8##

6. A composition according to claim 1 comprising a solution of (1) an HIV protease inhibiting compound 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-quinolylcarbony l)-L-asparaginyl)amino)butyl)-(4aS,8aS)-isoquinoline-3(S)-carboxamide;

5(S)-Boc-amino-4(S)-hydroxy-6-phenyl-2(R)-phenylmethylhexanoyl-(L)-Val-(L)- Phe-morpholin-4-ylamide;

1-Naphthoxyacetyl-beta-methylthio-Ala-(2S,3S)-3-amino-2-hydroxy-4-butanoyl- 1,3-thiazolidine-4-t-butylamide;

5-isoquinolinoxyacetyl-beta-methylthio-Ala-(2S,3S)-3-amino-2-hydroxy-4-buta noyl-1,3-thiazolidine-4-t-butylamide;

(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; ##STR9## in the amount of from about 2% to about 30% by weight of the total solution and (2) a total of from about 0.2 to about 2 molar equivalents, based upon the amount of the compound of part (1), of (i) a pharmaceutically acceptable acid or (ii) a mixture of pharmaceutically acceptable acids, said HIV protease inhibiting compound and pharmaceutically acceptable acid or acids being dissolved in a pharmaceutically acceptable organic solvent comprising a mixture of (a) propylene glycol in the amount of from about 4% to about 40% by weight of the total solution, (b) ethanol in the amount of from about 2% to about 20% by weight of the total solution, and (c) either polyethylene glycol 540 in the amount of from about 20% to about 60% by weight of the total solution or a total amount of from about 20% to about 60% by weight of the total solution of (i) a saturated polyglycolized glyceride or (ii) a mixture of saturated polyglycolized glycerides.

7. The composition of claim 6 wherein the solution is encapsulated in a hard gelatin capsule or a soft elastic gelatin capsule.

8. The composition of claim 6 wherein the HIV protease inhibitor 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.

9. The composition of claim 6 wherein the HIV protease inhibitor 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.

10. The composition of claim 6 wherein the HIV protease inhibitor is ##STR10##

11. The composition of claim 6 wherein the HIV protease inhibitor is ##STR11##

12. The composition of claim 1 wherein the solution is encapsulated in a hard gelatin capsule or a soft elastic gelatin capsule.

13. The composition of claim 1 further comprising an additive or a mixture of additives independently selected from the group consisting of glycerin, pharmaceutically acceptable surfactants and antioxidants.
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