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Claims for Patent: 6,514,953

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Claims for Patent: 6,514,953

Title: Calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1 -benzyl-2-(phosphonooxy)propylcarbamate
Abstract:The invention relates to calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1 -benzyl-2-(phosphonooxy)propylcarbamate, to processes for its preparation, and to its use in the treatment of diseases caused by retroviruses. ##STR1##
Inventor(s): Armitage; Ian Gordon (Arlesey, GB), Searle; Andrew David (Stevenage, GB), Singh; Hardev (Dartford, GB)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Application Number:09/744,051
Patent Claims: 1. Calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1 -benzyl-2-(phosphonooxy)propylcarbamate Form (1).

2. A pharmaceutical composition comprising a compound as claimed in claim 1 together with at least one pharmaceutically acceptable diluent or carrier therefor.

3. A method for the treatment of an HIV infection in a human which comprises administering to said human, an effective anti-HIV infection treatment amount of a compound as claimed in claim 1.

4. A pharmaceutical composition according to claim 2 in the form of a powder.

5. A pharmaceutical composition according to claim 2 in the form of a suspension.

6. A pharmaceutical composition according to claim 2 in the form of a tablet.

7. A process for the preparation of a compound of formula (I) in a crystalline form, ##STR6##

comprising i) reacting a compound of formula (II) ##STR7## with a phosphorylating agent; ii) reducing the resultant compound with a reducing agent in a suitable solvent; and iii) adding to the resultant compound a source of calcium ions in the presence of a suitable solvent.

8. A process for the preparation of a compound of formula (I) ##STR8##

comprising dissolving a compound of formula (III) ##STR9##

in a suitable solvent, and adding to the solution water and a source of calcium ions.

9. A process for the preparation of a compound of formula (I) ##STR10##

comprising the reduction of a compound of formula (IV) ##STR11##

in the presence of a suitable reducing agent in a suitable solvent, followed by adding water and a source of calcium ions.

10. A process for the preparation of a compound of formula (I) as claimed in claim 7, wherein the phosphorylating agent is phosphorus oxychloride.

11. A process for the preparation of a compound of formula (I) as claimed in claim 7, wherein the phosphorylating agent is added in the presence of a base.

12. A process for the preparation of a compound of formula (I) as claimed in claim 7, wherein the product of step i) is converted to its sodium salt prior to step ii).

13. A process for the preparation of a compound of formula (I) as claimed in claim 7, wherein the reducing agent is hydrogen with a palladium on carbon catalyst.

14. A process for the preparation of a compound of formula (I) as claimed in claim 7, wherein the calcium ion source is calcium acetate.

15. A process for the preparation of a compound of formula (I) as claimed in claim 7, additionally comprising recrystallising the compound from an appropriate solvent.

16. A process for the preparation of a compound of formula (I) as claimed in claim 15, wherein the solvent is a mixture of industrial methylated spirit and water.

17. A process for the preparation of a compound of formula (I) as claimed in claim 7, additionally comprising heating the product in water to a temperature in the range 70 to 99.degree. C. for 2.5 to 6 hours, then cooling to ambient temperature and harvesting to solid.

18. Calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1 -benzyl-2-(phosphonooxy)propylcarbamate Form (1) characterized by an X-ray powder diffraction trace substantially as shown in FIG. 1.

19. A crystalline form of calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1 -benzyl-2-phosphonooxy)propylcarbamate characterised by an X-ray powder diffraction pattern expressed in terms of 2 theta angles, wherein said X-ray powder diffraction pattern has peaks that may occur at the following approximate 2 theta angles: 5.735, 9.945, 11.500, 13.780, 14.930, 15.225, 17.980, 19.745, 21.575, 22.170, 24.505 and 27.020 degrees.

20. A crystalline form of calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1 -benzyl-2-(phosphonooxy)propylcarbamate characterised by an X-ray powder diffraction pattern expressed in terms of 2 theta angles and relative intensities (1),
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