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Details for Patent: 6,777,399

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Details for Patent: 6,777,399

Title: Anti-inflammatory androstane derivative compositions
Abstract:There is provided a crystalline chemical composition comprising a compound of formula (I) ##STR1## in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P2.sub.1 2.sub.1 2.sub.1 having unit cell dimensions of about 12.1.+-.0.6 .ANG., 14.9.+-.0.7 .ANG., and 16.2.+-.0.8 .ANG. when determined at either 120K or 150K.
Inventor(s): Biggadike; Keith (Stevenage, GB), Coote; Steven John (Stevenage, GB), Craig; Andrew S. (Tonbridge, GB), Jacewicz; Victor W (Tonbridge, GB), Millan; Michael J. (Tonbridge, GB), Nice; Rosalyn K. (Stevenage, GB), Noga; Brian M (Durham, NC), Seager; John F. (Stevenage, GB), Theophilus; Andrew L. (Stevenage, GB), Crowe; David M. (Tonbridge, GB)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Filing Date:Feb 04, 2002
Application Number:10/067,010
Claims:1. A crystalline chemical composition comprising a compound of formula (I) ##STR8##

in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P2.sub.1 2.sub.1 2.sub.1 having unit cell dimensions of about 12.1.+-.0.6 .ANG., 14.9.+-.0.7 .ANG., and 16.2.+-.0.8 .ANG. when determined at either 20K or 150K.

2. A composition according to claim 1 wherein the guest molecule has a relative molecular weight in the range 16 to 150.

3. A composition according to claim 1 wherein the guest molecule contains a moiety capable of acting as a hydrogen bond acceptor.

4. A composition according to claim 1 wherein the guest molecule is selected from the list consisting of cyclopentanone, dimethylsulfoxide, ethanol, propan-1-ol, butan-1-ol, 1,4-dioxane, ethyl formate, methyl acetate, water and acetic acid.

5. A composition according to claim 1 wherein the guest molecule is acetone.

6. A composition according to claim 1 wherein the guest molecule is methylethylketone.

7. A composition according to claim 1 wherein the guest molecule is tetrahydrofuran.

8. A composition according to claim 1 wherein the guest molecule is propan-2-ol.

9. A composition according to claim 1 wherein the guest molecule is dimethylformamide.

10. A composition according to claim 1 wherein the guest molecule is butan-1-ol.

11. A composition according to claim 1 wherein the guest molecule is methyl acetate.

12. A composition according to claim 1 wherein the guest molecule is acetic acid.

13. A composition according to claim 1 wherein the guest molecule is propan-1-ol.

14. A composition according to claim 1 wherein the guest molecule is ethanol.

15. A composition according to claim 1 wherein the guest molecule is ethyl formate.

16. A composition according to claim 1 wherein the guest molecule is 1,4-dioxane.

17. A composition according to claim 1 wherein the guest molecule is dimethylsulphoxide.

18. A composition according to claim 1 wherein the guest molecule is N-methyl-2-pyrrolidinone.

19. A composition according to claim 1 wherein the guest molecule is dimethylacetamide.

20. A composition according to claim 1 wherein the guest molecule is cyclopentanone.

21. A composition according to claim 1 wherein the guest molecule is water.

22. A composition according to claim 1 wherein the guest molecule is .quadrature.-caprolactam.

23. A composition according to claim 1 wherein the ratio of compound of formula (I) to guest molecule is 1:2.0-0.3.

24. A pharmaceutical composition comprising a composition according to claim 1 together with a physiologically acceptable diluent or carrier.

25. A method for the treatment of a human or animal subject with an inflammatory and/or allergic condition, which method comprises administering to said human or animal subject an effective amount of the composition according to claim 1.

26. A pharmaceutical composition comprising a composition according to claim 1 in combination with another therapeutically active agent.

27. A composition according to claim 26 wherein the other therapeutically active ingredient is a long acting .beta..sub.2 -adrenoreceptor agonist.

28. A process for preparing a composition according to claim 1 which comprises (a) crystallising the composition from a solution containing a compound of formula (I) and the guest molecule; or (b) contacting the compound of formula (I) or a complex of the compound of formula (I) and a second guest molecule in solid form with a liquid containing the guest molecule and obtaining the composition therefrom; or (c) contacting a compound of formula (I) or a complex of the compound of formula (I) and a second guest molecule in solid form with a vapour containing the guest molecule and obtaining the composition therefrom.

29. A process for preparing compound of formula (I) in unsolvated form in the form of equant or substantially equant particles by a process comprising: (a) preparing a composition according to claim 1 in the form of equant or substantially equant particles; and (b) removing the guest molecule.

30. A process according to claim 29 wherein the composition is a composition with propan-2-ol or acetone as guest molecule.
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