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Claims for Patent: 8,501,818

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Claims for Patent: 8,501,818

Title:Stabilized compositions of alkylating agents and methods of using same
Abstract: Provided are stable compositions comprising alkylating agents, including nitrogen mustards, that are suitable for topical use, and methods for treating skin disorders comprising topically administering the compositions.
Inventor(s): Alonso; Robert (Rye, NH), Stogniew; Martin (Blue Bell, PA), Crooks; Peter A. (Nicholasville, KY), Pimley; Mark A. (Westchester, PA), Worthen; David R. (Wakefield, RI)
Assignee: Ceptaris Therapeutics, Inc. (Malvern, PA)
Application Number:12/687,605
Patent Claims: 1. A topical composition comprising: (a) an effective amount of bis-(2-chloroethyl)methylamine or a pharmaceutically acceptable salt or solvate thereof; and (b) a pharmaceutically acceptable excipient comprising a compound of the formula HOCH.sub.2CH.sub.2OCH.sub.2CH.sub.2OR.sub.79, wherein R.sub.79 is a linear alkyl group having 1-6 carbon atoms, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 3 months to about 3 years at a temperature of about -20.degree. C. to about 8.degree. C.

2. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 3 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

3. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 6 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

4. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 12 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

5. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 24 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

6. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 3 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

7. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 6 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

8. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 12 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

9. The composition of claim 1, wherein at least about 90% of the bis-(2-chloroethyl)methylamine or pharmaceutically acceptable salt or solvate thereof is present in the composition after storage for at least about 24 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

10. A topical composition comprising: (a) an effective amount of bis-(2-chloroethyl)methylamine or a pharmaceutically acceptable salt or solvate thereof; and (b) a pharmaceutically acceptable excipient comprising a compound of the formula HOCH.sub.2CH.sub.2OCH.sub.2CH.sub.2OR.sub.79, wherein R.sub.79 is a linear alkyl group having 1-6 carbon atoms, wherein the composition contains less than about 10% by weight of nitrogen mustard degradation product after storage for about 3 months to about 3 years at a temperature of about -20.degree. C. to about 8.degree. C.

11. The composition of claim 10, wherein the nitrogen mustard degradation product is a half-mustard.

12. The composition of claim 11, wherein the half-mustard has the following structure (DP-B): ##STR00061## wherein: E is --O--, --NH--, --S--; --OC(O)CH(CH.sub.3)OC(O)CH(CH.sub.3)-; --OCH(CH.sub.3)C(O)OCH(CH.sub.3)-; or --O(CH.sub.2).sub.20(CH.sub.2).sub.20-; and R.sup.80 is a linear or branched alkyl group having 1-12 carbon atoms, --COOH, or --OH.

13. The composition of claim 10, wherein the nitrogen mustard degradation product is ##STR00062##

14. The composition of claim 10, wherein the nitrogen mustard degradation product is ##STR00063##

15. The composition of claim 10, wherein the nitrogen mustard degradation product is ##STR00064##

16. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 3 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

17. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 6 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

18. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 12 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

19. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 24 months to about 3 years at a temperature of about 2.degree. C. to about 8.degree. C.

20. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 3 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

21. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 6 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

22. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 12 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

23. The composition of claim 10, wherein the composition contains less than about 10% by weight of the nitrogen mustard degradation product after storage for at least about 24 months to about 3 years at a temperature of about -20.degree. C. to about -10.degree. C.

24. The composition of claim 10, wherein the nitrogen mustard degradation product is: ##STR00065##
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