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Claims for Patent: 6,503,884

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Claims for Patent: 6,503,884

Title: Migraine treatment method using topiramate and related compounds
Abstract:A method for treating migraine in non-epileptic subjects which involves administering to subjects an effective amount of a pharmaceutical composition comprising a sulfamate of the following formula: ##STR1##
Inventor(s): Ehrenberg; Bruce L. (Boston, MA), Wagner; Anita K. (Arlington, MA)
Assignee: New England Medical Center Hospitals, Inc. (Boston, MA)
Application Number:09/436,003
Patent Claims: 1. A method of treating migraine in a non-epileptic human patient, the method comprising administering to the patient (a) an effective amount of a sulfamate of the following formula (I): ##STR6## wherein X is oxygen; R.sub.1 is hydrogen or a lower alkyl; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen or a lower alkyl, and R.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5 together are a methylenedioxy group of the following formula (II): ##STR7## wherein R.sub.6 and R.sub.7 are the same or different and are hydrogen, lower alkyl or are alkyl and are joined to form a cyclopentyl or cyclohexyl ring; or (b) an effective amount of a derivative of a sulfamate of formula I, wherein the derivative is (i) an ester of a sulfamate of formula I; (ii) a salt of the ester; (iii) a compound that upon administration to the patient provides, directly or indirectly, a compound of formula 1; or (iv) an anti-migraine active metabolite of formula I or a residue thereof.

2. The method of claim 1, wherein R.sub.2 and R.sub.3 and R.sub.4 and R.sub.5, together are groups of formula (II).

3. The method of claim 1, wherein R.sub.1 is an alkyl of 1 to 4 carbons; the lower alkyl group of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is an alkyl of 1 to 3 carbons; and the lower alkyl of R.sub.6 and R.sub.7 is an alkyl 1 to 3 carbons.

4. (Amended) The method of claim 1, wherein the sulfamate of formula (I) is: (tetrahydro-2H-pyran-2-yl)methane sulfamate; 2,3:4,5-bis-O-(1-methylethyldiene)-.beta.-D-fructopyranose sulfate; or 2,3:4,5-bis-O-(1-methylethyldiene)-.beta.-D-fructopyranose methylsulfamate.

5. The method of claim 4, wherein the sulfamate is 2,3:4,5-bis-O-(1-methylethyldiene).beta.-D-fructopyranose sulfamate.

6. The method of claim 4, wherein the sulfamate is 2,3:4,5-bis-O-(1-methylethyldiene)-.beta.-D-fructopyranose methylsulfamate.

7. The method of claim 1, wherein the sulfamate is administered together with a pharmaceutically acceptable carrier.

8. The method of claim 1, wherein the sulfamate is present in a unit dosage amount of about 50 to 400 milligrams.

9. The method of claim 1, wherein the two oxygen atoms of the group of formula (II) are attached on the same side of the six-membered ring depicted in formula (I).

10. The method of claim 1, wherein the sulfamate of formula (I) is fructopyranose.

11. The method of claim 1, wherein, in formula (I), R.sub.1 is hydrogen.

12. The method of claim 1, wherein the derivative is an imidate, a sorbopyranose sulfamate, a fructopyranose cyclic sulfite or sulfate, a phenylethyl sulfamate, acetazolamide, or methazolamide.

13. A method of reducing the frequency of migrainous episodes in a non-epileptic human patient in need thereof, the method comprising administering to the patient (a) an effective amount of a sulfamate of the following formula (I): ##STR8## wherein X is oxygen; R.sub.1 is hydrogen or a lower alkyl; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen or a lower alkyl, and, R.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5 together are a methylenedioxy group of the following formula (II): ##STR9## wherein R.sub.6 and R.sub.7 are the same or different and are hydrogen, lower alkyl or are alkyl and are joined to form a cyclopentyl or cyclohexyl ring; or (b) an effective amount of a derivative of a sulfamate of formula I, wherein the derivative is (i) an ester of a sulfamate of formula I; (ii) a salt of the ester; (iii) a compound that upon administration to the patient provides, directly or indirectly, a compound of formula I; or (iv) an anti-migraine active metabolite of formula I or a residue thereof.

14. The method of claim 13, wherein R.sub.2 and R.sub.3 and R.sub.4 and R.sub.5, together are groups of formula (II).

15. The method of claim 13, wherein R.sub.1 is an alkyl of 1 to 4 carbons; the lower alkyl group of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is an alkyl of 1 to 3 carbons; and the lower alkyl of R.sub.6 and R.sub.7 alkyl of 1 to 3 carbons.

16. The method of claim 13, wherein the sulfamate of formula (I) is: (tetrahydro-2H-pyran-2-yl)methane sulfamate; 2,3:4,5-bis-O-(1-methylethyldiene)-.beta.-D-fructopyranose sulfate; or 2,3:4,5-bis-O-(1-methylethyldiene)-.beta.-D-fructopyranose methylsulfamate.

17. The method of claim 16, wherein the sulfamate is 2,3:4,5-bis-O-(1-methylethyldiene).beta.-D-fructopyranose sulfamate.

18. The method of claim 16, wherein the sulfamate is 2,3:4,5-bis-O-(1-methylethyldiene)-.beta.-D-fructopyranose methylsulfamate.

19. The method of claim 13, wherein the sulfamate is administered together with a pharmaceutically acceptable carrier.

20. The method of claim 13, wherein the sulfamate is present in a unit dosage amount of about 50 to 400 milligrams.

21. The method of claim 13, wherein the two oxygen atoms of the group of formula (II) are attached on the same side of the six-membered ring depicted in formula (I).

22. The method of claim 13, wherein the sulfamate of formula (I) is fructopyranose.

23. The method of claim 13, wherein, in formula (I), R.sub.1 is hydrogen.

24. The method of claim 13, wherein the derivative is an imidate, a sorbopyranose sulfamate, a fructopyranose cyclic sulfite or sulfate, a phenylethyl sulfamate, acetazolamide, or methazolamide.

25. The method of claim 1, wherein the derivative is a pharmaceutically acceptable ester of formula I.

26. The method of claim 1, wherein the derivative is a pharmaceutically acceptable salt of an ester of formula I.

27. The method of claim 1, wherein the derivative is a compound that upon administration to the patient provides, directly or indirectly, a compound of formula I.

28. The method of claim 1, wherein the derivative is an anti-migraine active metabolite of formula I or a residue thereof.

29. The method of claim 13, wherein the derivative is a pharmaceutically acceptable ester of formula I.

30. The method of claim 13, wherein the derivative is a pharmaceutically acceptable salt of an ester of formula I.

31. The method of claim 13, wherein the derivative is a compound that upon administration to the patient provides, directly or indirectly, a compound of formula I.

32. The method of claim 13, wherein the derivative is an anti-migraine active metabolite of formula I or a residue thereof.
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