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Generated: December 15, 2017

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Claims for Patent: 5,998,380

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Claims for Patent: 5,998,380

Title: Treatment of migraine
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:08/542,950
Patent Claims: 1. A method of reducing the frequency or severity of migrainous episodes in a non-epileptic human patient, said method comprising administering to the patient an effective amount of a sulfamate of the following formula (I): ##STR6## wherein X is oxygen;

R.sub.1 is hydrogen or lower alkyl; and

R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen or lower alkyl and R.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5 together are a 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.

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 the formula (II).

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

4. The method of claim 1, wherein said sulfamate of formula (I) is selected from the group consisting of:

(tetrahydro-2H-pyran-2-yl)methane sulfamate;

2,3:4,5-bis--O--(l-methylethyldiene)-.beta.-D-fructopyranose sulfamate; and

2,3:4,5-bis--O--(l-methylethyldiene)-.beta.-D-fructopyranose methylsulfamate.

5. The method of claim 4, wherein said 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 said sulfamate is administered with a pharmaceutically acceptable carrier.

8. The method of claim 1, wherein said 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 a sulfamate of fructopyranose.

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

12. A method of treating migraine in a non-epileptic human patient, said method comprising administering to the patient an effective amount of a sulfamate of the following formula (I): ##STR8## wherein X is CH.sub.2 ;

R.sub.1 is hydrogen or lower alkyl; and

R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are independently hydrogen or lower alkyl and R.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5 together are a 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.

13. A method of reducing the frequency or severity of migrainous episodes in a non-epileptic patient, the method comprising administering to the patient a compound consisting of the sulfamate of claim 1 and an imidate group that

(a) masks the sulfamate portion of the sulfamate of claim 1, and

(b) can be removed in a physiological milieu to generate the sulfamate of claim 1.

14. A method of reducing the frequency or severity of migrainous episodes in a non-epileptic patient, the method comprising administering to the patient a sorbopyranose sulfamate, a fructopyranose cyclic sulfite, a fructopyranose cyclic sulfate, a phenylethyl sulfamate, acetazolamide, or methazolamide.
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