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Summary for Patent: 4,513,006
|Title:||Anticonvulsant sulfamate derivatives|
|Abstract:||Sulfamates of the following formula (I): ##STR1## wherein X is O or CH.sub.2 and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.|
|Inventor(s):||Maryanoff; Bruce E. (New Hope, PA), Gardocki; Joseph F. (Doylestown, PA)|
|Assignee:||McNeil Lab., Inc. (Fort Washington, PA)|
|Patent Litigation and PTAB cases:||See patent lawsuits and PTAB cases for patent 4,513,006|
1. A sulfamate of the following formula (I): ##STR11## wherein X is oxygen;
R.sub.1 is hydrogen or 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 may be a group of the following formula (II): ##STR12## 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 sulfamate 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 sulfamate of claim 1, wherein said alkyl group for 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 sulfamate of claim 1, wherein said sulfamate of formula (I) is selected from the group consisting of:
5. The sulfamate of claim 4, wherein said sulfamate is 2,3:4,5-bis-O-(1-methylethylidene)-.beta.-D-fructopyranose sulfamate.
6. A pharmaceutical composition effective for the treatment of convulsions comprising an anticonvulsantly effective amount of a sulfamate of claim 1 and a pharmaceutically-acceptable carrier.
7. The pharmaceutical composition of claim 6, wherein said sulfamate is present in a unit dosage amount of about 10 to 500 milligrams of the sulfamate.
8. A method for the treatment of convulsions in a mammal which comprises administering to the mammal, the pharmaceutical composition of claim 6.
9. The sulfamate of claim 4, wherein said sulfamate is
10. The sulfamate 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).
11. The sulfamate of claim 1, wherein the sulfamate of formula (I) is a fructopyranose.
12. The sulfamate of claim 1, wherein in formula (I), R.sub.1 is hydrogen.
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