Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-02-18
2001-11-27
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S455000, C514S459000, C514S463000
Reexamination Certificate
active
06323236
ABSTRACT:
TECHNICAL FIELD
The present invention generally relates to the use of drugs for the treatment of mental disorders. More specifically, the invention describes methods for the treatment and prevention of Impulse Control Disorders (ICD's) by administering sulfamate derivatives.
BACKGROUND OF THE INVENTION
Sulfamate derivatives having useful pharmaceutical activity in the areas of epilepsy, glaucoma, peptic ulcers and male infertility are disclosed in U.S. Pat. Nos. 4,075,351, 4,513,006, 4,591,601, 4,792,569, and 5,760,007. One of these compounds 2,3:4,5-bis-O-(1-methylethylidene)-beta-D-fructopyranose sulfamate known as topiramate has been demonstrated in clinical trials of human epilepsy to be effective as adjunctive therapy or as monotherapy in treating simple and complex partial seizures and secondarily generalized seizures and is currently marketed for the treatment of simple and complex partial seizure epilepsy with or without secondary generalized seizures.
Binge eating disorder (BED) is characterized by discrete periods of binge eating during which large amounts of food are consumed in a discrete period of time and a sense of control over eating is absent. Persons with bulimia nervosa have been reported to have electroencephalographic abnormalities and to display reduced binge eating in response to the anti-epileptic drug phenytoin. Also, in controlled trials in patients with epilepsy, topiramate was associated with suppression of appetite and weight loss unreleated to binge eating.
Binge eating disorder is a subset of a larger classification of mental disorders broadly defined as Impulse Control Disorders (ICDs) characterized by harmful behaviors performed in response to irresistible impulses. It has been suggested that ICDs may be related to obsessive-compulsive disorder or similarly, maybe forms of obsessive-complusive disorders. It has also been hypothesized that ICDs may be related to mood disorder or may be forms of affective spectrum disorder, a hypothesized family of disorders sharing at least one common physiologic abnormality with major depression. In the Diagnostic and Statistical Manual of Mental Disorders (DSM-IV), the essential feature of an ICD is the failure to resist an impulse, drive, or temptation to perform an act that is harmful to the person or to others. For most ICDs, the individual feels an increasing sense of tension or arousal before committing the act, and then experiences pleasure, gratification, or release at the time of committing the act. After the act is performed, there may or may not be regret or guilt. ICDs are listed in a residual category, the ICDs Not Elsewhere Classified, which includes intermittent explosive disorder (IED), kleptomania, pathological gambling, pyromania, trichotillomania, and ICD not otherwise specified (NOS). Examples of ICDs NOS are compulsive buying or shopping, repetitive self-mutilation, nonparaphilic sexual addictions, severe nail biting, compulsive skin picking, personality disorders with impulsive features, attention deficit/hyperactivity disorder, eating disorders characterized by binge eating, and substance use disorders.
SUMMARY OF THE INVENTION
It is an object of the present invention to describe the use of sulfamate derivatives for the treatment of Impulse Control Disorders.
The present invention comprises methods for the treatment or prevention of Impulse Control Disorders using the compounds of formula (I), pharmaceutical compositions containing one or more of the compounds of formula (I), or pharmaceutical compositions containing one or more of the compounds of formula (I) in addition to a safe and effective amount of one or more additional agents to treat related symptoms and conditions.
DETAILED DESCRIPTION OF THE INVENTION
The sulfamates of use in the present invention are of the following formula (I):
wherein
X is CH
2
or oxygen;
R
1
is hydrogen or alkyl; and R
2
, R
3
, R
4
and R
5
are independently hydrogen or lower alkyl and, when X is CH
2
, R
4
and R
5
may be alkene groups joined to form a benzene ring and, when X is oxygen, R
2
and R
3
and/or R
4
and R
5
together may be a methylenedioxy group of the following formula (II):
wherein
R
6
and R
7
are the same or different and are hydrogen, lower alkyl or are alkyl and are joined to form a cyclopentyl or cyclohexyl ring. R
1
in particular is hydrogen or alkyl of about 1 to 4 carbons, such as methyl, ethyl and iso-propyl. Alkyl throughout this specification includes straight and branched chain alkyl. Alkyl groups for R
2
, R
3
, R
4
, R
5
, R
6
and R
7
are of about 1 to 3 carbons and include methyl, ethyl, iso-propyl and n-propyl. When X is CH
2
, R
4
and R
5
may combine to form a benzene ring fused to the 6-membered X-containing ring, i.e., R
4
and R
5
are defined by the alkatrienyl group ═C—CH═CH—CH═.
A particular group of compounds of formula (I) is that wherein X is oxygen and both R
2
and R
3
and R
4
and R
5
together are methylenedioxy groups of the formula (II), wherein R
6
and R
7
are both hydrogen, both alkyl or combine to form a spiro cyclopentyl or cyclohexyl ring, in particular where R
6
and R
7
are both alkyl such as methyl. A second group of compounds is that wherein X is CH
2
and R
4
and R
5
are joined to form a benzene ring. A third group of compounds of formula (I) is that wherein both R
2
and R
3
are hydrogen.
The compounds of formula I: may be made by the processes disclosed in U.S. Pat. Nos. 4,075,351, 4,513,006, 4,591,601, 4,792,569, 5,242,942, 5,387,700, which are incorporated in their entirety herein by reference.
The compounds of formula I include the various individual isomers as well as the racemates thereof. For treating ICDs, a compound of formula (I) may be employed at a daily dosage in the range of about 15 to 1400 mg administered orally, for an average adult human.
To prepare the pharmaceutical compositions of this invention, one or more sulfamate compounds of formula (I) are intimately admixed with a pharmaceutical carrier according to conventional pharmaceutical compounding techniques, which carrier may take a wide variety of forms depending on the form of preparation desired for administration, e.g., oral, by suppository, or parenteral. In preparing the compositions in oral dosage form, any of the usual pharmaceutical media may be employed. Thus, for liquid oral preparations, such as for example, suspensions, elixirs and solutions, suitable carriers and additives include water, glycols, oils, alcohols, flavoring agents, preservatives, coloring agents and the like; for solid oral preparations such as, for example, powders, capsules and tablets, suitable carriers and additives include starches, sugars, diluents, granulating agents, lubricants, binders, disintegrating agents and the like. Because of their ease in administration, tablets and capsules represent the most advantageous oral dosage unit form, in which case solid pharmaceutical carriers are obviously employed. If desired, tablets may be sugar coated or enteric coated by standard techniques. Suppositories may be prepared, in which case cocoa butter could be used as the carrier. For parenterals, the carrier will usually comprise sterile water, though other ingredients, for example, for purposes such as aiding solubility or for preservation, may be included. Injectable suspensions may also be prepared in which case appropriate liquid carriers, suspending agents and the like may be employed. Topiramate is currently available for oral administration in round tablets containing 25 mg, 100 mg or 200 mg of active agent. The tablets contain the following inactive ingredients: lactose hydrous, pregelatinized starch, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, purified water, carnauba wax, hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol, synthetic iron oxide, and polysorbate
80
.
The pharmaceutical compositions herein will contain, per dosage unit, e.g., tablet, capsule, powder injection, teaspoonful, suppository and the like from about 5 to about 1000 mg of
Frost Brown Todd LLC
Jarvis William R. A.
University of Cincinnati
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