Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
2000-11-28
2002-01-01
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
C514S650000
Reexamination Certificate
active
06335372
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates in general to a method for the treatment of obsessive compulsive disorder in a mammal. More particularly, this invention relates to a method for the treatment of obsessive compulsive disorder in a mammal by administering to the mammal an effective amount of 1,7,7-trimethylbicyclo[2.2.1]heptane derivative of Formula I
wherein R is hydrogen or methyl, or a pharmaceutically acceptable salt thereof.
Additional objects and advantages of the invention will be set forth in part in the description which follows, and in part will be obvious from the description, or may be learned by practice of the invention. The objects and advantages of the invention will be realized and attained by means of the elements and combinations particularly pointed out in the appended claims.
BACKGROUND OF THE INVENTION
Obsessive Compulsive Disorder (OCD) is a chronic condition associated with obsessional and compulsive features, such as repetitive compulsive behaviour performed in a ritualistic manner and/or recurrent, intrusive, obsessional thoughts. A patient may suffer from OCD as a single disorder, or OCD may be accompanied by an affective disorder, such as depression or other anxiety disorders, such as Generalized Anxiety Disorder (GAD), Social Anxiety Disorder (SAD), Panic Disorder (PD) or agarophobia.
The active ingredients of this invention, (1R,2S,4R)-(−)-2-phenyl 2-(dimethylaminoethoxy)-1,7,7-trimethyl-bicyclo[2.2.1]heptane, known as deramciclane, and (1R,2S,4R)-(−)-2-phenyl-2-(methylaminoethoxy)-1,7,7-trimethyl-bicyclo[2.2.1]heptane, and their pharmaceutically acceptable acid addition salts with inorganic and organic acids generally used for the purpose, fall within the disclosures of U.S. Pat. No. 4,342,762 and International Patent Application No. WO 98/17230, respectively, which are both incorporated herein by reference.
These compounds are selective serotonin 5HT2A- and/or 5HT2C-receptor antagonists. They have shown anxiolytic-like effects in animal test models.
DESCRIPTION OF THE INVENTION
Applicants have surprisingly discovered that the compounds of formula (I) do reduce one or several symptoms of OCD in a mammal. Accordingly, an object of the present invention is a method for treating OCD in a mammal by administering to the mammal an effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Another object of the invention is a method for treating OCD in a mammal by administering to the mammal an effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof together with a benzodiazepine or an antidepressant. The antidepressant may be a tricyclic antidepressant, such as clomipramine, a SSRI, such as fluoxetine or paroxetine, or a SNRI, such as venlafaxine.
For the purposes of this disclosure and claims the term “treatment” is relating to treatment in order to cure or alleviate the disease or its symptoms, and to treatment in order to prevent the development or the exacerbation of the disease or its symptoms.
Pharmaceutically acceptable salts of the compound of Formula (I) can be formed with inorganic acids, e.g. hydrohalogenic acid such as hydrochloride acid or hydrobromic acid, sulfuric acid, phosphoric acid or nitric acid, or organic acids e.g., tartaric acid, succinic acid, malic acid, maleic acid, fumaric acid, citric acid, or lactic acid. Salt with fumaric acid is preferred.
Pharmaceutical compositions containing a compound of Formula (I) or a pharmaceutically acceptable salt thereof as the active ingredient include the usual oral dosage forms, such as tablets, capsules, and liquid preparations. In oral dosage forms, the active ingredient can be mixed with suitable pharmaceutically acceptable excipients, such as starch, lactose, sucrose and magnesium stearate, in accordance with conventional pharmaceutical practice.
The precise amount of the drug to be administered to a mammal for treating or preventing OCD is dependent on numerous factors known to one skilled in the art, such as the compound to be administered, the general condition of the patient, the condition to be treated etc. For example, the usual recommended oral daily dose of deramciclane would be about 5-150 mg, preferably 30-60 mg.
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Jaskari Martti
Lehtonen Leena
Mäki-Ikola Outi
Rouru Juha
Wallin Matti
Finnegan Henderson Farabow Garrett & Dunner L.L.P.
Jarvis William R. A.
Orion Corporation
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