Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Utility Patent
1999-07-09
2001-01-02
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...
C514S456000
Utility Patent
active
06169098
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a composition which comprises a first component (a) which is (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is paroxetine, or a pharmaceutically acceptable salt and/or solvate thereof The present invention also relates to a process for the preparation of the inventive composition, pharmaceutical formulations containing said composition and to the use of said composition either by concomitant administration or by separate administration as an improvement of the treatment of affective disorders such as depression, anxiety, obsessive compulsive disorder (OCD), etc.
BACKGROUND OF THE INVENTION
Today, it is generally considered that antidepressants take 2-4 weeks to reach full clinical effect. In contrast, the side effects occur immediately. Thus, slow onset of action of antidepressants leads to a vulnerable period for patients in which they experience the side effects, but not the therapeutic effects of drugs. There is often a heavy burden on the treating physician to persuade the patient to continue with the treatment during this period. Furthermore, in suicidal patients, as the onset of action is gradual, initiative may be regained without the experiencing of full reversal of symptoms, leaving a window of risk for suicide and a frequent requirement for hospitalization. An antidepressant with fast onset of action would not only be beneficial due to the faster symptom reduction, but would also be more acceptable to patients and physicians and reduce the need for, and duration of, hospitalization. The same long period to reach full clinical effect has been shown in the treatment of other affective disorders such as anxiety and OCD.
PRIOR ART
In WO 96/33710 is disclosed that the compound (R)-5-carbamoyl-8-fluoro-3-N,N-dicyclobutylamino-3,4-dihydro-2H-1-benzopyran, which has high affinity to 5-HT receptors and antagonizes 5-HT
IA
-mediated responses, induces a rapid improvement of depressed patients treated with serotonin reuptake inhibitors.
SUMMARY OF THE INVENTION
The present invention is directed to a new composition comprising a first component (a) which is the specific 5-HT
IA
antagonist (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate (NAD 299) and a second component (b) which is paroxetine, in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof Said composition attains a faster onset of action and, consequently, provides a more efficacious treatment of patients suffering from affective disorders, particularly depression.
REFERENCES:
patent: 4698342 (1987-10-01), Crosby
patent: 5616610 (1997-04-01), Evenden et al.
patent: WO 95/11891 (1995-05-01), None
Artigas et al, Arch. Gen. Psychiatry, vol. 51, pp. 248-251, 1994.*
Evenden John
Thorberg Seth-Olov
Astra Aktiebolag
Jarvis William R. A.
White & Case LLP
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