Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-11-24
2002-06-25
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...
C514S465000, C514S539000, C514S567000
Reexamination Certificate
active
06410560
ABSTRACT:
TECHNICAL FIELD
The present invention relates to drug compositions for relieving pain and promoting the removal of calculi in urolithiasis. The drug compositions of this invention contain active ingredients having stimulating effects on both &bgr;
2
- and &bgr;
3
-adrenoceptors.
BACKGROUND OF THE INVENTION
It is known that three subtypes of &bgr;-adrenoceptor, which have been classified as &bgr;
1
, &bgr;
2
and &bgr;
3
are present in the human body. Each receptor subtype is distributed in specified organs. &bgr;
1
-Adrenoceptor is mainly present in the heart and its stimulation enhances the function of the heart. &bgr;
2
-Adrenoceptor is mainly present in the trachea, peripheral blood vessels and the uterus. Smooth muscle of such organs is relaxed by the stimulation of this receptor. In addition, it has recently been reported that &bgr;
3
-adrenoceptor is present in the digestive tract and adipocytes. The stimulation of &bgr;
3
-adrenoceptor leads to the relaxation of gastrointestinal smooth muscle, lipolysis and energy expenditure in adipose tissues and so on.
Thus, the distribution of &bgr;-adrenoceptor subtypes is specified by organs and tissues. Various receptor subtypes including &bgr;-adrenoceptor have been actively studied for developing more effective medicinal treatment of some diseases. Consequently, efforts have been paid extensively to develop more effective and highly selective drugs that act upon a specified organ. However, &bgr;-adrenoceptor subtypes distributed in human ureter have not yet been elucidated, although the progress of studies to develop drugs that act more effectively on human ureter has been desired.
Urolithiasis is a disease generating calculi in the lumen of the entire urinary tract from kidney to urethra. The calculi is thought to be formed in a series of events such as nucleation of urinary component, crystallization, aggregation, concretion and enlargement. Urinary flow is often obstructed by calculi, which results in the rise of intra-ureteral pressure leading to pain. An analgesic and an antispastic are prescribed for the pain. However, the use of the analgesic is only temporary symptomatic therapy for the pain, and is not expected to fundamentally treat urolithiasis. The effectiveness of an anti-cholinergic, one of the antispastics, is also not satisfactory. Therefore, drugs which can relieve pain and promote the removal of calculi by widening the ureter due to strong relaxing effects are desired (The Journal of Urology, Vol. 152, pp. 1095-1098 (1994)).
SUMMARY OF THE INVENTION
The present inventors have extensively studied drug effects on the human ureter in order to elucidate the &bgr;-adrenoceptor subtypes distributed therein. As a result, it has been surprisingly found that &bgr;
3
-adrenoceptor in addition to &bgr;
2
-adrenoceptor was present in human ureter, thereby forming the basis of the present invention.
Accordingly, the present invention is to provide novel drugs for relieving pain and for promoting the removal of calculi in urolithiasis. Useful drugs of this invention contain active ingredients which exert a strong relaxing effect on human ureteral smooth muscle by stimulating both &bgr;
2
- and &bgr;
3
-adrenoceptors.
REFERENCES:
Galitzky et al, American Journal of Physiology, vol. 264, No. 3, Part 1, pp. E403-E412, 1993.*
Medline abstract, AN 96165630, Morita, T. et al (Aug. 1995).
HCAPLUS abstract, AN 1989:400644, Morita T. (1989).
Melchior, H., Spasmolysis through Beta-adrenergic Drugs, vol 10, No. 4, pp. 183-188 (1971).
Morita, T., Urol. Int., vol. 45, No. 1, pp. 10-15 (1990).
Longrigg, J.N., J.R. Coll. Surg. Edinburg, vol. 22, No. 5, pp. 309-318, XP-002085648 (Sep. 1977).
Lindsey et al, Urol. Res., vol. 7, No. 1, pp. 13-17 (1979).
Blooch et al, Urol. Int. vol. 39, No. 5, pp. 308-311 (1984), XP-002085650.
Akahane Masuo
Tomiyama Yoshitaka
Frenkel Stuart D.
Jarvis William R. A.
Kissei Pharmaceutical Co. Ltd.
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