Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-12-29
1998-01-06
Nutter, Nathan M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514323, 514374, 514378, 514385, 514406, 514414, 514415, 548504, 548505, A01N 4342
Patent
active
057055068
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP 93/01077 filed May 3, 1993.
The present invention relates to a pharmaceutical composition containing as active ingredient a compound having selective agonist activity at 5HT.sub.1 -like receptors, in particular a composition for rectal administration.
5-HT.sub.1 -like receptors are located, for example, in the dog saphenous vein and the 5-HT.sub.1 -like receptor agonists with which the present invention is concerned contract the dog saphenous vein. Such compounds may therefore be identified by their contractile effect on the dog isolated saphenous vein strip as described, for example, by Apperley et al., Br. J. Pharmacol, 68, 215-224 (1980). Compounds which are selective 5-HT.sub.1 -like receptor agonists have also been found to selectively constrict the carotid arterial bed of the anaesthetised dog.
A variety of compounds which selectively constrict the dog isolated saphenous vein strip and which constrict the carotid arterial bed of the anaesthetised dog have been described in the art. These include indole derivatives such as those disclosed inter alia in published British Patent Specifications Nos. 2082175, 2081717, 2083463, 2124210, 2150932, 2162522, 2168347, 2168973, 2185020, 2186874, 2191488, 2208646, published European Patent Specifications Nos. 147107, 237678, 242939, 244085, 225726, 254433, 303506, 313397, 354777, 382570, 464558, 506363, 506369, 450238, 451022, 451008, 478954, 438230, 494774, 497512, 501568 and published International patent application Nos. WO92/11013, WO92/11014, WO92/06973, WO93/00086. WO92/13856, WO93/00094, WO91/18897 and WO93/00333. The compounds disclosed in the specifications (hereinafter described as compounds A) are useful in the treatment of migraine and cluster headache.
Oral administration constitutes the generally preferred route for administration of pharmaceuticals since this route is particularly convenient and acceptable to patients. Unfortunately oral compositions may be associated with certain disadvantages, particularly in the treatment of conditions such as migraine which may be accompanied by nausea and/or vomiting. Furthermore, migraine is associated with delayed gastric emptying which may lead to both a delay and an impairment of drug absorption following oral administration. It is highly desirable, particularly in the treatment of acute conditions such as migraine, that pharmaceutical compositions have a rapid and consistent onset of action combined with sustained activity and good bioavailability. Rapid absorption can be achieved by parenteral injection but this is unacceptable to some patients, particularly if the drug is to be administered without direct medical supervision, i.e. self-administered.
The present invention provides a pharmaceutical composition for rectal administration which comprises a compound which acts as a 5HT.sub.1 -like receptor agonist in the form of its free base or a physiologically acceptable solvate thereof as active ingredient, together with one or more pharmaceutically acceptable carriers or excipients.
In a preferred embodiment of the invention we provide a pharmaceutical composition for rectal administration which comprises one or more of compounds A in the form of its free base or a pharmaceutically acceptable solvate thereof as active ingredient.
Compositions according to the invention are preferably in a form adapted for use in medicine, in particular human medicine.
Particularly preferred compounds for use in the compositions of the present invention are N-methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulphonamide, especially may be represented by the formula (I) ##STR1## and its physiologically acceptable salts and solvates are disclosed in GB 2162522. The compound of formula (I) is described as useful in treating and/or preventing pain resulting from dilatation of the cranial vasculature, in particular migraine.
Numerous clinical studies have demonstrated the effectiveness of the compound of formula (I) in migraineurs. Hitherto, the drug has always been administered in the fo
REFERENCES:
patent: 4785016 (1988-11-01), Evans et al.
patent: 4994483 (1991-02-01), Oxford et al.
patent: 5037845 (1991-08-01), Oxford
Arnold, Neurol. Neurochir. Pol., 26, No. S.2, 1992, 49-56.
Klapper, Headache Quart., 2, No. 2, 1991, 83-90.
Merlet Nadine
Richard Isabelle
Thielemans Isabelle
Laboratoires Glaxo SA
Nutter Nathan M.
Truong Duc
LandOfFree
Pharmaceutical compositions of alkylsulphonamides 5HT1 agonists does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical compositions of alkylsulphonamides 5HT1 agonists , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical compositions of alkylsulphonamides 5HT1 agonists will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2329369