Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-08-26
2000-05-09
Jones, Dwayne C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
548490, 548491, A01N 4338
Patent
active
060604980
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to a composition containing N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide which is an antitumor agent.
PRIOR ART
N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide is an antitumor agent, which terminates multiplication of tumor cells by a novel mechanism of action. The excellent effects of the antitumor agent has been demonstrated by experiments on animals. A group of the compounds encompassing the compound of the present invention is disclosed in JP-A-7-165708. On the other hand, various methods for administering an antitumor agent are known, among which oral administration is generally regarded as the easiest to dose and the least troublesome for a patient. However, oral administration cannot always be applied depending on degrees of progression of the disease of a patient or sites of formation of tumors, so that it often becomes inevitable to form an antitumor agent into a preparation for injection.
N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide is a compound which is sparingly soluble in water. The compound is substantially insoluble in water at a pH around the range of 5 to 7, at which a preparation for injection is commonly used. In general, it is necessary to dissolve a pharmaceutical substance in water for forming a preparation for injection. Therefore, it is very difficult to form the compound of the present invention into a preparation for injection. The inventors of the present invention have intensively studied to obtain an aqueous solution of N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide. As a result of the studies, they have found that an aqueous solution which is safe and stable for a long period and also a preparation for injection thereof can be obtained by the means as described below. The present invention has been accomplished on the basis of this finding.
DISCLOSURE OF THE INVENTION
The present invention relates to a composition containing N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide, which is characterized in that the composition contains N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide and a basic substance and will provide an aqueous solution having a pH of 7 or higher when dissolved in water.
In other words, the present invention provides a pharmaceutical composition containing N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide in a pharmacologically effective dose and a basic substance and providing an aqueous solution having a pH of 7 or higher when dissolved in water.
The basic substance is preferably at least one selected from the group consisting of meglumine, sodium carbonate, monoethanolamine and sodium hydroxide.
Furthermore, the present invention also provides a use of N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide and a basic substance for producing an injection of an antitumor agent.
DETAILED DESCRIPTION OF THE INVENTION
N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide is a novel sulfonamide derivative having a bicyclic heterocycle, which is a compound exhibiting an excellent antitumor activity based on the mechanism of action and having a low toxicity. The compound (hereinafter sometimes referred to as the present compound) is represented by the following structural formula. ##STR1##
The synthesis of the present compound can be carried out according to the process disclosed in JP-A-7-165708. For example, the present compound can be synthesized as follows. After dissolving 264 mg (2 mmol) of 7-amino-1H-indole in pyridine, 767 mg (3 mmol) of 4-sulfamoylbenzenesulfonyl chloride is added thereto under stirring at room temperature. After the mixture is stirred overnight at room temperature, the solvent is evaporated under reduced pressure. Ethyl acetate and 0.2 N hydrochloric acid are added to the resulting residue. The organic layer is separated, washed with water, and dried over magnesium sulfate, followed by evaporation of the solvent. The resulting residue is purified by silica gel column chromatography to give 445 mg of N-(1H-i
REFERENCES:
patent: 4416874 (1983-11-01), Kaplan et al.
Abstract to Yoshino et al. of J07165708, Jun. 1995.
Ando Hidenobu
Ashizawa Kazuhide
Eisai Co. Ltd.
Jones Dwayne C.
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