Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1990-07-20
1992-10-13
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514365, 514371, 514438, 514622, 544 584, 548195, 548200, 549 77, 564177, C07D27706, A61K 31425
Patent
active
051551063
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel cysteamine derivative and an antirheumatic agent containing the novel cysteamine derivative.
BACKGROUND ART
Steroids, acidic anti-inflammatory agents, and the like have been used for the therapy of rheumatism.
DISCLOSURE OF THE INVENTION
Steroids, however, involve various undesirable side-effects, and acidic anti-inflammatory agents remain nosotropic. Accordingly, there is a strong demand for a truly effective therapeutic agent.
The inventors of the present invention synthesized various cysteamine derivatives, extensively studied their physiological activities, and found that the cysteamine derivative in accordance with the present invention suppresses adjuvant arthritis, which is an animal experimental model for the rheumatism, to complete the present invention.
Therefore, an object of the present invention is to provide a novel cysteamine derivative and an antirheumatic agent containing such a cysteamine derivative.
The present invention, which accomplishes the aforesaid object, provides a cysteamine derivative represented by general formula (I): ##STR7## wherein R.sub.1 represents a straight-chain or a branched alkyl radical having 1 to 6 carbon atoms, R.sub.2 represents hydrogen atom or n-propyl radical, and X represents a radical selected from the group consisting of radicals containing cysteamine moiety (N S) represented by formula (II): ##STR8## formula (III): ##STR9## formula (IV): ##STR10## formula (V): ##STR11## or formula (VI): ##STR12## wherein R.sub.2 represents hydrogen atom or a straight-chain or a branched alkyl group having 1 to 10 carbon atoms.
The present invention also provides an antirheumatic agent containing a cysteamine derivative represented by general formula (I): ##STR13## wherein R.sub.1 represents a straight-chain or a branched alkyl radical having 1 to 6 carbon atoms, R.sub.2 represents hydrogen atom or n-propyl radical, and X represents a radical selected from the group consisting of radicals containing cysteamine moiety (N S) represented by formula (II): ##STR14## formula (III): ##STR15## formula (IV): ##STR16## formula (V): ##STR17## or formula (VI): ##STR18## wherein R.sub.2 represents hydrogen atom or a straight-chain or a branched alkyl group having 1 to 10 carbon atoms.
The cysteamine derivative in accordance with the present invention which is represented by the above-mentioned formula (I) is produced by a condensation reaction and a protective group-removing reaction between a derivative of a carboxylic acid represented by the following formula (VII): ##STR19## wherein R.sub.1 represents a straight-chain or a branched alkyl group containing 1 to 6 carbon atoms, R.sub.2 represents hydrogen atom or n-propyl group, and R.sub.3 represents hydrogen atom or methoxymethyl group and an amine derivative represented by the following formula (VIII): ##STR20## formula (IX): ##STR21## formula (X): ##STR22## formula (XI): ##STR23## or formula (XIII) ##STR24## wherein R.sub.2 represents hydrogen atom or a straight-chain or a branched alkyl group having 1 to 10 carbon atoms.
The cysteamine derivative of the present invention is used particularly for an antirheumatic agent, and is administered in a dose ranging from 10 to 2,000 mg per day, preferably from 20 to 600 mg per day in the case of an adult, although the dose may vary in accordance with the symptom. Such a dose of the antirheumatic agent is administered either at once or in two or three times a day as desired in accordance with the symptom. The administration may be carried out by any suitable method, and preferably, by oral administration. Intravenous injection may also be employed.
The compound of the present invention is employed either alone or as a mixture with another pharmaceutical carrier or vehicle as the only effective component or as one of effective components to form tablets, sugar-coating tablets, powders, capsules, granules, suspensions, emulsions, injections, and other pharmaceutical preparations. Examples of the carriers and vehicles include calc
REFERENCES:
patent: 3455940 (1969-07-01), Stecker
patent: 3917617 (1975-11-01), Razdan et al.
patent: 3985891 (1976-10-01), Kutter
Chemical Abstracts 82(1) 4251y RN 53930-87-3.
Inoue Kazuhito
Kohama Hiromasa
Koyama Shingo
Nanba Ryoichi
Shimizu Masaki
Gerstl Robert
Terumo Kabushiki Kaisha
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