Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Para-n-benzene - sulfoxy-n containing doai – and said benzene...
Patent
1988-12-28
1991-06-25
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Para-n-benzene - sulfoxy-n containing doai, and said benzene...
514604, A01N 5100, A01N 4106
Patent
active
050266900
DESCRIPTION:
BRIEF SUMMARY
The invention relates to an antiviral agent, especially for measures against enclosed viruses, such as herpes viruses, having a content of sulphonamide derivatives of 4,4'-diaminostilbene disulphonic acid-2,2', and/or of 4,4'-diaminodiphenylethane disulphonic acid-2,2', the use of these derivatives for the treatment and prevention of virus diseases, especially of diseases caused by enclosed viruses, such as herpes virus, as well as the use of these derivatives for the preparation of an antiviral agent.
Such sulphonamide derivatives of the general formula ##STR1## wherein X represents the group --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, Z represents chlorine or bromine, Me represents a non-toxic cation, preferably alkali or ammonium, and R.sub.1 and R.sub.2 which may be the same or different represent hydrogen or the 3,4-dihalogenobenzene sulphonyl group are known from DE-PS 24 33 723. These products absorb radiation (especially UV-radiation), have a protein coagulating effect, and are used as active substance in skin protecting agents.
These sulphonamide derivatives which derive from the 4,4'-diaminostilbene disulphonic acid-2,2' and its analogon with the stilbene double-bond being hydrogenated, the 4,4'-diaminodiphenyleth disulphonic acid-2,2', are produced by condensation of the starting products 4,4'-diaminostilbene disulphonic acid-2,2' or 4,4'-diaminodiphenylethane disulphonic acid-2,2' in the form of their salts or their N,N'-monosubstituted derivatives in aqueous solution either with 1-chlorosulphonyl-4-acetaminobenzene or with 1-chlorosulphonyl-4-carbethoxi aminobenzene respectively the N-substituted derivatives of these compounds, subsequent deliberation of the terminal primary or secondary amino group by hydrolysis and final reaction of these saponification products with 1-chlorosulphonyl-3,4-dihalogenobenzene, preferably with 3,4-dichlorobenzene sulphonyl chloride. It is preferred to use for the reaction the water-soluble salts of the starting products, especially the calcium or sodium salts. The final products in which Me represents a non-toxic cation, preferably alkali, such as sodium or ammonium, are received, if necessary, from the soluble salts with other cations (e.g.,the calcium salts) by reacting with sodium carbonate, -bicarbonate or ammonium oxalate.
Surprisingly, it has been found that the above mentioned sulphonamide derivatives have a high virucidal and antiviral effect, especially against viruses provided with an enclosure, further called "enclosed" viruses, without evolving cytotoxic side effects.
Typical examples of such "enclosed" viruses are the herpes viruses, especially herpes simplex, but the varicella zoster viruses as well.
On the basis of the therapy measures today available, diseases caused by herpes simplex viruses, such as herpes labialis and herpes genitalis, can be treated only with very unsatisfying results (Wassilew Sawko W., Moglichkeiten und Grenzen der Chemotherapie bei Erkrankungen durch das Herpes-simples- und Varicella-Zoster-Virus, Der Hautarzt, 34, 1 to 5, (1983); Wassilew, Sawko W., Virustatika in der Dermatologie Der Hautarzt, 37, 259-262, (1986), Ring, J., Frohlich, H.H., Wirkstoffe in der dermatologischen Therapie, 140 to 143, Springer Verlag (1985)).
Most of the products used so far, proved to be ineffective or showed unacceptable side effects in clinical studies. Primarily these side effects are toxic influences on the host cell affected by the virus, but as well, e.g., the initiation of allergies (see Wassilew, Sawko, indicated above).
Thus the object of the invention is the preparation of an effective antiviral agent which is suitable especially for the treatment and prevention of diseases caused by enclosed viruses, such as herpes simplex viruses of type 1 and 2, and which shows no, or at least negligible side effects
This object is achieved by an agent containing as active substance the sulphonamide derivatives mentioned in the beginning. In other words, the object is achieved by using the a.m. special sulphonamide derivatives for the treatment of
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patent: 4034110 (1977-07-01), Mitrovic
patent: 4870107 (1989-09-01), Yoshimoto
Banthell, E., CA 107:197789w, 1987.
Schmid, Otto, CA 84:150378c, 1976.
Komp Bernd
Kresken Joachim
Stockhausen Dolf
Chemische Fabrik Stockhausen GmbH
Friedman Stanley J.
Travers Russell
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