Antiviral agent containing benzodithiin derivative as active ing

Details Antiviral agent containing benzodithiin derivative as active ing Antiviral agent containing benzodithiin derivative as active ing

1996-12-16

1997-12-16

Dees, Jose G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549 20, 549 21, A61K 31385, C07D33908

Patent

active

056985800

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP95/01107 filed Jun. 6, 1995.


TECHNICAL FIELD

The present invention relates to an antiviral agent containing a 1,4-dihydro-2,3-benzodithiin derivative or a pharmacologically acceptable salt thereof as an active ingredient, and to a 1,4-dihydro-2,3-benzodithiin derivative which is the active ingredient of said antiviral agent. More particularly, the present invention relates to an antiviral agent efficacious for the preventive or therapeutic treatment of vital diseases represented by respiratory diseases such as oropharyngolaryngitis, inflammation of lower airway, bronchitis, bronchiolitis, croup and the like, which are caused by RS virus (Respiratory Syncytial virus).


BACKGROUND ART

As pharmaceutical agents useful for the therapy of vital diseases, there guanine derivative), ganciclovir (a guanine derivative), idoxuridine (2'-deoxy-5-iodouridine) and vidarabine (an adenine derivative)!, !-decane), and the like. Meanwhile, Ribavirin which is a nucleic acid analog is used as an antiviral agent against RS virus which causes severe respiratory diseases in infants.
Yet, a pharmaceutical agent has not been developed, which exhibits sufficient therapeutic effects on vital diseases and which is associated with less toxicity and less side-effects. For example, Ribavirin, though effective against RS virus, has high toxicity and cannot be administered orally but only locally by inhalation. Ribavirin has been recognized to be teratogenic, carcinogenic and mutagenic, and is associated with difficulty in clinical application. Therefore, an antiviral agent has been desired, which shows clinically sufficient therapeutic effects and is associated with less toxicity and less side-effects.
It is therefore an object of the present invention to provide an antiviral agent having superior antiviral activity and less toxicity and less side-effects.


DISCLOSURE OF THE INVENTION

Accordingly, the present invention provides the following.
(1) Antiviral agents comprising, as an active ingredient, a sometimes referred to briefly as 1,4-dihydro-2,3-benzodithiin derivative (I)! ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each a hydrogen atom, an optionally substituted lower alkyl, an optionally substituted lower alkenyl, an optionally substituted aryl, an optionally substituted aralkyl, a nitro, a cyano, a carboxy, an alkoxycarbonyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, an arylsulfonyl, a sulfamoyl, a carbamoyl, an acyl, a hydrazino, a halogen atom, a group of the formula: OR.sup.5, a group of the formula: SR.sup.5 or a group of the formula: NR.sup.6 R.sup.7 optionally substituted lower alkenyl or optionally substituted aryl, and R.sup.6 and R.sup.7 are each hydrogen atom, optionally substituted lower alkyl, optionally substituted lower alkenyl or optionally substituted aryl, or
(2) 1,4-Dihydro-2,3-benzodithiin derivatives of the formula (II) ##STR3## wherein R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are each an optionally substituted lower alkyl or a halogen atom.
(3) Pharmaceutical compositions for therapy of viral diseases, which comprises, as an active ingredient, the 1,4-dihydro-2,3-benzodithiin derivative of the formula (I) of (1) or a pharmacologically acceptable salt thereof.
(4) Methods for treating viral dishes, which comprise administering to patients a pharmaceutically effective amount of the 1,4-dihydro-2,3-benzodithiin derivative of the formula (I) of (1) or a pharmacologically acceptable salt thereof.
(5) Use of the 1,4-dihydro-2,3-benzodithiin derivative of the formula (I) of (1) or a pharmacologically acceptable salt thereof for the therapy of viral diseases.
(6) Use of the 1,4-dihydro-2,3-benzodithiin derivative of the formula (I) of (1) or a pharmacologically acceptable salt thereof for the production of a pharmaceutical composition for the therapy of viral diseases.
In the above-mentioned formulas (I) and (II), each symbol denotes the following.
The lower alkyl at R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.s

REFERENCES:
patent: 3682953 (1972-08-01), Sestanj
patent: 3845047 (1974-10-01), Egli et al.

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