Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-08-23
1998-10-27
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514912, A61K 3147
Patent
active
058278621
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of the PCT/JP94/00265, filed on Feb. 22, 1994.
TECHNICAL FIELD
The present invention relates to an agent for prophylaxis or treatment of cataract comprising as an active ingredient a specific carbostyril compound or benzazepine compound, and a method for prophylaxis or treatment of cataract by using the same.
BACKGROUND ART
The carbostyril and benzazepine compounds used as an active ingredient in this invention have already been known. For example, the carbostyril compounds are disclosed in European Patent Publication No. 0382185 (published on Aug. 15, 1990) and U.S. Pat. No. 5,225,402 (issued on Jul. 6, 1993), wherein it is disclosed that these compounds have vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, and platelet aggregation inhibitor. The benzazepine compounds are disclosed in WO 91/05549 (published on May 2, 1991) and U.S. Pat. No. 5,258,510 (issued on Nov. 2, 1993), wherein it is disclosed that the compounds have vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, and platelet aggregation inhibitor. However, it has never been known that the specific carbostyril and benzazepine compounds are effective for the prophylaxis or treatment of cataract.
The present inventors have intensively studied in order to develop a novel agent for prophylaxis or treatment of cataract, and a novel method for prophylaxis or treatment of cataract, and have found that some specific carbostyril compounds and benzazepine compounds are useful in the prophylaxis or treatment of cataract.
Cataract means the condition of the crystalline lens which loses the transparency thereof by storage of water in lens fiber and between lens fibers, or the mass caused by the coagulation of protein, and includes, for example, congenital cataract, or acquired cataracts such as senile cataract, anterior subcapsular cataract, posterior subcapsular cataract, diabetic cataract, cataract accompanying with muscular rigiditic atrophy, irradiation cataract, cataract owing to siderosis, Down's syndrome cataract, Christmas-tree cataract, and the like. Although there are many theories concerning factors causing cataract, for example, disorder in crystalline lens, changes of transparency of lens capsule and lens epithelial, change in ciliary epithelial, i.e. change in chamber water, and the like, it has not been proved yet.
DISCLOSURE OF THE INVENTION
An agent for prophylaxis or treatment of cataract of the present invention comprises as an active ingredient at least one of the compounds selected from a group consisting of a carbostyril compound of the formula: ##STR2## wherein R.sup.1 is a lower alkanoylamino-substituted lower alkoxy group, and the bond between the 3- and 4-positions of the carbostyril nucleus is single bond or double bond, a salt thereof, benzazepine and trahydro-1H-benzazepine.
The "lower alkanoylamino-substituted lower alkoxy group" in the above formula (1) includes a straight chain or branched chain alkoxy group having 1 to 6 carbon atoms which is substituted by a straight chain or branched chain alkanoyl group having 1 to 6 carbon atoms, for example, acetylaminomethoxy, 2-(formylamino)ethoxy, 1-(propionylamino)ethoxy, 3-(butyrylamino)propoxy, 3-(acetylamino)-propoxy, 4-(isobutyrylamino)butoxy, 5-(pentanoylamino)pentyloxy, 6-(hexanoylamino)hexyloxy, and the like.
Among the active compounds (1) of the present invention, the compounds (1) having an acidic group can easily be converted into salts by treating with a pharmaceutically acceptable basic compound. The basic compound includes, for example, alkali metal or alkaline earth metal hydroxides (e.g. sodium hydroxide, potassium hydroxide, lithium hydroxide, calcium hydroxide, etc.), alkali metal carbonates or hydrogen carbonates (e.g. sodium carbonate, sodium hydrogen carbonate, etc.), and alkali metal alcoholates (e.g. sodium methylate, potassium methylate, etc.). Besides, among the active compounds (1) of the present invention, the compounds
Mori Toyoki
Nakamura Shigeki
Ogawa Hidenorii
Onogawa Toshiyuki
Tominaga Michiaki
Fay Zohreh
Otsuka Pharmaceutical Company Limited
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