JP2548223B2 - Kidney disease treatment - Google Patents
Kidney disease treatmentInfo
- Publication number
- JP2548223B2 JP2548223B2 JP62213804A JP21380487A JP2548223B2 JP 2548223 B2 JP2548223 B2 JP 2548223B2 JP 62213804 A JP62213804 A JP 62213804A JP 21380487 A JP21380487 A JP 21380487A JP 2548223 B2 JP2548223 B2 JP 2548223B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- kidney disease
- disease treatment
- renal diseases
- present
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】 ＜産業上の利用分野＞ 本発明は,2−フェニル−1,2−ベンゾイソセレナゾー
ル−３（2H）−オン（以下，化合物Ａと称す）又はその
生理学的許容塩を有効成分とする腎臓疾患の予防及び治
療剤に関する。DETAILED DESCRIPTION OF THE INVENTION <Industrial field of application> The present invention relates to 2-phenyl-1,2-benzisoselenazol-3 (2H) -one (hereinafter referred to as compound A) or its physiological tolerance. The present invention relates to a preventive and / or therapeutic agent for kidney diseases, which contains salt as an active ingredient.
＜従来の技術＞ 腎臓疾患に対し治療効果が確認されている薬剤を大別
するとステロイド環構造体，免疫抑制剤，抗血液凝固
剤，抗血小板剤，非ステロイド性抗炎症剤，利尿剤及び
線溶剤となる。これらの薬剤はそれぞれの特徴に基づき
臨床に使用され，治療に多大な貢献をしている。しかし
ながら，これらの薬剤は未だ臨床的に十分満足できるも
のではない。近年，腎臓疾患の成因及び病態解析が進
み，作用機序が明確になるにつれ腎臓疾患の治療効果が
より明確で，副作用の少ない薬剤の開発が望まれてい
る。<Prior Art> Drugs that have been confirmed to have therapeutic effects on renal diseases are roughly classified into steroid ring structures, immunosuppressants, anticoagulants, antiplatelets, nonsteroidal anti-inflammatory agents, diuretics and lines. It becomes a solvent. These drugs are clinically used based on their characteristics and make a great contribution to treatment. However, these drugs are not yet clinically satisfactory. In recent years, as the etiology and pathological condition of renal diseases have been advanced and the mechanism of action has been clarified, it has been desired to develop a drug having more clear therapeutic effect on renal diseases and less side effects.
化合物Ａの薬理活性についてはグルタチオンペルオキ
シダーゼ様抗酸化作用及び抗炎症作用が知られている
（バイオケミカル ファーマコロジー33,NO.20,3235〜3
239（1984）及び33,NO.20,3241〜3245（1984））。しか
しながら，かかる作用は腎臓疾患の予防及び治療効果と
結びつくものではない。Regarding the pharmacological activity of Compound A, glutathione peroxidase-like antioxidant activity and anti-inflammatory activity are known (Biochemical Pharmacology 33 , NO.20, 3235-3).
239 (1984) and 33 , NO.20, 3241 to 3245 (1984)). However, such effects are not associated with the preventive and therapeutic effects of renal diseases.
＜発明が解決しようとする問題点＞ 本発明者等は，化合物Ａの薬理活性について鋭意検討
した結果，化合物Ａが優れた腎臓疾患の予防及び治療効
果を有することを見い出し本発明を完成した。<Problems to be Solved by the Invention> As a result of diligent studies on the pharmacological activity of Compound A, the present inventors have found that Compound A has an excellent preventive and therapeutic effect for renal diseases, and completed the present invention.
＜発明の構成＞ 本発明は，化合物Ａ又はその生理学的許容塩を有効成
分とする腎臓疾患の予防及び治療剤に関する。<Structure of Invention> The present invention relates to a prophylactic and therapeutic agent for renal diseases, which comprises Compound A or a physiologically acceptable salt thereof as an active ingredient.
本発明にかかわる腎臓疾患の具体例としては，ネフロ
ーゼ症候群等をあげることができ，、中でも好ましい治
療効果を期待しうるものとしては微小変化型ネフローゼ
症候群，巣状糸球体硬化症等をあげることができる。Specific examples of the renal diseases related to the present invention include nephrotic syndrome and the like, and among them, those with expected favorable therapeutic effects include minimal change nephrotic syndrome, focal glomerulosclerosis and the like. it can.
化合物Ａ又はその生理学的許容塩を含有する製剤とし
ては，錠剤，カプセル剤，散剤，顆粒剤等をあげること
ができ，これらの製剤は化合物Ａを製剤技術上繁用され
る滑沢剤，崩壊剤，結合剤，賦形剤等の添加剤と共に公
知の製剤技術を用いることにより製造することができ
る。製剤の具体的処方例を以下に示す。Examples of the preparation containing Compound A or a physiologically acceptable salt thereof include tablets, capsules, powders, granules and the like. These preparations are prepared by using Compound A as a lubricant and a disintegrator. It can be produced by using known formulation techniques together with additives such as agents, binders and excipients. A specific formulation example of the formulation is shown below.
錠剤 化合物Ａ 50mg カルボキシメチルセルロース 25mg でんぷん 5mg 結晶セルロース 40mgステアリン酸マグネシウム 2mg 計 122mg 化合物Ａ又はその生理学的許容塩は，通常，経口又は
非経口投与され，その投与量は通常成人一人当り経口投
与の場合100〜2000mg/日，好ましくは200〜1000mg/日で
あり，患者の症状に応じて適宜増減すればよい。Tablets Compound A 50 mg Carboxymethylcellulose 25 mg Starch 5 mg Crystalline cellulose 40 mg Magnesium stearate 2 mg Total 122 mg Compound A or a physiologically acceptable salt thereof is usually administered orally or parenterally, and the dose is usually 100 per oral administration for an adult. The dose is up to 2000 mg / day, preferably 200 to 1000 mg / day, and may be adjusted according to the patient's symptoms.
化合物Ａの毒性は，マウス及びラットに経口又は腹腔
内投与して検討した結果，下記LD50（mg/kg）値で示さ
れている通り極めて低毒性のものであり，又高用量投与
時の所見として，副作用的に問題となるものは認められ
なかった。The toxicity of Compound A was extremely low as shown by the following LD 50 (mg / kg) values as a result of oral or intraperitoneal administration in mice and rats, and also at high doses. As a finding, no side effects were observed.
＜発明の効果＞ 化合物Ａは，腎臓疾患の代表的モデルの一つであるピ
ュロマイシンアミノヌクレオシド腎臓疾患モデルにおけ
る尿蛋白改善試験に対して優れた改善効果を示した。従
って，化合物Ａ及びその塩は腎臓疾患の予防及び治療剤
として優れたものである。 <Effect of the Invention> Compound A showed an excellent improving effect on the urine protein improving test in the puromycin aminonucleoside renal disease model which is one of the typical models of renal disease. Therefore, Compound A and its salts are excellent as preventive and therapeutic agents for renal diseases.
以下，本発明を実施例により説明するが，本発明はこ
れによって限定されるものではない。Hereinafter, the present invention will be described with reference to examples, but the present invention is not limited thereto.
実施例 ピュロマイシンアミノヌクレオシド誘発性腎臓疾患モデ
ルの尿蛋白に対する作用 体重176〜199gのSlc:SD系雄性ラットを用いた。ピュ
ロマイシンアミノヌクレオシドは生理食塩水に溶解して
10mg/kgを背部皮下に１日１回10日間（計10回）投与
（0.1ml/100g）した。化合物Ａは0.5％カルボキシメチ
ルセルロースナトリウム水溶液（以下,0.5％CMC）に懸
濁してピュロマイシンアミノヌクレオシド投与開始の日
から14日間経口投与（0.5ml/100g）した。尚，無処置
群，病態対照群には、0.5％CMCのみを投与した。化合物
Ａの投与開始の10日及び14日目にラットを代謝ゲージに
入れて24時間採尿し，腎障害の指標として尿蛋白量をKi
ngsbury−clark法（J.Lab.Med.11,981（1962））によっ
て測定した。結果を表２に示した。尚，数値は各群（１
群８匹）における個々の動物値の平均値±標準誤差で表
示した。Example Action of puromycin aminonucleoside-induced renal disease model on urinary protein Slc: SD male rats weighing 176 to 199 g were used. Puromycin amino nucleoside dissolved in saline
10 mg / kg was subcutaneously administered to the back once a day for 10 days (total 10 times) (0.1 ml / 100 g). Compound A was suspended in a 0.5% sodium carboxymethylcellulose aqueous solution (hereinafter, 0.5% CMC) and orally administered (0.5 ml / 100 g) for 14 days from the day on which administration of puromycin aminonucleoside was started. Incidentally, only 0.5% CMC was administered to the untreated group and the pathological condition control group. On the 10th and 14th day after the start of administration of Compound A, rats were put in a metabolic gauge and urine was collected for 24 hours.
It was measured by the ngsbury-clark method (J.Lab.Med. 11 , 981 (1962)). The results are shown in Table 2. The numerical values are for each group (1
The average value of individual animals in 8 animals in a group ± standard error is shown.
上表より明らかなように，化合物Ａを投与した群では
腎臓疾患の指標である尿蛋白量が病態対照群に比べ有意
に減少した。従って，化合物Ａは腎臓疾患の予防及び治
療剤として優れたものであることが確認された。 As is clear from the above table, the amount of urinary protein, which is an index of renal disease, in the group to which compound A was administered was significantly decreased as compared with the disease state control group. Therefore, it was confirmed that the compound A is excellent as a prophylactic and therapeutic agent for renal diseases.
Claims (1)
ール−３（2H）−オン又はその生理学的許容塩を有効成
分とする腎臓疾患の予防及び治療剤1. A preventive and / or therapeutic agent for renal diseases containing 2-phenyl-1,2-benzisoselenazol-3 (2H) -one or a physiologically acceptable salt thereof as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP62213804A JP2548223B2 (en) | 1987-08-27 | 1987-08-27 | Kidney disease treatment |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP62213804A JP2548223B2 (en) | 1987-08-27 | 1987-08-27 | Kidney disease treatment |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS6456615A JPS6456615A (en) | 1989-03-03 |
| JP2548223B2 true JP2548223B2 (en) | 1996-10-30 |
Family
ID=16645320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP62213804A Expired - Fee Related JP2548223B2 (en) | 1987-08-27 | 1987-08-27 | Kidney disease treatment |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2548223B2 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU5513796A (en) * | 1995-04-25 | 1996-11-18 | Daiichi Pharmaceutical Co., Ltd. | Remedy for acquired immunodeficiency syndrome |
| WO2000010606A1 (en) | 1998-08-24 | 2000-03-02 | Kurokawa, Kiyoshi | Drugs for relieving carbonyl stress and peritoneal dialysates |
| US10058542B1 (en) | 2014-09-12 | 2018-08-28 | Thioredoxin Systems Ab | Composition comprising selenazol or thiazolone derivatives and silver and method of treatment therewith |
-
1987
- 1987-08-27 JP JP62213804A patent/JP2548223B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6456615A (en) | 1989-03-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| LAPS | Cancellation because of no payment of annual fees |