JPH0228114A - Remedy for nephritis - Google Patents
Remedy for nephritisInfo
- Publication number
- JPH0228114A JPH0228114A JP10081989A JP10081989A JPH0228114A JP H0228114 A JPH0228114 A JP H0228114A JP 10081989 A JP10081989 A JP 10081989A JP 10081989 A JP10081989 A JP 10081989A JP H0228114 A JPH0228114 A JP H0228114A
- Authority
- JP
- Japan
- Prior art keywords
- 1alpha
- oxa
- glomerulonephritis
- present
- active ingredient
- 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.)
- Granted
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
産２又上ｙと刊朋り分ＩＬ
本発明は、１α、３β−ジヒドロキン−２０α（３−ヒ
ドロキン−３−メチルブチルすキ／）−９，１０−セコ
−５，７，１０（１９）−プレグ フ“ト リ エ
ン・ （以 ド ｒ２２−ｏｘａ−４ａ、 ２５−
（ＯＨ）２ Ｄａ Ｊと記す）を仔効成分として含伺
゛する医薬９具体的には糸球体腎炎の治療薬に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention provides 1α,3β-dihydroquine-20α(3-hydroquine-3-methylbutylsuki/)-9,10-seco-5, 7,10(19)-Pregfutrie
(r22-oxa-4a, 25-
Specifically, the present invention relates to a drug for treating glomerulonephritis.
の ′ ゛ ４本を明の
化合物である２２−ｏｘａ−１α、２５−（Ｏ）（）
２ Ｄ・〕は公知化合物であり、特開昭８！−２６７５
５０号公報に記載されている。該公報には、種々の２２
−オキサービタミノＤ３誘導体が記載され、それらは免
疫調節作用および腫婆細胞の分化誘導能を灯し、抗アレ
ルギー剤、抗リウマチ剤および抗Ｎｆｔ１剤として使用
し得る旨申し述べられている。しかしながら、糸球体腎
炎に対し、有効である旨の記載はもとより、本発明の化
合物である２２−ｏｘａ−４α、２５− （ＯＨ）２Ｄ
３については、その薬理作用についは、何ら具体的な記
載は見受（」られない、っ
一方、糸球体腎炎は、腎の大多数の糸球体に様な炎症性
病変を生じ、ある時期には多情の蛋白尿やｌ１腫等を生
じ、ときにネフローゼ症候群ともなる疾患で、その臨床
経過により）、性、亜急性。' ゛ 4 are the clear compounds 22-oxa-1α, 25-(O)()
2 D.] is a known compound and was published in JP-A-8! -2675
It is described in Publication No. 50. The publication contains various 22
- Oxervitamino D3 derivatives have been described and it is stated that they exhibit immunomodulatory effects and the ability to induce differentiation of tumor cells and can be used as anti-allergic, anti-rheumatic and anti-Nft1 agents. However, the compound of the present invention, 22-oxa-4α, 25-(OH)2D, is said to be effective against glomerulonephritis.
Regarding No. 3, there are no specific descriptions of its pharmacological action.On the other hand, glomerulonephritis causes inflammatory lesions in the majority of the glomeruli of the kidney, and It is a disease that causes hyperthermic proteinuria and 11 tumor, sometimes resulting in nephrotic syndrome.
慢性に大別され、抗原抗体反応によるとみなされている
。現在、この糸球体腎炎にλ１する治療薬は、対症療法
的なものが殆どであり、ｆ１１作用の少ない根治療法的
な治療薬の開発が強く望まれている。It is broadly classified as chronic and is considered to be caused by an antigen-antibody reaction. Currently, most of the therapeutic drugs that affect λ1 for glomerulonephritis are symptomatic, and there is a strong desire for the development of radical therapeutic drugs with less f11 action.
本発明石は、この糸球体腎炎の治療薬につき鋭意研究し
た結果、２２−ｏｘａ−１α、２５−（０Ｈ）２ Ｄ３
が、極めて低い投与量で慢性糸球体腎炎等の自己免疫疾
患の病態モデル動物であるＭＲＬ／ｐマウスにおける自
己免疫病変を改善するという新知見を得た。本発明は、
この新知見に基づき更に検討を加え完成したもので、２
２−０Ｘａ−１ａ、２５− （ＯＨ）２ Ｄ３を有効成
分として含有する糸球体腎炎の治療薬に関する。The stone of the present invention was created as a result of intensive research into therapeutic agents for glomerulonephritis.
However, we have obtained new findings that an extremely low dose improves autoimmune lesions in MRL/p mice, which are pathological model animals for autoimmune diseases such as chronic glomerulonephritis. The present invention
Based on this new knowledge, it was further examined and completed.
The present invention relates to a therapeutic agent for glomerulonephritis containing 2-0Xa-1a, 25-(OH)2D3 as an active ingredient.
の
本発明の２２−ｏｘａ−１ａ、２５−（ＯＨ）２［）３
は、例えば１α、３β−ジヒドロキシ−５゜７−プレグ
ナジェン−２０α−オールを出発物質とし、特開昭８１
−２６７５５０号公報記載に従って合成される。22-oxa-1a of the present invention, 25-(OH)2[)3
For example, using 1α,3β-dihydroxy-5°7-pregnagen-20α-ol as a starting material,
It is synthesized according to the description in JP-A-267550.
本発明の化合物は、糸球体腎炎、殊に慢性の糸球体腎炎
に対して有効である。本発明の化合物は常法に従い、例
えば経口剤または注射剤の形に製剤化され投与される。The compounds of the present invention are effective against glomerulonephritis, especially chronic glomerulonephritis. The compounds of the present invention are formulated and administered, for example, in the form of oral preparations or injections, according to conventional methods.
好ましい剤型としては、例えば錠剤、カプセル剤および
顆粒剤等が挙げられる。本発明の化合物の投与量は症状
および投与方法によって若干具なるが、通常ヒト成人で
１日量０．０１〜１０μｇの範囲で適宜選択される。Preferred dosage forms include, for example, tablets, capsules, and granules. The dosage of the compound of the present invention varies depending on the symptoms and administration method, but is usually appropriately selected within the range of 0.01 to 10 μg per day for adult humans.
実験例
ＭＲＬ／Ｑ？ウスに２２−ｏｘａ−１ａ、２５− （Ｏ
Ｈ）２ Ｄ３を経口投与し、投与後縁時的に尿蛋白レベ
ルおよびＢＵＮ値について測定した。Experimental example MRL/Q? 22-oxa-1a, 25-(O
H) 2D3 was orally administered, and urinary protein levels and BUN values were measured at intervals after administration.
１）尿蛋白υＦ泄抑制効果
６週齢のＭＲＬ／Ｒ？ウスに２２−ｏｘａ−１ａ、２５
− （ＯＨ）２ Ｄ３２βｇ／ｋｇを１週間に５回経口
投与した。対照群には、同容量の溶剤（１％エタノール
水溶液）を投与した。尿蛋白の測定は、フンビスティク
ス紙（三共■製）を用いた。その結果を第１図に示す。1) Suppressive effect on urine protein υF excretion 6-week-old MRL/R? 22-oxa-1a, 25 in mice
- (OH)2D 32βg/kg was orally administered 5 times a week. The same volume of solvent (1% ethanol aqueous solution) was administered to the control group. Urine protein was measured using Humbistics paper (manufactured by Sankyo ■). The results are shown in FIG.
図中０〜４のカテゴリーは、各々０〜３０．３０〜ｔｏ
ｏ、ｔｏ。Categories 0 to 4 in the figure are 0 to 30, respectively.
o, to.
〜３００．３００〜１０００＞ １０００ｍｇ／ｄ９を
示し、２３週目および２５週目の＋１および＋２は死亡
したマウスの数を示す。~300.300~1000 > 1000 mg/d9, +1 and +2 at 23 and 25 weeks indicate the number of dead mice.
第１図に示すように、本発明の化合物は２βｇ／ｋｇと
いう低投与量で極めて顕著な尿蛋白排泄抑制効果を示し
ている。As shown in FIG. 1, the compound of the present invention exhibits extremely significant urinary protein excretion suppressing effects at a low dose of 2βg/kg.
２）ＢＵＮ値
前記１）と同様にし、ＢＵＮ値を測定した。ＢＵＮ値の
測定は２８週齢に、ウレアーゼ・インドフェノール法に
よった。その結果を第２図に示す。2) BUN value The BUN value was measured in the same manner as in 1) above. BUN values were measured at 28 weeks of age using the urease-indophenol method. The results are shown in FIG.
第２図に示すように、本発明の化合物は対照群に対し、
有意にＢＵＮ値の上昇を抑制する作用が見られる。更に
、本発明の化合物を投与したマウスは、外観から見て本
マウスに特徴的に見られる皮膚の発赤、脱毛、リンパ節
腫脹が殆ど検出されていない。As shown in FIG. 2, the compound of the present invention compared to the control group.
The effect of significantly suppressing the increase in BUN value is seen. Furthermore, in the mice to which the compound of the present invention was administered, almost no skin redness, hair loss, or lymph node swelling, which are characteristically observed in these mice, was detected.
以上の結果から、本発明の化合物はＭＲＬ／Ωマウスに
認められる免疫異常の発生を阻止し、糸球体腎炎等の自
己免疫病を改善していることが明らかとなった。この結
果は、本発明の化合物の糸球体腎炎の治療薬としての可
能性を充分裏づけるものである。The above results revealed that the compound of the present invention prevents the occurrence of immune abnormalities observed in MRL/Ω mice and improves autoimmune diseases such as glomerulonephritis. These results fully support the potential of the compound of the present invention as a therapeutic agent for glomerulonephritis.
第１図および第２図は、本発明の化合物の尿蛋白排泄抑
制効果およびＢＵＮ値の上昇抑制効果を示したものであ
る。図中２２−ｏｘａとあるのは、２２−ｏｘａ−１α
＋ ２５− （ＯＨ）２ Ｄ３を示す。
λ′１
図
象６ａｌ
＋２
参
ノら、！］ Ｚ、ｆ
−書一
拳・・
・―Ｏ−
ハｌｌ！。
ノブ・θメ久
ｚ２・θγへ
才２図
−一いΔFigures 1 and 2 show the effects of the compounds of the present invention on suppressing urinary protein excretion and on increasing BUN values. In the figure, 22-oxa means 22-oxa-1α
+25- (OH)2D3 is shown. λ'1 Icon 6al +2 Sanno et al! ] Z, f -Shoichiken... -O- Harll! . Knob, θmeku z2, θγ to 2 figure - one Δ
Claims (1)
−３−メチルブチルオキシ）−９，１０−セコ−５，７
，１０（１９）−プレグナトリエンを有効成分として含
有する糸球体腎炎の治療薬。1α,3β-dihydroxy-20α-(3-hydroxy-3-methylbutyloxy)-9,10-seco-5,7
, 10(19)-A therapeutic agent for glomerulonephritis containing pregnatriene as an active ingredient.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63-97665 | 1988-04-21 | ||
| JP9766588 | 1988-04-21 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0228114A true JPH0228114A (en) | 1990-01-30 |
| JP2854600B2 JP2854600B2 (en) | 1999-02-03 |
Family
ID=14198342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10081989A Expired - Fee Related JP2854600B2 (en) | 1988-04-21 | 1989-04-20 | Nephritis treatment |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2854600B2 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995028162A1 (en) * | 1994-04-19 | 1995-10-26 | Chugai Seiyaku Kabushiki Kaisha | Ameliorant or remedy for paraneoplastic syndrome |
| WO2000067758A1 (en) * | 1999-05-10 | 2000-11-16 | Toshio Doi | Remedies for glomerulosclerosis |
-
1989
- 1989-04-20 JP JP10081989A patent/JP2854600B2/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995028162A1 (en) * | 1994-04-19 | 1995-10-26 | Chugai Seiyaku Kabushiki Kaisha | Ameliorant or remedy for paraneoplastic syndrome |
| WO2000067758A1 (en) * | 1999-05-10 | 2000-11-16 | Toshio Doi | Remedies for glomerulosclerosis |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2854600B2 (en) | 1999-02-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |