JPS61130218A - Antitumor agent - Google Patents

Abstract

PURPOSE:To provide an antitumor agent containing a specific compound including known substance having sufficiently ascertained safety, exhibiting the effect to decrease the number of tumor cells, improve the life prolongation rate and suppress the proliferation of the tumor cell, and effective to animal or human tumor. CONSTITUTION:The objective agent contains the compound of formula I (R is H, CH3 or OCH3) or its salt, preferably 6-chloro-5-cyclohexyl-1- indanecarboxylic acid of formula II (R is H) as an active component. The active component is used singly or as a mixture with pharmacologically permissible carrier or adjuvant, and administered orally in the form of powder, tablet, capsule, etc. including sublingual administration, or parenterally in the form of injection in ampule, etc., suppository, ointment, etc. by injection, rectal infusion, etc. or dermal application. The content of the active component in the medicinal drug is 0.1-100wt%, and the component is administered at a dose of 0.1-1,000mg/kg daily for human optionally in 2-4 divided doses.

Description

【発明の詳細な説明】 本発明は抗腫瘍剤に関する。[Detailed description of the invention] TECHNICAL FIELD The present invention relates to antitumor agents.

本発明は、下記一般式（Ｉ）で表わされる化合物又はそ
の塩（以下、本物質と略称する）および本物質を活性成
分として含有する抗腫瘍剤に関する。The present invention relates to a compound represented by the following general formula (I) or a salt thereof (hereinafter abbreviated as the present substance) and an antitumor agent containing the present substance as an active ingredient.

ただし、式中のＲはＨ，Ｃ１−１３又はＱＣ，）−１３
を表わす。However, R in the formula is H, C1-13 or QC, )-13
represents.

尚、本物質中には新開発医薬品便覧、第２版追補、１９
−２１頁、１９８１年、薬業時報社：最近の新薬、３３
集、２４３〜２４６頁、１９８２年、薬事日報社等に記
載されている公知物質も含まれ、その安全性は十分確認
されている。In addition, this substance contains the newly developed drug handbook, 2nd edition supplement, 19
-21 pages, 1981, Yakugyo Jihosha: Recent new drugs, 33
It also includes known substances described in Yakuji Nippo Publishing Co., Ltd., pp. 243-246, 1982, and their safety has been sufficiently confirmed.

その物理学的並びに毒物学的特性を表１に示す。Its physical and toxicological properties are shown in Table 1.

表　　１ 本物質は動物又は人腫瘍に有効である。Table 1 This substance is effective against animal or human tumors.

本物質は、腫瘍細胞数の減少、延命率、増殖抑制率等に
おいてその効果を確認し有効性を判断した。The effectiveness of this substance was determined by confirming its effectiveness in reducing the number of tumor cells, prolonging survival rate, suppressing proliferation rate, etc.

本物質を抗腫瘍剤として用いる場合、症状に応じて薬効
を得るのに十分な泄の有効成分が含有された投薬単位形
態で提供することができる。その形態としては経口用と
して散剤、細粒剤、顆粒剤、錠剤、緩衝錠剤、糖衣錠剤
、カプセル剤、シロップ剤、乳剤、懸濁剤、液剤、乳剤
などの形態をとり得る。非経口用として注射液としての
アンプル、ビンなどの形態をとり得る。廃剤、軟膏の形
態でもよい。When the present substance is used as an antitumor agent, it can be provided in a dosage unit form containing sufficient excretion of the active ingredient to obtain a medicinal effect depending on the symptoms. For oral use, it can take the form of powder, fine granules, granules, tablets, buffered tablets, sugar-coated tablets, capsules, syrups, emulsions, suspensions, solutions, and emulsions. For parenteral use, it can be in the form of an ampule or bottle as an injection solution. It may also be in the form of a waste agent or ointment.

本物質は単独又は製薬上許容し得る希釈剤及び他の薬剤
と混合して用いてもよく、希釈剤として固体、液体、半
固体の斌形剤、増量剤、結合剤、湿潤化剤、崩壊剤、表
面活性剤、滑沢剤、分散剤、緩衝剤、香料、保存料、溶
解補助剤、溶剤等が使用され得る。The substance may be used alone or in admixture with pharmaceutically acceptable diluents and other agents, including solid, liquid, and semi-solid injections, fillers, binders, wetting agents, disintegrating agents, etc. agents, surfactants, lubricants, dispersants, buffers, fragrances, preservatives, solubilizing agents, solvents, etc. may be used.

本物質を製剤の形で用いる場合、製剤中に活性成分は一
般に０．０１〜１００ｆｆｌｆｆｔ％、好ましくは０．
０５〜８０重量％含まれる。When the substance is used in the form of a formulation, the active ingredient in the formulation is generally 0.01 to 100 fflfft%, preferably 0.01 to 100 fflfft%.
05 to 80% by weight.

本物質は人間及び動物に経口的または非経口的に投与さ
れる。経口的投与は舌下投与を包含する。The substance is administered orally or parenterally to humans and animals. Oral administration includes sublingual administration.

非経口的投与は注射投与（例えば皮下、筋肉、静脈注射
、点滴）、直腸投与などを含む。塗布してもよい。Parenteral administration includes injection administration (eg, subcutaneous, intramuscular, intravenous injection, infusion), rectal administration, and the like. May be applied.

本物質の投与ｍは動物か人間により、また年齢、個人差
、病状などに影響されるので場合によっては下記範囲外
ωを投与する場合もあるが、一般に人間を対象とする場
合、本物質の投与ωは１日当り０．１〜１０００１１１
ｇ／／（ｇ、好ましくは１〜３００１１ｇ／Ｋｇである
。１日２〜４回に分け【投与してもよい。The administration of this substance depends on whether it is an animal or a human, and is influenced by age, individual differences, medical conditions, etc. Therefore, in some cases, doses outside the range shown below may be administered, but in general, when administering this substance to humans, Administration ω is 0.1-1000111 per day
g//(g, preferably 1 to 30011 g/Kg. It may be administered in divided doses 2 to 4 times a day.

以下、実施例により本発明をさらに説明する。The present invention will be further explained below with reference to Examples.

実施例１Ｓａｒｃｏｍａ−１８０に対する　腫　効果Ｓ
ａｒｃｏｍａ−１８０＠胞１×１０６個をＩＣＲ−ＪＣ
Ｌ　？ウスの腋下部皮下に移植し、移植２４時間後より
隔日に１０回、０．５％ＣＭＣ溶液中に溶解もしくは懸
濁させた本物質の所定量を経口投与した。移植後２５日
目に腫瘍結節を摘出し、次式により増殖抑制率（１，Ｒ
，％）を算出した。Example 1 Effect on Sarcoma-180
arcoma-180@ICR-JC 1 x 106 cells
L? The substance was implanted subcutaneously in the axilla of a mouse, and a predetermined amount of the substance dissolved or suspended in a 0.5% CMC solution was orally administered 10 times every other day starting 24 hours after implantation. Tumor nodules were excised on the 25th day after transplantation, and the growth inhibition rate (1, R
,%) was calculated.

（１−Ｔ／Ｃ）ｘｌ　００−　ｔ、Ｒ，’（％）Ｔ：投
与群平均腫瘍重量 Ｃ：対照群平均腫瘍型の 結果を表２に示す。尚１群１０匹ずつ用いてその平均値
を用いた。(1-T/C)xl 00-t,R,'(%)T: Administration group average tumor weight C: Control group average tumor type The results are shown in Table 2. Each group of 10 mice was used, and the average value was used.

表２から明らかな如く、本物質に腫瘍縮小効果がみられ
、抗腫瘍効果が認められた。As is clear from Table 2, this substance had a tumor shrinking effect and an antitumor effect.

表１１本物質のＳａｒｃｏｍａ−１８０に対する抗腫瘍
作用製剤化例１ ６−クロｏ−５−シクロへキシル−１−インダンカルボ
２１１１．５重量部、単シロップ８．０重量部、精製水
１００重量部を加えて経口剤とした。Table 11 Antitumor effect of this substance against Sarcoma-180 Formulation Example 1 211.5 parts by weight of 6-chloro-o-5-cyclohexyl-1-indanecarbo, 8.0 parts by weight of simple syrup, 100 parts by weight of purified water was added to form an oral formulation.

Claims (2)

【特許請求の範囲】[Claims] （１）一般式： ▲数式、化学式、表等があります▼ （式中、ＲはＨ、ＣＨ＿３又はＯＣＨ＿３を表わす。）
で示される化合物又はその塩を活性成分として含有する
抗腫瘍剤。(1) General formula: ▲There are mathematical formulas, chemical formulas, tables, etc.▼ (In the formula, R represents H, CH_3 or OCH_3.)
An antitumor agent containing a compound represented by or a salt thereof as an active ingredient. （２）活性成分が式： ▲数式、化学式、表等があります▼ で示される化合物であることを特徴とする特許請求の範
囲第１項に記載の抗腫瘍剤。(2) The antitumor agent according to claim 1, wherein the active ingredient is a compound represented by the formula: ▲A mathematical formula, a chemical formula, a table, etc.▼.