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

[Detailed description of the invention] TECHNICAL FIELD The present invention relates to antitumor agents.

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.

However, R in the formula is H, C1-13 or QC, )-13
represents.

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.

Its physical and toxicological properties are shown in Table 1.

Table 1 This substance is effective against animal or human tumors.

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.

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.

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.

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.

The substance is administered orally or parenterally to humans and animals. Oral administration includes sublingual administration.

Parenteral administration includes injection administration (eg, subcutaneous, intramuscular, intravenous injection, infusion), rectal administration, and the like. May be applied.

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.

The present invention will be further explained below with reference to Examples.

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: 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.

As is clear from Table 2, this substance had a tumor shrinking effect and an antitumor effect.

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)

[Claims] (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) 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.▼.