JPS61130222A - Antitumor agent - Google Patents

Abstract

PURPOSE:To provide an antitumor agent containing a compound such as 2-(5 H-[1]benzopyrano[2,3-b]pyridin-7-yl)propionic acid, etc. as an active component, effective to the animal or human tumor, and exhibiting the effect e.g. to decrease the number of tumor cells. CONSTITUTION:The objective agent contains the compound of formula (R1 is -O- or -S-; R2 is H or CH3), e.g. 2-(5H-[1]benzopyrano[2,3-b]pyridin-7-yl) propionic acid as an active component. The antitumor agent is administered orally in the form of powder, particle, granule, etc. or parenterally in the form of injection solution sealed in an ampule, bottle, etc. or suppository or ointment. The amount of the active component in the agent is generally 0.01-100wt%, preferably 0.05-80wt%.

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 (1) or a salt thereof (hereinafter abbreviated as the present substance) and an antitumor agent containing the present substance as an active ingredient.

[However, R1 in the formula represents 10- or -8-, and R represents H or CH3.

In addition, this substance contains the newly developed drug handbook, 2nd edition supplement, 22
-24 pages, 1981, Yakugyo Jihosha; Recent new drugs, 33
It also includes known substances described in Yakuji Nippo Publishing Co., Ltd., pp. 248-250, 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 the most active ingredient sufficient to obtain a medicinal effect depending on the symptom. 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 therapeutic agent or ointment.

The substance may be used alone or in combination with pharmaceutically acceptable diluents and other agents, including solid, liquid, or semisolid excipients, fillers, binders, wetting agents, Disintegrants, surfactants, lubricants, dispersants, buffers, fragrances, preservatives, solubilizing agents, solvents, and the like 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% by weight, preferably 0.05 to 8% by weight.
Contains 0% by weight.

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

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

The dose of this substance depends on whether it is an animal or a human, and is influenced by age, individual differences, medical conditions, etc. Depending on the case, the dose of this substance may be administered within the following range, but in general, when administering this substance to humans, Dosage m is 0.1-500Rg/K per day
g, preferably 1 to 200 Rg/Ng. 1 day 2
It may be administered in ~4 divided doses.

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

Transfer to LUI 5arCo”a-180 1x106 Sarcoma-180 cells to ICR-J
CL? 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. 25 days after transplantation
On day 1, tumor nodules were excised and the growth inhibition rate (1,
R,%) was calculated.

(1-T/C)X100=1. 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 20 Antitumor effect of this substance against 5arcola-180 Formulation Example 1 2-(5H-[1]benzopyrano[2,3-b]pyridin-7-yl)propionic acid 1.5 parts by weight, simple syrup 8. 0 parts by weight and 100 parts by weight of purified water were added to prepare an oral preparation.

Claims (2)

[Claims] (1) General formula: ▲There are mathematical formulas, chemical formulas, tables, etc.▼ (In the formula, R_1 is -O- or -S-, R_2 is H or C
Represents H_3. ) An antitumor agent containing the compound or its salt 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.▼.