JPH0442368B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to antitumor agents. The present invention relates to a compound represented by the following () or a salt thereof (hereinafter abbreviated as the present substance) and an antitumor agent containing the present substance as an active ingredient. In addition, this substance contains information in Newly Developed Drug Handbook, 2nd Edition Supplement, pp. 22-24, 1981, Yakugyo Jihosha; Recent New Drugs, Vol. 33, pp. 248-250, 1982, Yakuji Nipposha, etc. The list also includes known substances whose safety has been fully confirmed. Its physical and toxicological properties are shown in Table 1.

[Table] 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 a sufficient amount of the active ingredient to obtain a medicinal effect depending on the symptom. For oral use, it can take the following forms: powder, fine granules, granules, tablets, buffered tablets, sugar-coated tablets, capsules, syrups, pills, suspensions, solutions, emulsions and the like. 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 suppositories or ointments. The substance may be used alone or in admixture with pharmaceutically acceptable diluents and other agents, including solid, liquid, or semi-solid 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%.
Contains ~80% by weight. Oral or parenteral administration of this substance to humans and animals includes sublingual administration. Administered parenterally. Oral administration can be administered by injection (e.g. subcutaneously, intramuscularly,
(intravenous injection, infusion), rectal administration, etc. 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. In some cases, doses outside the range below may be administered, but in general, when administering to humans, The dose of the substance is 1
0.1-500mg/Kg per day, preferably 1-200mg/
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 Antitumor effect against Sarcoma-180 1×10 ⁶ Sarcoma-180 cells were subcutaneously transplanted into the lower axilla of ICR-JCL mice, and 10 times every other day starting 24 hours after transplantation, they were dissolved in 0.5% CMC solution or A predetermined amount of the suspended substance was orally administered. Tumor nodules were excised on the 25th day after transplantation, and the growth inhibition rate (IR%) was calculated using the following formula. (1-T/C)×100=IR (%) T: Administration group average tumor weight C: Subject group average tumor weight The results are shown in Table 2. In addition, 10 animals were used for each group, and the average value was used. As is clear from Table 2, this substance had a tumor shrinking effect and an antitumor effect.

[Table] Formulation example 1 2-(5H-[1]benzopyrano[2,3-b]
1.5 parts by weight of pyridin-7-yl)propionic acid,
8.0 parts by weight of simple syrup and 100 parts by weight of purified water were added to prepare an oral preparation.

Claims (1)

[Claims] 1 set: An antitumor agent containing a compound represented by or a salt thereof as an active ingredient.