JPS61129128A - Antitumor agent - Google Patents

Abstract

PURPOSE:An antitumor agent having reducing action on tumor, containing a 5-alkyl-1-cyclohexyl-2,4,6-trioxo-perhydropyrimidine as an active ingredient. CONSTITUTION:An antitumor agent containing a compound shown by the formu la (R is 1-4C alkyl) as an active ingredient. The compound is well-known as a substance having partially anti-inflammatory action, has effects on reduc tion in number of tumor cells, prolongation of life, inhibition of tumor multiplica tion, etc. in tumor of animal or human, useful as an antitumor agent. The antitumor agent is administered orally or parenterally, and parenteral administra tion includes injection, rectum administration, application, etc. A dose is gener ally 0.1-1,000mg/kg/day, preferably 1-500mg/kg/day, may be daily administered twice-4 times dividedly in case of human.

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) and an antitumor agent containing the compound as an active ingredient.

(In the formula, R is an alkyl group having 1 to 4 carbon atoms)
Among the substances of the present invention represented by the above general formula (1), there are
Also included are known substances described in Yakugyo Jihosha and other publications as substances having anti-inflammatory effects.

5-n-butyl-1-, a representative compound of this substance
The physicochemical properties and toxicity of cyclohexyl-2,4,6-trioxo-berhydropyrimidine (which is a compound of Rtfin-butyl in general formula (1)) are as follows.

Molecular formula: C14H22N203 Molecular weight: 266.34 White to almost white crystalline powder, almost no odor, bitter taste.

Easily soluble in methanol, ethanol, acetone, chloroform, and benzene, almost insoluble in water.

111, p, 81-85°C LD 5 () (oral, mouse) 1550
M/N5F This substance has effects such as reducing the number of tumor cells, prolonging life, and inhibiting tumor growth in animal or human tumors, and is useful as an antitumor agent.

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 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 admixture with pharmaceutically acceptable diluents and other agents, including solid, liquid, or semi-solid excipients, 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% 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 sublingual administration.

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

The dosage 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, doses outside the range below may be administered, but in general, when administering this substance to humans, Dosage: 0.1-1100OI per day
rt/K9, preferably 1 to sooRg/Ky. 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.

3 arcOIIla-180 cells 1X10
Transplanted subcutaneously into the axillary region of CR-, lCL mice, and transplanted 2
After 4 hours, 10 times every other day, a prescribed dose of 5-n-butyl-1-cyclohexyl-2,4,6-1-lioxoberhydropyrimidine dissolved or suspended in 0.5% CMG solution was administered. 1 (sooη/Ky·times) was orally administered.

On the other hand, only the CMC solution was orally administered to the control group.

Tumor nodules were excised on the 25th day after transplantation, and the growth inhibition rate ([,R,) was calculated from the average tumor weight of 10 animals in each group according to the following formula:
was calculated.

(1-T/C)Xloo = 1. R, (%) T: Average tumor weight of administration group C: Average tumor weight of control group A growth inhibition rate of 40.6% was obtained. As is clear from these results, it was confirmed that this substance has a tumor reduction effect and is effective as an antitumor agent.

Formulation Example 1 5-n-butyl-1-cyclohexyl-2,4,6
- Dryoxoperhydropyrimidine 1,5 hyponymph,
An oral preparation was prepared by adding 8.0 parts by weight of simple syrup and 100 parts by weight of purified water.

7BmA〒”°A long time ago 〒11

Claims (2)

[Claims] (1) An antitumor agent containing a compound represented by the general formula ▲Mathematical formula, chemical formula, table, etc.▼ (in the formula, R is an alkyl group having 1 to 4 carbon atoms) as an active ingredient. (2) The antitumor agent according to claim 1, which contains a compound represented by the formula ▲ which includes mathematical formulas, chemical formulas, tables, etc. as an active ingredient.