JPS61129129A - Antitumor agent - Google Patents

Abstract

PURPOSE:An antitumor agent containing 1-(4-metoxy-6-methyl-2-pyrimidinyl)-3- methyl-5-methoxypyrazole, etc. as an active component. CONSTITUTION:An antitumor agent containing 0.01-100wt%, preferably 0.05-80wt% compound shown by the formula(r is methyl, or phenyl) as an active ingredient. It has effects on reduction in number of tumor cells, prolongation of life, inhibition of tumor multiplication, etc. in tumor of animal or human. A dosage form oral administration includes powder, fine granule, granule, tablet, capsule, solution, etc. Ampule of injection, bottle, etc. may be cited as parenteral administration, and suppository, or ointment may be used. A dose is 0.1-500mg/kg, preferably 1-200mg/kg, may be daily administered twice-4 times dividedly.

Description

[Detailed description of the invention] 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 methyl or phenyl.) In addition, the present invention v1 represented by the above general formula (1) includes the following: Medical Drugs Japan Pharmaceutical Collection, 5th edition, p. 758 (1979), Shiraki Compiled by the Drug Information Center: Recent New Drugs Volume 34, p. 130 (
Also included are known substances described in Yakuji Nipposha (1983) as substances having anti-inflammatory effects.

1-(4-methoxy-6, a representative compound of this substance)
The physicochemical properties and toxicity of -methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole (a compound in which R is methyl in the general formula (1)) are as follows.

Molecular formula C11H14N40□ Molecule M 234.2G White or slightly yellow crystals or crystalline powder, peculiar odor,
bitter taste.

Slightly soluble in water, slightly soluble in methanol or ethanol.

Stable against acids and alkalis.

m, p, 87.5-89°C pH of aqueous solution (1-,100) is 13.4-6.7, o
Ka is 18 (spectroscopy).

Absorbance λ 251nn+ ε: 1.76x 104l
1ax (ethanol solution) λ 251nl 6: 1.68X 10'a
x (methanol solution) λ 250nva 6 2 1.77x
104aX (aqueous solution EIH7) LD5o (oral, mouse) 10221R9/
This substance has been shown to cause Il! in animal or human tumors. r+
It has effects such as reducing the number of tumor cells, prolonging life, and suppressing tumor growth.
It 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 sufficient active ingredients to obtain medicinal efficacy depending on the symptoms. For oral use, it takes the form of powder, fine granules, granules, tablets, buffered tablets, sugar-coated tablets, capsules, syrups, chips, suspensions, solutions, emulsions, etc. 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, such as solid, liquid, or semi-solid excipients, bulking agents, binders, wetting agents. , disintegrants, surfactants, lubricants, dispersants, buffers, fragrances, preservatives, solubilizing agents, solvents, etc. may be used.

When the substance is used in the form of a preparation, the active ingredient in the preparation is generally 0.01 to 100%, preferably 0.05 to 8%.
Contains 0% by weight.

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

Parenteral administration includes Note 41 administration (VA: subcutaneous, intramuscular, intravenous injection, drip), rectal administration, etc. 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. In some cases, doses outside the range shown below may be administered, but in general, when administering this substance to humans, Dosage is 0.1-5001R9 per day
/K9, preferably 1-200 #Ig/K'J. 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 3 arcoma-180 tumor J of this substance
Fruit 3 1 x 106 arcoma-180 cells were ICed.
1-(4-methoxy-6-methyl-2-
A predetermined fit (1soRg/Kg·times) of (pyrimidinyl)-3-methyl-5-methocypyrazole 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 (1,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 57.1% 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.

1 milk [1 unit 1-ri-4-methoxy-6-methyl-2-pyrimidinyl]
-3-methyl-5-methoxyvirazole 1.5 parts by weight,
8.0 parts by weight of simple syrup and 1001 parts of purified water were added to prepare an oral preparation.

Formulation Example 2 l-(4-methoxy-6-methyl-2-pyrimidinyl)
-3-Methyl-5-methoxypyrazole was added to sterilized physiological saline to form a 10 m injection.

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 methyl or phenyl) 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.