Cancer metastasis inhibitor

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Silicon containing doai

Patent

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Details

514569, 514559, 514568, A61K 31695, A61K 3120, A61K 3119

Patent

active

057505152

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to a cancer metastasis inhibitor that markedly inhibits the metastasis of cancer cells.


BACKGROUND ART

Recently, the cancer treatment has notably progressed. Especially, the success rate of cure of a primary cancer by surgery or radiotherapy has been improved, thereby contributing greatly to the progress of the cancer treatment. However, even if the primary cancer is completely removed, the patient will often die eventually because of the cancer relapse caused by cancer metastasis. Accordingly, there were limitations to the complete blocking of cancer metastasis using surgery, radiotherapy or the like, and therefore the metastasis of a cancer to distant tissue is still a direct or indirect cause of patients' death.
Currently, the mechanism of cancer metastasis is presumed as follows. That is, (1) cancer cells proliferate in a primary cancer colony; (2) blood vessels are newly formed; (3) the malignant cancer cells infiltrate and penetrate the newly formed blood vessels; (4) the cancer cells circulate within the human body; (5) the cancer cells reach a target organ; (6) the cancer cells extravasate from blood vessels; (7) the cancer cells proliferate in the target organ; and (8) a metastatic focus is formed.
To date, many chemotherapeutic agents (antineoplastic agents) have been known. These agents are used as pharmaceuticals that serve to act on the above process (1) of the above mechanism, since they reduce the size of tumors and exhibit direct anti-proliferation and cytocidal properties against cancer cells. However, these agents are never satisfactory in that they cause various kinds of adverse reaction, such as toxicity to bone marrow, and almost can not act on the other stages of metastatic processes.
Generally, cancer metastasis inhibitors are intended not only to prevent the metastasis of cancer cells but also to prevent the growth of a micro metastatic focus formed so as to interdict the metastasis and relapse of a cancer. So, the evaluation for the cancer metastasis inhibitors is totally different from that for the typical antineoplastic agents, which, in turn, are expected to diminish tumor size by their cytocidal properties. Accordingly, in view of the metastatic process, a new type of pharmaceutical, which causes little adverse reaction and can be administered for a long period of time, is extremely valuable and has been expected.
As apparent from the foregoing, it has gradually been recognized that from the view point of cancer treatment, blocking of cancer metastasis is an important matter to be achieved in treating a cancer, and in the United States of America, United Kingdom, etc., clinical studies of cancer metastasis inhibitors have been conducted. Recently, several genes considered to be related to cancer metastasis and infiltration have been discovered from one to another, and it has been reported that retinoid compounds, in particular all-trans-retinoic acid can prevent the expression of these genes to interdict metastasis and infiltration of cancer cells in concentration dependent manner. However, their effects have proved not so satisfactory. Therefore, no effective cancer metastasis inhibitor has been developed heretofore.


DISCLOSURE OF THE INVENTION

In view of the above-described situation, the present inventors have studied the pharmacological action of some specific benzoic acid derivatives in various respects, which derivatives have not been reported to have cancer metastasis inhibiting properties. As a result, they have found that these compounds have extremely effective properties for inhibiting metastasis of cancer to thereby complete the present invention.
More specifically, the present invention provides a cancer metastasis inhibitor comprising, as an active ingredient, a benzoic acid derivative represented by the following formula (I) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each represents hydrogen atom, hydroxyl group or trimethylsilyl group, or R.sub.3 and R.sub.4 are bonded

REFERENCES:
patent: 5081271 (1992-01-01), Shudo
patent: 5155249 (1992-10-01), Shudo

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