Antitumor agents comprising as the principal compounds containin

Details Antitumor agents comprising as the principal compounds containin Antitumor agents comprising as the principal compounds containin

1997-09-10

1999-06-08

Goldberg, Jerome D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 63, A61K 3170, A61K 31695

Patent

active

059104856

DESCRIPTION:

BRIEF SUMMARY
CROSS-REFERENCE TO RELATED APPLICATION

This is the National Phase application based on International Application PCT/JP97/00200 filed Jan. 29, 1997 and published on Aug. 7, 1997 under number WO 97/27859.


FIELD OF THE INVENTION

This invention relates to an antitumor agent whose principal ingredient is a mixture of an organic compound which contains an amino group and a silyl group, and Adriamycin.


BACKGROUND OF THE INVENTION

The conventional antitumor agents in chemotherapy are mainly classified into a group of antibiotics (for instance Adriamycin) and a group of antimetabolites (for instance 5-fluorouracil). Each group relatively has a feature of a concentration dependence drug and a time dependence drug, and both groups have a problem of being toxic to normal cells. Recently, along with the progress of surgical treatment techniques, expectations for chemotherapy, especially for an antitumor agent whose side effects are minimized, are increasing.
Strong physiological activity of organic silicon compounds has been found by Voronkov et al of Russia (silatrane), and have been investigated in detail. However, sometimes some kinds of silatrane are strongly toxic in accordance with species of substitution group, and some of them have more strong toxicity than hydrocyanamic acid or strychnine. Recently, a group comprised of Shin-etsu Chemical Products Co., Ltd, and Keio University have investigated antineoplastic features of various kinds of organic silicon compounds, and have proceeded with development of relatively low toxicity and high activaty antitumor agents (Chemical Society of Japan, 1990, No. 5, 566-574).
Inventors of this invention have already developed new antitumor agents of ring and chain compounds including silicon and nitrogen (hereafter; shortened to silamine compounds) by investigating thoroughly the antitumor features of silamine compounds (Japanese Patent Application 157518/94 and 157519/94).
However, although the toxicity of these silamine compounds are weaker than that of the antitumor agents such as Adriamycin, its antitumor activity is about 1/10, and said lower antitumor activity is pointed out as a problem.
The object of this invention is to solve the above mentioned problem of silamine compounds, and to provide a new antitumor agent of lower toxicity and high effectiveness.


DISCLOSURE OF THE INVENTION

The important point of this invention is an antitumor agent which comprises a mixture of a compound having the following chemical formula (A) and Adriamycin, ##STR2## and R.sub.8 represent hydrogen atom, or alkyl group, allyl group or aralkyl group of carbon number 1 to 10; further, a pair of R.sub.1 and R.sub.2, and a pair of R.sub.5 and R.sub.6 can be chemically bonded via alkylene, allylene or aralkylene group! and an antitumor agent which comprises a mixture of a compound indicated by following chemical formula (B) and Adriamycin, ##STR3## R.sub.8 represent hydrogen atom, or alkyl group, allyl group or aralkyl group of carbon number 1 to 10; further, a pair of R.sub.1 and R.sub.3, and a pair of R.sub.6 and R.sub.7 can be chemically bonded via alkylene, allylene or aralkylene group!.
That is, in this invention, by combining Adriamycin which is an antitumor agent classified into conventional antibiotics with silamine compounds, those antitumor features act synergistically, and as the result, the toxicity which is a feature of Adriamycin can be relatively weakened. Adriamycin, as noted in The Merck Index, Eleventh Edition (1989), was formerly the generic name for Doxorubicin, and is 8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-5,12-naphth acenedione.
As the compound indicated by chemical formula (A) of this invention, following compounds can be mentioned. 4,7,13,16-tetraethyl-1,1,10,10-tetramethyl-4,7,13,16-tetraaza-1,10-disilac yclooctadecane, 1,1,4,7,10,10,13,16-octamethyl-4,7,13,16-tetraaza-1,10-disilacycloctadecan e, 1,1,4,7,10,10,13,16-octamethyl-4,7,13,16-tetraaza-1,10-disilacycloctadecan e and others.
Compound (A) can be obtained by the method disclosed

REFERENCES:
patent: 5646124 (1997-07-01), Prakash et al.
Carter et al., Chemotherapy of Cancer, second edition, Wiley & Sons, NY ,NY, p. 90-1, 1981.
Wong, et al., Med. Sci. Res., 1989, vol. 17, No. 3, pp. 167-169.

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