Organic compounds -- part of the class 532-570 series – Organic compounds – Heavy metal containing
Patent
1990-10-03
1992-02-11
Prescott, Arthur C.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heavy metal containing
556 9, 556431, 514492, 528 15, C07F 1500
Patent
active
050877127
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE ART
The present invention relates to the art of bioinorganic chemistry and, more particularly, to novel compounds--derivatives of platinum (II) with polymethylsiloxane, to a method for preparing same and to an agent of an antitumor effect based thereon.
PRIOR ART
At the present time the death rate of the population, especially of persons of a young and middle age due to malignant tumors of different location is growing everywhere. In this connection, a great attention is paid to the development and investigation of antitumor-action pharmaceutical preparations.
Among chemotherapeutic preparations employed as antitumor agents one of the most active and widely used in medicinal practice is a synthetic preparation of an inorganic nature--cis-dichlorodiammonioplatinum (II)/CDDP, Cis-platin/ (Handbook of Cancer. Combination chemotherapy'85, Bleomycin, Peplomycin, Cisplatin, Nippon Kayaku 1986, p. 6-7, 26-27, 46-47, 61-63). As an antitumor preparation CDDP is used in mono- and polychemotherapy in cases of cancer of the urogenital sphere, tumors of lungs, head, neck and central nervous system, as well as in the cases of lymphomae and in oncogenicology. The effectiveness of therapy of ovary carcinoma through administration of the preparation CDDP in combination with vinblastin, actinomycin and prednisolone is as high as 100%.
However, CDDP is a highly toxic preparation which causes injury of kidneys, vomition, giddiness, suppression of medullary hemopoiesis, disturbances of audition, allergic responses, electrolytical disorders and neurological symptoms.
The most dangerous side effect which is revealed in the therapy with the preparation CDDF is its nephrotoxicity limiting the therapeutic dose of the preparation. The disturbance of the kidneys' function is associated with the injury of glomerules and tubules and is manifested in a high level of urina, creatinine, uric acid in the biochemical blood examination parameters.
The suppression of the medullary hemopoiesis can be caused also by the dose and duration of the treatment. The preparation CDDF injures all three branches of the hemopoiesis. The appearance of leukopeniae varies from 0 to 52%, that of anemiae--from 9 to 40%. There are also cases of gemolytic anemia.
Due to the high nephro- and hematotoxicity, during the treatment with the preparation of CDDF it is necessary to regularly ccary out analyses of biochemical parameters and blood formula.
Well known in the art at the present ime are also antitumor preparations containing, as the active principle, organic substances of a synthetic or natural origin (alkylation agents, antimetabolics, antibiotics, alkaloids, enzymes, hormones and the like).
These preparations are inferior to the preparation CDDF in respect of the level of their anti-tumor effect. Furthermore, they produce a side effect on the cardiac muscle, hemopoiesis, gastro-intestinal tract. All known preparations of the anti-tumor effect suppress the immunological reactivity of the organisms to a certain extent.
DISCLOSURE OF THE INVENTION
The compounds according to the present invention, the method for preparing same and a pharmaceutical agent based thereon are novel and hitherto unknown in the literature.
The main object of the present invention is to provide novel compounds featuring a high antitumor activity in combination with a low toxicity, which would not suppress the immunological reactivity of the organism and be useful as antitumor agents for administration directly onto the tumor and adjacent tissues, as well as to provide a method for preparing said compounds.
The object of the present invention is accomplished by novel compounds, viz. derivatives of platinum (II) with polymethylsiloxane comprising xerogels--a product of interaction of a complex compound of platinum (II) in an aqueous solution of sodium chloride with a hydrogel of polymethylsiloxane at a molar of Pt:Si:NaCl equal to 1-3:50:23-69 representing a three-dimensional cross-linked polymer of a globular structure with a globule diameter of 4.0 to 7.0 nm and ha
REFERENCES:
patent: 4544759 (1985-10-01), Hlavka et al.
patent: 4647679 (1987-03-01), Panster et al.
patent: 4847228 (1989-07-01), Saruyama
patent: 4870062 (1989-09-01), Kurono et al.
Handbook of Cancer Combination Chemotherapy '85; Nippon Kayaku, Nov. 1986, Japanese Originals and English Originals.
Budarin Lev. I.
Girin Vitaly N.
Maidanevich Nadezhda N.
Samodumova Inna M.
Volchenskova Ilima I.
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