Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
  • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
  • C07F7/30—Germanium compounds

Definitions

• the compound of the invention inhibits the proliferation of Ehrlich ascites tumor cells.
• Germanium which has the atomic number of 32, is an atom having 32 electrons. Four of these electrons are located in an outer orbit and are unstable, being capable of separation from the rest under certain conditions. This property of germanium is utilized for transistors or diode rectifiers, as is popularly known. And there is a phenomenon that, when one of these four electrons has escaped, there results what is referred to as a positive hole of electric potential, to which other nearby electrons are drawn in. The composition of germanium being so, its organic compound is apt to cause electric charge transfer and to generate organic free radicals.
• Applicants have for a long time studied the components of plant substances used for the so-called Chinese medical herbs, which have been known to be effective to check abnormal cells in the living body, and discovered that they contained a very large content of germanium, for example, 320 ppm in ginseng, 257 ppm in water-caltrop nut, 124 ppm in box-thorn nut, 108 ppm in wisteriaknot, 50 ppm in pearlbarley seed, 58 ppm in erythrorhizon, 76 ppm in comfry, and 756 ppm in garlic. This fact appears to indicate that germanium exists within these plants in the form of organic compounds.
• B-cyanoethyltrichlorogermanium trichlorogermanium ethylene cyanide is obtained by the action of acrylonitrile on the known compound trichlorogermanium (germaniumchloroform).
• B-Cyanoethyltrichlorogermanium is converted into B- trichlorogermanium propionic acid (trichlorogermanium propionic acid) by hydrolysis in the presence of a mineral acid and by the action of thionylchloride, this latter compound is converted to trichlorogermanium propionyl chloride. Hydrolysis of this compound with water produces bis-carboxylethyl germanium sesquioxide.
• Test mice DD Shizuoka, 4 weeks old.
• the administered group were very vigorous and had good appetite compared with the control group, showing no external appearance of reaction, the control group showed stagnant ascites whereas the administered group showed neither ascites stagnation nor bleeding, the proportion of the number of tumor cells in the bodies of the administered group was approximately 26 percent against percent in the bodies of the control group, and that there was a good indication of the effective checking of fissiparism.
• the compound, bis-carboxyethyl germanium sesquioxide is a, are white, crystalline powder, and capable of polymerization on heating. Its melting point is impossible to measure, since heating to a higher temperature causes decomposition. In water solution, the oxygen in germanium sesquioxide is hydrated and the hydrogen stimulates charge transfer, thus causing activation. 7
• the novel compound according to the present invention is of a very low order of toxicity.
• the LD in mice as determined by hypodermic injection is 3,5g/kg of body weight.
• the compound of the invention is soluble in water, and therefore it is most convenient to formulate it as solutions in sterile, pyrogen-free water, although any pharmaceutically acceptable carrier may be used.
• a preferred therapeutic composition of the invention will comprise an aqueous solution containing from 0.01 to 0.4 by weight of the active ingredient.
• compositions containing the compound according to the invention can be administered orally or Number of E.A.'I. Ascites amount, Aver- '1.I.,
• Example l To 18 gr. of germaniumchloroform are added 6 gr. of acrylonitrile, and by heating under an atmosphere of 55 nitrogengas, Byanoethyltrichlorogermanium is obtained. This is converted to B-trichlorogermanium propionic acid by adding hydrochloric acid solution and heating. This is converted through reaction upon the dropwise addition of 12 gr. of thionylchloride, to trichlorogermanium propionyl chloride, which is recovered by distillation in vacuo. After complete hydrolysis takes place with water, bis-carboxyethyl germanium sesquioxide is obtained. This is washed with water until chlorine reaction disappears and a white powder is obtained. The yield is about 6 gr. Anal. calcd. for C,l-l ,O,(I1E Calculated value: 1 H2294, Ge:42.64 Found 113.00, Ge:42.41
• the carrier can be a solid and in the form of a powder or tablet.
• the solid carrier can be any of those commonly used in making medicinal formulations.

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• Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

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Publications (1)

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Cited By (9)

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• 1968
  • 1968-08-27 DE DE19681793288 patent/DE1793288B1/de active Pending
  • 1968-10-21 CH CH1569168A patent/CH521376A/de not_active IP Right Cessation
• 1969
  • 1969-03-07 US US805370A patent/US3689516A/en not_active Expired - Lifetime
  • 1969-03-28 FR FR6909416A patent/FR2005110A1/fr active Pending
  • 1969-03-28 BE BE730615D patent/BE730615A/xx not_active IP Right Cessation
  • 1969-03-28 NL NL6904836A patent/NL6904836A/xx unknown
  • 1969-03-31 GB GB1257225D patent/GB1257225A/en not_active Expired

Non-Patent Citations (1)

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