Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1977-08-29
1979-01-30
Sneed, Helen M. S.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
424287, C07F 1500
Patent
active
041372484
ABSTRACT:
##STR1## 4-Carboxyphthalato (1,2-diaminocyclohexane)platinum(II) (and alkali metal salts thereof) has shown antileukemic activity in mice against murine leukemia L1210. It is effective in dosages of 5-60 mg/kg of body weight and is potentiated in a treatment with cyclophosphamide (CY) (50 mg/kg of body weight) to which may be added 5-fluorouracil (5-FU) (75 mg/kg of body weight) or hydroxyurea (HU) (1000 mg/kg of body weight). Some previous platinum chelate compounds show dosage limitation due to renal impairment but the free carboxyl of the present Pt compound offers a possible route of oral administration and absorption by the stomach.
The Pt compound may be prepared by reacting the known dichloro(1,2-diaminocyclohexane)platinum(II) (NSC 194814) with silver nitrate to replace chloro with nitro. Subsequently, benzene tricarboxylic acid is added to form an off-white precipitate (2 hrs, dark, 5.degree. C) of the desired product which is preferably utilized as the alkali metal salt.
The 4-carboxyphthalato(1,2-diaminocyclohexane)-platinum(II) and alkali metal salts thereof may be combined in multiple drug regimen with substantially improved yield cures over the parent compound. For example, the compound denoted Pt-307 may be combined in a dual regimen with cyclophosphamide (CY) and in a triple drug regimen of Pt-307 plus cyclophosphamide (CY) and either 5-fluorouracil (5-FU) or hydroxyurea (HU) as the third component.
REFERENCES:
patent: 3892790 (1975-07-01), Tobe et al.
patent: 3904663 (1975-09-01), Tobe et al.
Hill et al., J. of Clinical Hematology & Oncology, 7 681-697 (1977).
Schwartz et al., Cancer Treatment Reports, 61, 1519-1525 (1977).
Gale Glen R.
Schwartz Paul
Ferris Thomas G.
Latker Norman J.
Roberts, Jr. John S.
Sneed Helen M. S.
The United States of America as represented by the Department of
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