Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1980-06-09
1981-08-18
Sneed, Helen M. S.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
424166, 424287, C07F 1500
Patent
active
042845793
ABSTRACT:
##STR1## where X is Na.sup.+, K.sup.+, Li.sup.+ or H (N-phosphonacetyl-L-aspartato)(1,2-diaminocyclohexane)platinum(II) or alkali metal salt thereof has shown antitumor activity in animals such as activity against murine leukemia L1210. Additionally, this agent is used against B-16 and Colon 38 tumors and also Ehrlich ascites tumor. 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 hydroxyurea (HU) (1000-1500 mg/kg of body weight).
In binary treatment with cis-dichlorodiamine-platinum(II) (or cisplatin) the preferred ratio of the present compound to cisplatin is about 10:1 with a range of about 10:1 to 1:10 in mg/kg of body weight.
As to the variations in the formula on the left hand side of the formula, it may be varied as monodentate, such as cisplatin containing a single amine group proceeding from the ring, or bidentate, such as the present compound. The saturated cyclo ring may be C.sub.4 or C.sub.5 -C.sub.7 in addition to the present cyclohexane.
The present platinum compound may be prepared by reacting the known L-aspartic acid, N-(phosphonacetyl-) disodium salt (PALA; NSC-224131), with dinitrato(1,2-diaminocyclohexane)platinum(II) (NSC-239851). This compound N-phosphonacetyl-L-aspartato(1,2-diaminocyclohexane)platinum(II) may be combined in multiple drug regimen with substantially improved yield cures over the parent compounds. For example, the compound denoted Pt-268 may be combined in a dual regimen with cyclophosphamide (CY), hydroxyurea (HU), and cisplatin.
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Gale Glen R.
Meischen Sandra J.
Naff Marion B.
Roberts, Jr. John S.
Sneed Helen M. S.
The United States of America as represented by the of the Depart
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