(n-phosphonacetyl-l-aspartato)...

C - Chemistry – Metallurgy – 07 – F

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260/429.4

C07F 15/00 (2006.01) C07F 9/38 (2006.01)

Patent

CA 1151663

ABSTRACT OF THE DISCLOSURE Image where X is Na+, K+, Li+, NH4 or H (N-phosphonacetyl-L-aspartato) (1,2-diaminocyclohexane)platinum(II) or alkali metal or ammonium 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 treat- ment with cis-dichlorodiamineplatinum(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. The present platinum compound may be pre- pared 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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