C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
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.
356429
Gale Glen R.
Meischen Sandra J.
Naff Marion B.
Government Of The United States Of America As Represented By The Department Of Commerce
Smart & Biggar
LandOfFree
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