Marion B Naff

US Patent:

42845793, Aug 18, 1981

Filed:

Jun 9, 1980

Appl. No.:

6/155531

Inventors:

Sandra J. Meischen - Charleston SC
Glen R. Gale - Charleston SC
Marion B. Naff - Bethesda MD

Assignee:

The United States of America as represented by the of the Department of
Health & Human Services - Washington DC

International Classification:

C07F 1500

US Classification:

260429R

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.

US Patent:

44289430, Jan 31, 1984

Filed:

Jul 15, 1981

Appl. No.:

6/283376

Inventors:

Sandra J. Meischen - Charleston SC
Glen R. Gale - Charleston SC
Marion B. Naff - Bethesda MD

Assignee:

The United States of America as represented by the Department of Health
and Human Services - Washington DC

International Classification:

A61K 3166
A61K 3128

US Classification:

424211

Abstract:

##STR1## where X is Na. sup. +, K. sup. +, Li. sup. + or H (N-phosphonacetyl-L-asparato) (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.