Claims
- 1. The blue or green platinum-[2,4-dioxopyrimidine] complex or the mixture thereof prepared by reacting a 2,4-dioxopyrimidine having the formula: ##STR3## wherein R.sub.1 and R.sub.2 may be the same or different and are selected from the group consisting of H, lower alkyl, di-lower alkyl amino, di-halo lower alkyl amino, halogen, hydroxy, hydroxy lower alkyl, carboloweralkoxy,
- R.sub.3 and R.sub.4 may be the same or different and are selected from the group consisting of H, lower alkyl ribosyl, deoxyribosyl, ribosyl, triacetyl-, tribenzoyl- or 2',3' loweralkylidene ribosyl, ribosyl phosphates and deoxyribosyl phosphates or
- a 5,6-2H derivative thereof
- with cis-diaquodiammineplatinum(II) wherein the molar ratio of 2,4-dioxopyrimidine to cis-diaquodiammineplatinum(II) is from about 2:1 to about 1:1 at a temperature of from about 0.degree. to about 55.degree. C., a pH of from about 3 to about 8 and for a time sufficient to form said complex or mixture.
- 2. A complex according to claim 1 wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each H.
- 3. A method of preparing a blue or green platinum[2-4-dioxopyrimidine] complex or a mixture thereof consisting essentially of reacting a 2,4-dioxopyrimidine having the formula: ##STR4## wherein R.sub.1 and R.sub.2 may be the same or different and are selected from the group consisting of H, lower alkyl, di-lower alkyl amino, di-halo lower alkyl amino, halogen, hydroxy, hydroxy lower alkyl, carboloweralkoxy
- R.sub.3 and R.sub.4 may be the same or different and are selected from the group consisting of H, lower alkyl ribosyl, deoxyribosyl, triacetyl-, tribenzoyl- or 2',3'-loweralkylidene ribosyl, ribosyl phosphates and deoxyribosyl phosphates or
- a 5,6-2H derivative thereof
- with cis-diaquodiammineplatinum(II) in aqueous solution wherein the molar ratio of 2,4-dioxopyrimidine to cis-diaquodiammineplatinum(II) is from about 2:1 to about 1:1 at a temperature of from about 0 to about 55.degree. C., at a pH of from about 3 to about 8 and for a time sufficient to form said complex or mixture and isolating said complex or mixture.
- 4. A method according to claim 3 wherein said temperature is about room temperature.
- 5. A method according to claim 4 wherein said reaction is conducted for from about 1 to about 21 days.
- 6. The blue or green platinum complex or the mixture thereof prepared by reacting a 2,4-dioxopyrimidine having the structural formula: ##STR5## of the 5,6-2H derivative thereof with cis-diaquodiammineplatinum(II) wherein the molar ratio of 2,4-dioxopyrimidine to cis-diaquodiammineplatinum(II) is from about 2:1 to about 1:1 at a temperature of from about 0.degree. to about 55.degree. C., a pH of from about 3 to about 8 and for a time sufficient to form said complex or mixture.
- 7. A composition adapted for intraperitoneal, intramuscular, subcutaneous or intravenous injection or per os administration to treat malignant tumor cells sensitive to a complex of claim 1 comprising, in unit dosage form, a pharmaceutically acceptable carrier and from about 0.1 mg/ml to about 50 mg/ml of a complex of claim 1.
- 8. A method for the treatment of malignant tumor cells sensitive to a complex of claim 1 comprising the administration to a living being afflicted therewith from about 1 mg/kg to about 800 mg/kg of body weight of a complex according to claim 1.
Parent Case Info
This is a continuation, of application Ser. No. 803,269, filed June 3, 1977, now abandoned which is a continuation of Ser. No. 508,854, filed Sept. 24, 1974 abandoned.
Government Interests
The invention described herein was made in the course of work under a grant or award from the Department of Health and Human Services.
Non-Patent Literature Citations (5)
Entry |
Cleare et al., Coordination Chemistry Reviews, vol. 12, pp. 349 and 399-405, Jun. 1974. |
Rosenberg, Die Naturwissenschaften, vol. 69, pp. 399-406 (1973). |
Connors et al., Platinum Coordin. Complexes in Cancer Chemother., title pp. IX, 40-41, 51, 61 and 66 (1974). |
Gelfman et al., Russian J. of Inorganic Chemistry, vol. 5, pp. 16-2-1604 (1970). |
Mansy et al., J. Am. Chem. Soc. vol. 95, pp. 1633-1646 (1973). |
Continuations (2)
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Number |
Date |
Country |
Parent |
803269 |
Jun 1977 |
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Parent |
508854 |
Sep 1974 |
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