US4452812A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Organic complex of platinum, its preparation and its use for treating malignant tumors
Assignee: Sanofi SA
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Filing: 1981-04-27
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Granted: 1984-06-05
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Expires: 2001-04-27
Abstract
Abstract An organic complex of platinum, cis-isocitrato (1,2 diaminocyclohexane) platinum (II) having improved anti-tumor activity and water-solubility. The complex is prepared by reacting cis-dichloro (1,2-diaminocyclohexane) platinum (II) with silver nitrate, removing the silver chloride formed, and reacting the resulting liquid with trisodium isocitrate. The complex is administered in the form of a pharmaceutical composition.
Inventors
- 👤 Jean-Pierre Macquet
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 09:21
CPC Classifications
C; C07; C07C; C07C59/00; C07C59/235; C07C59/245; A; A61; A61P; A61P35/00; C07F; C07F15/00; C07F15/0006; C07F15/0086; C07F15/0093
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
4 words
Cis-isocitrato (1,2-diaminocyclohexane) platinum (II).
Claim 2
Dependent Claim
4 words
Cis-isocitrato (1,2-diaminocyclohexane) platinum (II).
Claim 3
Dependent Claim
26 words
A process for forming cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex which comprises reacting a platinum atom which is partially chelated with 1,2-diaminocyclohexane together with trisodium isocitrate (dl-isomer).
Claim 4
Dependent Claim
26 words
A process for forming cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex which comprises reacting a platinum atom which is partially chelated with 1,2-diaminocyclohexane together with trisodium isocitrate (dl-isomer).
Claim 5
Dependent Claim
16 words
A process according to claim 2 wherein cis-dichloro (1,2-diaminocyclohexane) platinum (II) is reacted with trisodium isocitrate.
Claim 6
Dependent Claim
36 words
A process according to claim 2, wherein cis-dichloro (1,2-diaminocyclohexane) platinum (II) is first reacted with silver nitrate to form the corresponding dinitratoplatinum compound which is thereafter reacted with trisodium isocitrate to form the required platinum complex.
Claim 7
Dependent Claim
40 words
In the process of claim 2 wherein the reaction is carried out in an aqueous medium and the platinum complex is formed including, the step of adding an organic solvent, whereby the recovery of an insoluble platinum complex is promoted.
Claim 8
Dependent Claim
17 words
The process of claim 2 which comprises carrying out the reaction at a temperature above room temperature.
Claim 9
Dependent Claim
25 words
The process of claim 6, which comprises prior, to adding the organic solvent, the step of removing part of the water from the reaction mixture.
Claim 10
Dependent Claim
20 words
The process of claim 5 in which the platinum complex is recovered in a yield of at least about 85%.
Claim 11
Dependent Claim
42 words
A process for preparing cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex which comprises reacting a compound of the formula: cis--[Pt(1,2-diaminocyclohexane)(H.sub.2 O).sub.2 ](NO.sub.3).sub.2 with trisodium isocitrate at a temperature of from about 60° to about 65° C. in water and then recovering the product formed.
Claim 12
Dependent Claim
42 words
A process for preparing cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex which comprises reacting a compound of the formula: cis--[Pt(1,2-diaminocyclohexane)(H.sub.2 O).sub.2 ](NO.sub.3).sub.2 with trisodium isocitrate at a temperature of from about 60° to about 65° C. in water and then recovering the product formed.
Claim 13
Dependent Claim
31 words
The process of claim 9 wherein the product is recovered by the steps comprising concentrating the aqueous solution, filtering and then precipitating the product in a mixture of ethanol and acetone.
Claim 14
Dependent Claim
55 words
A therapeutic composition comprising the compound cis-isocitrato (1,2 diaminocyclohexane) platinum (II) complex for use in the treatment of tumors and a pharmaceutically acceptable carrier, the amount of said platinum II complex in the composition being a therapeutically effective amount and the composition being effective to inhibit L 1210 Leukemia or sarcoma 180 cells in baboons.
Claim 15
Dependent Claim
55 words
A therapeutic composition comprising the compound cis-isocitrato (1,2 diaminocyclohexane) platinum (II) complex for use in the treatment of tumors and a pharmaceutically acceptable carrier, the amount of said platinum II complex in the composition being a therapeutically effective amount and the composition being effective to inhibit L 1210 Leukemia or sarcoma 180 cells in baboons.
Claim 16
Dependent Claim
22 words
The therapeutic composition of claim 11 wherein the composition is in a dosage unit form suitable for oral, intramuscular or intravenous administration.
Claim 17
Dependent Claim
47 words
A pharmaceutical composition for inhibiting tumors in warm-blooded animals which comprises an effective amount of cis-isocitrato (1,2-diaminocyclohexane) platinum (II) in a pharmaceutically acceptable vehicle, which cis-isocitrato (1,2-diaminocyclohexane) platinum (II) is effective to inhibit tumors selected from the group consisting of leukemia L1210 or sarcoma S180 in baboons.
Claim 18
Dependent Claim
47 words
A pharmaceutical composition for inhibiting tumors in warm-blooded animals which comprises an effective amount of cis-isocitrato (1,2-diaminocyclohexane) platinum (II) in a pharmaceutically acceptable vehicle, which cis-isocitrato (1,2-diaminocyclohexane) platinum (II) is effective to inhibit tumors selected from the group consisting of leukemia L1210 or sarcoma S180 in baboons.
Claim 19
Dependent Claim
42 words
A therapeutic composition comprising the compound cis-isocitrato (1,2-diaminocyclohexane) platinum (II) in a therapeutically effective amount, and a pharmaceutically acceptable carrier, said compound being effective to inhibit sarcoma S 180, said composition being effective for inhibiting 1210 Leukemia or sarcoma 180 in baboons.
Claim 20
Dependent Claim
42 words
A therapeutic composition comprising the compound cis-isocitrato (1,2-diaminocyclohexane) platinum (II) in a therapeutically effective amount, and a pharmaceutically acceptable carrier, said compound being effective to inhibit sarcoma S 180, said composition being effective for inhibiting 1210 Leukemia or sarcoma 180 in baboons.
Claim 21
Independent Claim
44 words
A method for use in the treatment of mammals which comprises administering to a mammal a therapeutically effective amount of a composition comprising cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex and pharmaceutically acceptable carrier, which composition is effective to inhibit L 1210 Leukemia cells in baboons.
Claim 22
Independent Claim
44 words
A method for use in the treatment of mammals which comprises administering to a mammal a therapeutically effective amount of a composition comprising cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex and pharmaceutically acceptable carrier, which composition is effective to inhibit L 1210 Leukemia cells in baboons.
Claim 23
Dependent Claim
13 words
The method of claim 15 wherein the administration is oral, intramuscular or intravenous.
Claim 24
Dependent Claim
24 words
The method of claim 16 wherein the composition is administered in a dosage range of 1 to 400 mg/kg of body weight per day.
Claim 25
Dependent Claim
35 words
A method of inhibiting tumors in a warm-blooded animal which comprises administering to said animal an effective amount of the composition of claim 13, which platinum compound is effective to inhibit L1210 cells the baboons.
Claim 26
Dependent Claim
44 words
A method of inhibiting tumors in a warm-blooded animal which comprises administering to said animal an effective amount of the composition of claim 13, which composition is effective to inhibit tumors selected from the group consisting of leukemia L1210 or sarcoma S180 in baboons.
Claim 27
Independent Claim
47 words
A method for the treatment of mammals which comprises administering to a mammal an effective amount of a composition which comprises cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex in a therapeutically effective amount, and a pharmaceutically acceptable carrier, which composition is effective to inhibit sarcoma S 180 in baboons.
Claim 28
Independent Claim
47 words
A method for the treatment of mammals which comprises administering to a mammal an effective amount of a composition which comprises cis-isocitrato (1,2-diaminocyclohexane) platinum (II) complex in a therapeutically effective amount, and a pharmaceutically acceptable carrier, which composition is effective to inhibit sarcoma S 180 in baboons.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-06-05 | 1987-12-05 | 1988-06-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-06-05 | 1991-12-05 | 1992-06-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-06-05 | 1995-12-05 | 1996-06-05 | $7700.00 | Window Closed / Lapsed |