US4457926A
Expired / Lapsed
US
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Cis-Platinum(II) amine ascorbate complexes
Assignee: BASF Catalysts LLC
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Filing: 1981-12-18
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Granted: 1984-07-03
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Expires: 2001-12-18
Abstract
Abstract There are described ascorbate complexes of platinum(II) coordinated to ammonia, a monodentate amine ligand or a bidentate amine ligand as, for example, an alkylamine, an alkylenediamine or a cycloalkylamine. Said complexes are useful in the treatment of malignant tumors in animals and they are characterized by high solubility in water and low toxicity.
Inventors
- 👤 Alan R. Amundsen
- 👤 Eric W. Stern
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 17:20
CPC Classifications
C; C07; C07F; C07F15/00; C07F15/0006; C07F15/0086; C07F15/0093
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
81 words
A cis-diamineplatinum(II) ascorbate compound of the formula: cis-[Pt(II)A.sub.2 (X).sub.m (OH).sub.n ] wherein Pt is in valence state II and is coordinated to A in a cis configuration; A is ammonia or a monodentate alkylamine ligand; A 2 is a bidentate diamine ligand; X is the ascorbate moiety; m is a number having a value of from 1 to 2; n is a number having a value of from 0 to 1, and the sum of m+n is not greater than 2.
Claim 2
Dependent Claim
81 words
A cis-diamineplatinum(II) ascorbate compound of the formula: cis-[Pt(II)A.sub.2 (X).sub.m (OH).sub.n ] wherein Pt is in valence state II and is coordinated to A in a cis configuration; A is ammonia or a monodentate alkylamine ligand; A 2 is a bidentate diamine ligand; X is the ascorbate moiety; m is a number having a value of from 1 to 2; n is a number having a value of from 0 to 1, and the sum of m+n is not greater than 2.
Claim 3
Dependent Claim
26 words
A compound according to claim 1 wherein A has the formula RNH 2 and R is selected from the group consisting of hydrogen or lower alkyl.
Claim 4
Dependent Claim
10 words
A compound according to claim 2 wherein R is hydrogen.
Claim 5
Dependent Claim
11 words
A compound according to claim 2 wherein R is lower alkyl.
Claim 6
Dependent Claim
10 words
A compound according to claim 4 wherein R is methyl.
Claim 7
Dependent Claim
73 words
A compound according to claim 1 wherein A 2 is represented by the formula: ##STR3## wherein each of R 1 and R 2 , taken separately, is selected from the group consisting of hydrogen and lower alkyl, or R 1 and R 2 , taken together, afford a 1,2-diaminocycloalkane ligand containing from about 4-8 nuclear carbon atoms which may be optionally substituted by one or more linear or branched chain lower alkyl groups.
Claim 8
Dependent Claim
16 words
A compound according to claim 6 wherein each of R 1 and R 2 is hydrogen.
Claim 9
Dependent Claim
11 words
A compound according to claim 6 wherein A 2 is 1,2-diaminocyclohexane.
Claim 10
Dependent Claim
39 words
A pharmaceutical composition effective for treating animal malignant tumor cells sensitive to a platinum compound of claim 1 comprising an effective amounts of a compound of claim 1 in combination with a non-toxic pharmacologically acceptable inert carrier or diluent.
Claim 11
Dependent Claim
22 words
The composition of claim 9 wherein the active ingredient is selected from the group consisting of cis-diamineplatinum(II) ascorbate and cis-bis(lower alkylamine)platinum(II) ascorbate.
Claim 12
Dependent Claim
12 words
The composition of claim 10 wherein the active ingredient is cis-diamineplatinum(II) ascorbate.
Claim 13
Dependent Claim
13 words
The composition of claim 10 wherein the active ingredient is cis-bis(lower alkylamine)platinum(II) ascorbate.
Claim 14
Dependent Claim
12 words
The composition of claim 12 wherein the active ingredient is cis-bis(methylamine)platinum(II) ascorbate.
Claim 15
Dependent Claim
85 words
The composition of claim 9 wherein A 2 in the complex: cis-[Pt(II)A 2 (X) m (OH) n ] represents a bidentate amine ligand of the formula: ##STR4## wherein each of R 1 and R 2 , taken separately, is selected from the group consisting of hydrogen and lower alkyl, or R 1 and R 2 , taken together, afford a 1,2-diaminocycloalkane ligand containing from about 4-8 nuclear carbon atoms which may be optionally substituted by one or more linear or branched chain lower alkyl groups.
Claim 16
Dependent Claim
12 words
The composition of claim 14 wherein the active ingredient is ethylenediamineplatinum(II) ascorbate.
Claim 17
Dependent Claim
12 words
The composition of claim 14 wherein the active ingredient is 1,2-diaminocyclohexaneplatinum(II) ascorbate.
Claim 18
Dependent Claim
22 words
The composition of claim 9 wherein the complex: cis-[Pt(II)A 2 (X) m (OH) n ] represents a mixture of cis-diamine-platinum(II) ascorbate compounds.
Claim 19
Dependent Claim
12 words
The composition of claim 9 in a form suitable for parenteral administration.
Claim 20
Dependent Claim
12 words
The composition of claim 9 in a form suitable for oral administration.
Claim 21
Dependent Claim
11 words
The composition of claim 19 in the form of a tablet.
Claim 22
Dependent Claim
8 words
The composition of claim 19 in capsule form.
Claim 23
Dependent Claim
19 words
The composition of claim 9 wherein the active ingredient is present in an amount of from about 10-450 mg/kg.
References Cited (Backward Citations)
GB488784A
Cited
FR3385M
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US4140707A
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US4140707B1
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US4211712A
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US4234500A
Cited
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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) | 1987-07-03 | 1988-01-02 | 1988-07-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-07-03 | 1992-01-02 | 1992-07-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-07-03 | 1996-01-02 | 1996-07-03 | $7700.00 | Window Closed / Lapsed |