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US4797393A
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Bis-platinum complexes as chemotherapeutic agents
Assignee: University of Vermont
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Filing: 1986-07-25
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Granted: 1989-01-10
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Expires: 2006-07-25
Abstract
Abstract A bis-platinum complex having the structure: ##STR1## wherein X and Y are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate or dicarboxylate. B and C are the same or different and are primary or secondary amines, or pyridine type nitrogens. A is a diamine or polyamine wherein the primary amine N atoms are coordinated to the Pt atom such that platinum is present as Pt 2+ . The complexes are useful in the inhibition of tumors.
Inventors
- 👤 Nicholas Farrell
- 👤 Miles P. Hacker
- 👤 John J. McCormack
- 👤 Sergio G. DeAlmeida
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 21:02
CPC Classifications
C; C07; C07F; C07F15/00; C07F15/0006; C07F15/0086; C07F15/0093; A; A61; A61P; A61P35/00
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
76 words
A bis-platinum complex having the structure: ##STR5## in which X and Y are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, or dicarboxylate; B and C are the same or different groups selected from primary and secondary amines and pyridine type nitrogens; and A is a diamine or polyamine wherein the primary amine N atoms are coordinated to the Pt atom such that platinum is present as Pt 2+ .
Claim 2
Dependent Claim
76 words
A bis-platinum complex having the structure: ##STR5## in which X and Y are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, or dicarboxylate; B and C are the same or different groups selected from primary and secondary amines and pyridine type nitrogens; and A is a diamine or polyamine wherein the primary amine N atoms are coordinated to the Pt atom such that platinum is present as Pt 2+ .
Claim 3
Dependent Claim
121 words
The complex according to claim 1 wherein A has the formula: NDE--(C(R.sup.4).sub.2).sub.n (R.sup.5).sub.o (C(R.sup.6).sub.2).sub.p --NDE wherein n and p are integers from 1 to 4, inclusive, and o is 0 or 1; R 4 and R 6 are the same or different and are hydrogen, lower alkyl, aryl, cycloalkyl, cycloalkenyl, aralkyl, halogen, pseudohalogen, hydroxy, alkoxy, aryloxy, carboxylic ester, or carboxylic acid salt; D and E are the same or different and are hydrogen, lower alkyl, aryl, alkaryl, aralkyl, alkenyl, cycloalkyl, cycloalkenyl, halogen, pseudohalogen, hydroxy, alkoxy, aryloxy, sulphonic acid, or sulphonic acid salt; and R 5 is alkyl, aryl, amino, alkylamino, diamino of the formula: --(NH(CH.sub.2).sub.q NH)-- wherein q is an integer of 1 to 4, inclusive, hydroxyalkyl, alkoxy, sulfur or oxygen.
Claim 4
Dependent Claim
22 words
The complex of claim 2 wherein o is 0, and R 4 , R 6 , D and E are all hydrogen.
Claim 5
Dependent Claim
18 words
The complex of claim 1 wherein X and Y are all chlorine and B and C are amines.
Claim 6
Dependent Claim
18 words
The complex of claim 3 wherein X and Y are all chlorine and B and C are amines.
Claim 7
Dependent Claim
12 words
The complex of claim 1 wherein A is a naturally occurring polyamine.
Claim 8
Dependent Claim
12 words
The complex of claim 6 wherein the polyamine is spermidine or spermine.
Claim 9
Dependent Claim
27 words
The complex of claim 1 wherein A is H 2 N--(CH 2 ) r --NH 2 , and r is an integer from 2 to 12, inclusive.
Claim 10
Dependent Claim
59 words
The complex of claim 1 wherein X and Y are carboxylates or substituted carboxylates of the formula: CR.sup.3.sub.3 (C(R.sup.3).sub.2).sub.m CO.sub.2 wherein m is an integer from 0 to 5, inclusive; and the R 3 groups are the same or different and are hydrogen, substituted or unsubstituted straight or branched alkyl, aryl, alkaryl, carboxylic acid ester, or carboxylic acid salt.
Claim 11
Dependent Claim
67 words
The complex of claim 1 wherein X and Y combine to form a dicarboxylate of the formula: (R.sup.1 R.sup.2 C).sub.k (CH.sub.2).sub.1 (COO).sub.2 wherein R 1 and R 2 are the same or different, and are hydrogen, straight or branched alkyl or hydroxy substituted alkyl of 1-5 carbon atoms; and k and 1 are the same or different and are each an integer between 0 and 4, inclusive.
Claim 12
Dependent Claim
18 words
The complex of claim 10 wherein the dicarboxylate is oxalate, malonate, or malonate substituted by methyl or hydroxyethyl.
Claim 13
Dependent Claim
91 words
A bis-platinum complex having the structure: ##STR6## in which X and Y are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, or dicarboxylate; B and C are the same or different groups selected from primary and secondary amines and pyridine type nitrogens; the Z groups are the same or different and are nitrate, halogen, pseudohalogen, or hydroxy; and A is a diamine or polyamine wherein the primary amine N atoms are coordinated to the Pt atom such that platinum is present as Pt 4+ .
Claim 14
Dependent Claim
91 words
A bis-platinum complex having the structure: ##STR6## in which X and Y are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, or dicarboxylate; B and C are the same or different groups selected from primary and secondary amines and pyridine type nitrogens; the Z groups are the same or different and are nitrate, halogen, pseudohalogen, or hydroxy; and A is a diamine or polyamine wherein the primary amine N atoms are coordinated to the Pt atom such that platinum is present as Pt 4+ .
Claim 15
Dependent Claim
11 words
The complex of claim 12 wherein Z is hydroxy or chloro.
Claim 16
Dependent Claim
120 words
The complex according to claim 12 wherein A has the formula: NDE--(C(R.sup.4).sub.2).sub.n (R.sup.5).sub.o (C(R.sup.6).sub.2).sub.p --NDE wherein n and p are integers from 1 to 4, inclusive, and o is 0 or 1; R 4 and R 6 are the same or different and are hydrogen, lower alkyl, aryl, alkaryl, cycloalkyl, cycloalkenyl, aralkyl, halogen, pseudohalogen, hydroxy, alkoxy, aryloxy, carboxylic ester, or carboxylic acid salt and are the same or different and are hydrogen, lower alkyl, aryl, alkaryl, aralkyl, alkenyl, cycloalkyl, cycloalkenyl, halogen, pseudohalogen, hydroxy, alkoxy, aryloxy, sulphonic acid, or sulphonic acid salt, and R 5 is alkyl, aryl, amino, alkylamino, diamino of the formula: --(NH(CH.sub.2).sub.q NH)-- wherein q is an integer of 1 to 4 inclusive, hydroxyalkyl, alkoxy, sulfur or oxygen.
Claim 17
Dependent Claim
22 words
The complex of claim 13 wherein o is 0, and R 4 , R 6 , D and E are all hydrogen.
Claim 18
Dependent Claim
18 words
The complex of claim 12 wherein X and Y are all chlorine and B and C are amines.
Claim 19
Dependent Claim
18 words
The complex of claim 14 wherein X and Y are all chlorine and B and C are amines.
Claim 20
Dependent Claim
12 words
The complex of claim 12 wherein A is a naturally occurring polyamine.
Claim 21
Dependent Claim
12 words
The complex of claim 1 wherein the polyamine is spermidine or spermine.
Claim 22
Dependent Claim
27 words
The complex of claim 12 wherein A is H 2 N--(CH 2 ) r --NH 2 , and r is an integer from 2 to 12, inclusive.
Claim 23
Dependent Claim
19 words
A pharmaceutical composition comprising an effective amount of a complex according to claim 1 in a pharmaceutically acceptable carrier.
Claim 24
Dependent Claim
19 words
A pharmaceutical composition comprising an effective amount of a complex according to claim 12 in a pharmaceutically acceptable carrier.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1992-01-10 | 1992-07-11 | 1993-01-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-01-10 | 1996-07-11 | 1997-01-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-01-10 | 2000-07-11 | 2001-01-10 | $7700.00 | Window Closed / Lapsed |