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US4565884A
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Bis-platinum complexes as antitumor agents
Assignee: ANDRULIS RESEARCH Corp 7315 WISCONSIN AVENUE BETHESDA MN 20814
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Filing: 1984-05-10
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Granted: 1986-01-21
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Expires: 2004-05-10
Abstract
Abstract Bis-platinum complexes having the formula ##STR1## wherein A is a ligand having two pairs of platinum-coordinating acidic groups which are each independently a carboxylate, phenolate, sulfonate or phosphonate group, each said pair being capable of coordinating with a platinum ion to form a 5-10 membered chelate ring; Z is a water-solubilizing group; n is 0 or a positive integer, with the proviso that n is 0 only when at least one of said platinum-coordinating acidic groups is sulfonate or phosphonate or when at least one platinum ion is a Pt(IV) ion; and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each independently H or a C 1-20 alkyl, aryl, aralkyl, or alkaryl group, or together form one or more C 1-30 alkylene, cycloalkylene, arylene, aralkylene or alkarylene groups; or a pharmaceutically acceptable salt thereof, are useful as readily water-soluble antitumor agents.
Inventors
- 👤 Peter J. Andrulis, Jr.
- 👤 Paul Schwartz
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 07:21
CPC Classifications
C; C07; C07C; C07C65/00; C07C65/01; C07C65/03; C07C65/05; C07C51/00; C07C51/41; C07C51/418; C07C61/00; C07C61/04; C07C61/08; C07C61/16; C07C61/28; C07C61/29; C07C63/00; C07C63/313; C07C63/33; C07C63/337; C07C63/34; C07C63/40; C07F; C07F15/00; C07F15/0006; C07F15/0086; C07F15/0093
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
145 words
A bis-platinum complex having the formula ##STR20## wherein A is a ligand having two pairs of platinum-coordinating acidic groups which are each independently a carboxylate, phenolate, sulfonate or phosphonate group, each said pair being capable of coordinating with a platinum ion to form a 5-10 membered chelate ring; Z is a water-solubilizing group; n is 0 or a positive integer, with the proviso that n is 0 only when at least one of said platinum-coordinating acidic groups is sulfonate or phosphonate, or when at least one platinum ion is a Pt(IV) ion; and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each independently H or a C 1-20 alkyl, aryl, aralkyl or alkaryl group, or together form one or more C 1-30 alkylene, cycloalkylene, arylene, aralkylene or alkarylene groups; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
145 words
A bis-platinum complex having the formula ##STR20## wherein A is a ligand having two pairs of platinum-coordinating acidic groups which are each independently a carboxylate, phenolate, sulfonate or phosphonate group, each said pair being capable of coordinating with a platinum ion to form a 5-10 membered chelate ring; Z is a water-solubilizing group; n is 0 or a positive integer, with the proviso that n is 0 only when at least one of said platinum-coordinating acidic groups is sulfonate or phosphonate, or when at least one platinum ion is a Pt(IV) ion; and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each independently H or a C 1-20 alkyl, aryl, aralkyl or alkaryl group, or together form one or more C 1-30 alkylene, cycloalkylene, arylene, aralkylene or alkarylene groups; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
17 words
A complex according to claim 1, wherein A is a mononuclear, dinuclear or trinuclear aromatic ring system.
Claim 4
Dependent Claim
17 words
A complex according to claim 2, wherein said aromatic ring system is a benzene or naphthalene ring.
Claim 5
Dependent Claim
29 words
A complex according to claim 3, wherein R 1 and R 4 together are 1,2-cyclohexylene, and R 2 , R 3 , R5 and R 6 are each H.
Claim 6
Dependent Claim
7 words
Benzenepentacarboxylatobis[(1,2-diaminocyclohexane)platinum(II)], a complex according to claim 4.
Claim 7
Dependent Claim
21 words
A complex according to clai 3, wherein A is ##STR21## wherein G and G' are said pair of platinum-coordinating acid groups.
Claim 8
Dependent Claim
21 words
A complex according to clai 3, wherein A is ##STR21## wherein G and G' are said pair of platinum-coordinating acid groups.
Claim 9
Dependent Claim
14 words
A complex according to claim 6, wherein G and G' are both carboxylate groups
Claim 10
Dependent Claim
15 words
A complex according to claim 6, wherein at least one G is a phenolate oxygen.
Claim 11
Dependent Claim
30 words
A complex according to claim 6, wherein in each said G and G' pair, one of G and G' is a carboxylate group and the other is a phenolate oxygen.
Claim 12
Dependent Claim
16 words
A complex according to claim 1, wherein A is a monocyclic or polycyclic alicyclic ring system.
Claim 13
Dependent Claim
13 words
A complex according to claim 1, wherein A is a non-cyclic aliphatic chain.
Claim 14
Dependent Claim
30 words
A complex according to claim 1, wherein R 1 and R 4 together are 1,2-cyclohexylene; and R 2 , R 3 , R 5 and R 6 are each H.
Claim 15
Dependent Claim
14 words
A complex according to claim 1, wherein Z is COOH or SO 3 H.
Claim 16
Dependent Claim
14 words
A complex according to claim 1, wherein Z is a C 1-12 polyhydroxylic group.
Claim 17
Dependent Claim
14 words
A complex according to claim 14, wherein Z is a mono- or polysaccharide moiety
Claim 18
Dependent Claim
10 words
A complex according to claim 1, wherein Pt is Pt(II).
Claim 19
Dependent Claim
10 words
A complex according to claim 1, wherein n is 1-4.
Claim 20
Dependent Claim
39 words
A complex according to claim 1, wherein A has the formula ##STR22## wherein LGG' and L'GG' are each independently a bidentate ligand, G and G' being said pair of platinum-coordinating acid groups; and Q is a divalent linking moiety.
Claim 21
Dependent Claim
108 words
A complex according to claim 18, wherein Q is --N═N--; --CO--; --SO 2 --; --NHCO--(CH 2 ) p --CONH--, p being an integer from 0 to 30; --NHCONH--(CH 2 ) q --NHCONH--, q being an integer from 1 to 30; --(CR 1l R 2 )m--, R 1 and R 2 each independently being H, C 1-20 -alkyl, aryl, alkaryl, aralkyl, alkylidene, aralkylidene or quinoidal, m being an integer from 1 to 30; --N═N--Ar--Q'--, Ar being arylene; Q' being a divalent linking group selected from a single bond, --NHCO--, --NHCONH--, --CONH--, CH 2 , --CO-- and --SO 2 --; and --COO--R 3 --OOC--, R 3 being alkylene or arylene.
Claim 22
Dependent Claim
19 words
A complex according to claim 18, wherein L and L' are each aryl; and Q is --N═N-- or --CO--.
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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) | 1989-01-20 | 1989-07-22 | 1990-01-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-01-20 | 1993-07-22 | 1994-01-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-01-20 | 1997-07-22 | 1998-01-21 | $7700.00 | Window Closed / Lapsed |