US4661516A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Diaminocyclohexane platinum complexes
Assignee: Research Corp
•
Filing: 1985-04-15
•
Granted: 1987-04-28
•
Expires: 2005-04-15
Abstract
Abstract Diaminocyclohexane platinum complexes having the structural formula ##STR1## wherein: X is a monovalent anion selected from the group consisting of isoascorbate, monosaccharate, saccharate-4-lactone, shikimate, isethionate, 2-aminoethylsulfate, azetidinecarboxylate, proline, hydroxyproline, pipecolinate, cyclopropanecarboxylate, cyclobutanecarboxylate, cyclopentanecarboxylate, cyclopentenecarboxylate, cyclohexanecarboxylate, cyclohexenecarboxylate, bicine, glycine, 2-aminoethanesulfonate, 2-chloroethanesulfonate and Y is a divalent anion selected from the group consisting of iminodiacetate, isocitratelactone, furanedicarboxylate, cyclopropane-1,1-dicarboxylate, isocitratomonoethylester, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-benzyliminodiacetate, N-phenyliminodiacetate, N-(2-acetamido)iminodiacetate, cyclohexane-1,1-diacetate, trans-1,2-cyclopropanedicarboxylate, trans-1,2-cyclobutanedicarboxylate, trans-1,2-cyclopentanedicarboxylate and trans-1,2-cyclohexanedicarboxylate and their use in the treatment of tumors.
Inventors
- 👤 David B. Brown, deceased
- 👤 Abdul R. Khokhar
- 👤 Miles P. Hacker
- 👤 John J. McCormack
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 13:43
CPC Classifications
C; C07; C07C; C07C309/00; C07C51/00; C07C51/41; C07C51/418; C07C55/00; C07C55/26; C07C55/28; C07C59/00; C07C59/01; C07C59/10; C07C59/105; C07C61/00; C07C61/04; C07C61/06; C07C61/08; C07C61/09; C07C61/16; C07C61/20; C07C61/22; C07F; C07F15/00; C07F15/0006; C07F15/0086; C07F15/0093
Claims Analysis
Total Claims: 88
Claim 1
Independent Claim
70 words
A water-soluble square-planar DACH cis-platinum(II) four-coordinate complex having the formula: ##STR6## wherein: X is a monovalent anion selected from the group consisting of, monosaccharate, saccharate-4-lactone, shikimate, isethionate, 2-aminoethylsulfate, azetidinecarboxylate, proline, hydroxyproline, pipecolinate, cyclopropanecarboxylate, cyclobutanecarboxylate, cyclopentanecarboxylate, cyclopentenecarboxylate, cyclohexanecarboxylate, cyclohexenecarboxylate, bicine, glycine, 2-aminoethanesulfonate, 2-chloroethanesulfonate and Y is a divalent anion selected from the group consisting of iminodiacetate, isocitratelactone, furanedicarboxylate, cyclopropane-1,1-dicarboxylate, isocitratomonoethylester, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-benzyliminodiacetate, N-phenyliminodiacetate, N-(2-acetamido)iminodiacetate, cyclohexane-1,1-diacetate, trans-1,2-cyclopropanedicarboxylate, trans-1,2-cyclobutanedicarboxylate, trans-1,2-cyclopentanedicarboxylate and trans-1,2-cyclohexanedicarboxylate.
Claim 2
Dependent Claim
70 words
A water-soluble square-planar DACH cis-platinum(II) four-coordinate complex having the formula: ##STR6## wherein: X is a monovalent anion selected from the group consisting of, monosaccharate, saccharate-4-lactone, shikimate, isethionate, 2-aminoethylsulfate, azetidinecarboxylate, proline, hydroxyproline, pipecolinate, cyclopropanecarboxylate, cyclobutanecarboxylate, cyclopentanecarboxylate, cyclopentenecarboxylate, cyclohexanecarboxylate, cyclohexenecarboxylate, bicine, glycine, 2-aminoethanesulfonate, 2-chloroethanesulfonate and Y is a divalent anion selected from the group consisting of iminodiacetate, isocitratelactone, furanedicarboxylate, cyclopropane-1,1-dicarboxylate, isocitratomonoethylester, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-benzyliminodiacetate, N-phenyliminodiacetate, N-(2-acetamido)iminodiacetate, cyclohexane-1,1-diacetate, trans-1,2-cyclopropanedicarboxylate, trans-1,2-cyclobutanedicarboxylate, trans-1,2-cyclopentanedicarboxylate and trans-1,2-cyclohexanedicarboxylate.
Claim 3
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR7##
Claim 4
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR8##
Claim 5
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR9##
Claim 6
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR10##
Claim 7
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR11##
Claim 8
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR12##
Claim 9
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR13##
Claim 10
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR14##
Claim 11
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR15##
Claim 12
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR16##
Claim 13
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR17##
Claim 14
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR18##
Claim 15
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR19##
Claim 16
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR20##
Claim 17
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR21##
Claim 18
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR22##
Claim 19
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR23##
Claim 20
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR24##
Claim 21
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR25##
Claim 22
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR26##
Claim 23
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR27##
Claim 24
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR28##
Claim 25
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR29##
Claim 26
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR30##
Claim 27
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR31##
Claim 28
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR32##
Claim 29
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR33##
Claim 30
Dependent Claim
10 words
A platinum complex of claim 1 having the formula: ##STR34##
Claim 31
Dependent Claim
21 words
A water-soluble square-planar DACH cis-platinum (II) four-coordinate complex having the formula: ##STR35## wherein Y is iminodiacetate, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-phenyliminodiacetate or N-benzyliminodiacetate.
Claim 32
Dependent Claim
21 words
A water-soluble square-planar DACH cis-platinum (II) four-coordinate complex having the formula: ##STR35## wherein Y is iminodiacetate, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-phenyliminodiacetate or N-benzyliminodiacetate.
Claim 33
Dependent Claim
9 words
A complex according to claim 38 which is trans-R,R-DACH-Pt(II).
Claim 34
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is iminodiacetato(DACH)Pt(II).
Claim 35
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is iminodiacetato(trans-R,R-DACH)Pt(II).
Claim 36
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-methyliminodiacetato(DACH)Pt(II).
Claim 37
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-methyliminodiacetato(trans-R,R-DACH)Pt(II).
Claim 38
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-(2-hydroxyethyl)iminodiacetato(DACH)Pt(II).
Claim 39
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-(2-hydroxyethyl)iminodiacetato(trans-R,R-DACH)Pt(II).
Claim 40
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-phenyliminodiacetato(DACH)Pt(II).
Claim 41
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-phenyliminodiacetato(trans-R,R-DACH)Pt(II).
Claim 42
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-benzyliminodiacetato(DACH)Pt(II).
Claim 43
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-benzyliminodiacetato(trans-R,R-(DACH)Pt(II).
Claim 44
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-(2-acetamido)-iminodiacetato(DACH)Pt(II).
Claim 45
Dependent Claim
12 words
A platinum complex according to claim 1 wherein the complex is N-(2-acetamido)-iminodiacetato(trans,R,R-DACH)Pt(II).
Claim 46
Dependent Claim
20 words
A platinum complex of claim 1 having the formula: ##STR36## wherein R is hydrogen, phenyl, 2-acetamido, methyl, 2-hydroxyethyl or benzyl.
Claim 47
Dependent Claim
41 words
A pharmaceutical composition in unit dosage form suitable for administration to an animal afflicted with tumor cells sensitive to a platinum complex of claim 1 comprising a therapeutically anti-tumor effective amount of said platinum complex and a pharmaceutically acceptable carrier therefor.
Claim 48
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR37##
Claim 49
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR38##
Claim 50
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR39##
Claim 51
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR40##
Claim 52
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR41##
Claim 53
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR42##
Claim 54
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR43##
Claim 55
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR44##
Claim 56
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR45##
Claim 57
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR46##
Claim 58
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR47##
Claim 59
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR48##
Claim 60
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR49##
Claim 61
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR50##
Claim 62
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR51##
Claim 63
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR52##
Claim 64
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR53##
Claim 65
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR54##
Claim 66
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR55##
Claim 67
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR56##
Claim 68
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR57##
Claim 69
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR58##
Claim 70
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR59##
Claim 71
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR60##
Claim 72
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR61##
Claim 73
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR62##
Claim 74
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR63##
Claim 75
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR64##
Claim 76
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR65##
Claim 77
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR66##
Claim 78
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR67##
Claim 79
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR68##
Claim 80
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR69##
Claim 81
Dependent Claim
13 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR70##
Claim 82
Dependent Claim
22 words
The composition of claim 45 wherein said platinum complex has the formula: ##STR71## wherein Y is iminodiacetate, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-phenyliminodiacetate or N-benzyliminodiacetate.
Claim 83
Dependent Claim
10 words
The composition of claim 80 wherein said complex is trans-R,R-DACH-Pt(II).
Claim 84
Dependent Claim
15 words
The composition of claim 81 wherein said platinum complex is mono-iminodiacetato-(trans-R,R-DACH)Pt(II) and aqueous complexes thereof.
Claim 85
Dependent Claim
15 words
The composition of claim 81 wherein said platinum complex is mono-N-methyliminodiacetato-(trans-R,R,-DACH)Pt(II) and aqueous complexes thereof.
Claim 86
Dependent Claim
15 words
The composition of claim 81 wherein said platinum complex is mono-N-hydroxyethyliminodiacetato-(trans-R,R-DACH)Pt(II) and aqueous complexes thereof.
Claim 87
Dependent Claim
15 words
The composition of claim 81 wherein said platinum complex is mono-N-phenyliminodiacetato-(trans-R,R-DACH)Pt(II) and aqueous complexes thereof.
Claim 88
Dependent Claim
15 words
The composition of claim 81 wherein said platinum complex is mono-N-benzyliminodiacetato-(trans-R,R-DACH)Pt(II) and aqueous complexes thereof.
References Cited (Backward Citations)
US2166076A
Cited
US4140707A
Cited
US4140707B1
Cited
US4169846A
Cited
US4256652A
Cited
US4203912A
Cited
US4242430A
Cited
US4410544A
Cited
US4255347A
Cited
US4234499A
Cited
US4457926A
Cited
US4462998A
Cited
GB2055377A
Cited
US4452812A
Cited
US4359425A
Cited
EP0055300A1
Cited
GB2128615A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-04-27 | 1990-10-27 | 1991-04-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-04-27 | 1994-10-27 | 1995-04-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-04-27 | 1998-10-27 | 1999-04-28 | $7700.00 | Window Closed / Lapsed |