EP0113508A1
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EP
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Hydrophobic platinum compounds and their preparation
Assignee: Inco Research and Development Center Inc
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Filing: 1983-11-04
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Granted: —
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Expires: 2003-11-04
Abstract
Abstract Novel cis-platinum (II) compounds having amino and phosphatidic acid substituents, which may be incorporated in a phospholipid vesicle for therapeutic treatment of mammals, and their preparation.
Inventors
- 👤 Barry Sears
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-29 18:39
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K9/1271; C; C07; C07F; C07F15/00; C07F15/0006; C07F15/0086; C07F15/0093
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
106 words
A compound of the formula: wherein R 1 and R 2 are selected from the group NH 3 , 1,2 diaminocyclohexyl, cyclohexylaminyl, cyclopentylaminyl and isoamylaminyl, with the proviso that R 1 and R 2 are identical or, in the case of 1, 2 diaminocyclohexyl, R 1 and R 2 may be satisfied by the amino groups on the same ring to provide a bridging ligand; R 3 is a phosphatidyl group (PG) having a net negative charge and having fatty acid substituents containing from 12 to 20 carbon atoms and which may be saturated or unsaturated; and R 4 is a biologically compatible negatively charged ion.
Claim 2
Dependent Claim
106 words
A compound of the formula: wherein R 1 and R 2 are selected from the group NH 3 , 1,2 diaminocyclohexyl, cyclohexylaminyl, cyclopentylaminyl and isoamylaminyl, with the proviso that R 1 and R 2 are identical or, in the case of 1, 2 diaminocyclohexyl, R 1 and R 2 may be satisfied by the amino groups on the same ring to provide a bridging ligand; R 3 is a phosphatidyl group (PG) having a net negative charge and having fatty acid substituents containing from 12 to 20 carbon atoms and which may be saturated or unsaturated; and R 4 is a biologically compatible negatively charged ion.
Claim 3
Dependent Claim
15 words
A compound according to claim 1 wherein R 4 is PG, NO 3 and Cl.
Claim 4
Dependent Claim
19 words
A compound in accordance with claim 1 wherein R 1 and R 2 comprise a 1,2 diaminocyclohexyl bridging ligand.
Claim 5
Dependent Claim
56 words
A compound according to claim 1, being dipalmitoyl phosphatidic acid 1,2 diaminocyclohexane cis Pt(II), dioleyl phosphatidic acid 1,2 diaminocyclohexane cis Pt (II), egg phosphatidic acid 1, 2 diaminocyclohexane cis Pt (II), soy phosphaditic acid bis cyclohexylamine cis Pt (II), soy phosphaditic acid bis cyclopentylamine cis Pt (II), or soy phosphaditic acid bis isoamylamine cis Pt (II).
Claim 6
Dependent Claim
12 words
A compound according to any preceding claim incorporated in a phospholipid vesicle.
Claim 7
Dependent Claim
13 words
A compound according to claim 5 wherein said phospholipid is a phosphatidyl choline.
Claim 8
Dependent Claim
61 words
Method for preparing a cis platinum II phosphatidyl analogue according to claim 1 which comprises reacting a phosphatidyl donor with a dinitrato cis platinum II compound in a liquid reaction medium in which both reactants are soluble to interchange at least one phosphatidyl group with one nitrato group and precipitate the resulting cis platinum II phosphatidyl analogue from said liquid medium.
Claim 9
Dependent Claim
17 words
Method according to claim 7 wherein the phosphatidyl donor is an ammonium salt of a phosphatidic acid.
Claim 10
Dependent Claim
28 words
Method according to claim 6 or claim 7 wherein the dielectric strength of the reaction medium is equivalent to that of methanol containing about 17% water, by volume.
References Cited (Backward Citations)
FR2517310A1
Cited
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