EP0684044A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Composition consisting of a dendrimer and an active substance
Assignee: DSM BV
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Filing: 1995-05-24
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Granted: —
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Expires: 2015-05-24
Abstract
Abstract The invention relates to a composition consisting of a dendrimer provided with blocking agents and an active substance occluded in the dendrimer. According to the invention a blocking agent is a compound which is sterically of sufficient size, which readily enters into a chemical bond with the terminal groups of a dendrimer and which can also be split off from the dendrimer or be modified without thereby affecting the chemical structure of the dendrimer and the active substance. The blocking agent can be provided with protective groups. Such conjugates have the advantage that the time at which the releasing of the active substance starts, can be controlled. The invention also relates to a process for the preparation of such a composition and to a process for the controlled release of the active substance.
Inventors
- 👤 Johan Franz Gradus Antonius Jansen
- 👤 Egbert Willem Meijer
- 👤 Ellen Marleen Monique De Brabander-Van Den Berg
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 10:13
CPC Classifications
C; C08; C08G; C08G83/00; C08G83/002; C08G83/003; A; A61; A61K; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; B; B82; B82Y; B82Y5/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/582; Y10; Y10S; Y10S424/00; Y10S424/16
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
33 words
Composition consisting of a dendrimer and an active substance occluded in the dendrimer wherein the dendrimer has terminal groups, characterized in that the terminal groups of the dendrimer are provided with blocking agents.
Claim 2
Dependent Claim
19 words
Composition according to claim 1, characterized in that the blocking agents are at least partly provided with protective groups.
Claim 3
Dependent Claim
45 words
Composition according to claims 1-2, characterized in that the blocking agents are chosen from the group comprising branched and non-branched Michael acceptors, active esters which also comprise an ether and/or thiol group, amino acids, isocyanates, aziridines, acid chlorides, anhydrides, aldehydes, ketones, acrylates, chiral epoxides, bislactide.
Claim 4
Dependent Claim
18 words
Composition according to any one of claims 1-3, characterized in that the blocking agent is an amino acid.
Claim 5
Dependent Claim
40 words
Composition according to any one of claims 2-4, characterized in that the protective group is chosen from the range comprising hydrolyzable esters, ethers, thiol groups, sulphonic acid groups, trityl, silyl, BOC, FMOC, DBD-TMOC, Z, TEOC, AdMOC, STABASE and benzoSTABASE groups.
Claim 6
Dependent Claim
15 words
Composition according to claim 5, characterized in that the protective group is a BOC group.
Claim 7
Dependent Claim
28 words
Composition according to any one of claims 2-6, characterized in that at least 30% of the terminal groups are provided with a blocking agent with a protective group.
Claim 8
Dependent Claim
28 words
Composition according to claim 7, characterized in that at least 70% of the terminal groups of the dendrimer are provided with a blocking agent with a protective group.
Claim 9
Dependent Claim
18 words
Composition according to any one of claims 1-8, characterized in that the composition contains several different active substances.
Claim 10
Dependent Claim
64 words
Composition according to any one of claims 1-9, characterized in that the active substance belongs to the range of pharmaceutical compounds, agrochemicals, materials used in personal care products, cosmetic products, food additives, aspartame, additives for engineering plastics, signal absorbers, signal generators, chelating compounds, radicals, soaps, colourants, radio active labelled compounds, metals, metal compounds, radionuclides, electron deficient and non-metallic electron rich compounds and precursors thereof.
Claim 11
Dependent Claim
17 words
Composition according to any one of claims 1-10, characterized in that the dendrimer is a polypropylamine dendrimer.
Claim 12
Dependent Claim
18 words
Composition according to claim 11, characterized in that the dendrimer is a dendrimer of generation 4 or higher.
Claim 13
Dependent Claim
49 words
Process for the preparation of a composition according to any one of claims 1-12, characterized in that an amount of an active substance to be occluded is added to a reaction mixture containing dendrimers and simultaneously or subsequently an amount of blocking agent provided with protective groups is added.
Claim 14
Dependent Claim
32 words
Process for releasing an active substance from a composition according to any one of claims 1-12, characterized in that the active substance is released by splitting off or modifying the blocking agent.
Claim 15
Dependent Claim
30 words
Process for releasing an active substance from a composition according to any one of claims 2-12, characterized in that the active substance is released by splitting off the protective group.
Claim 16
Dependent Claim
27 words
Process according to claim 15, characterized in that the active substance is released by first splitting off the protective group and then splitting off the blocking agent.
Claim 17
Dependent Claim
55 words
Process according to any one of claims 13-16, characterized in that the protective group and/or the blocking agent are removed by means of a chemical reaction, hydrolysis in a neutral, acidic or basic medium, hydrogenation, a reaction under the influence of heat, a photochemical reaction, reaction in the presence of fluoride, a retro Michael reaction.
Claim 18
Dependent Claim
25 words
Process according to claim 14, characterized in that the active substance is released by changing the physical interactions within the dendrimer provided with blocking agents.
Claim 19
Dependent Claim
24 words
Composition, process for the preparation of the composition and process for releasing an active substance as described and elucidated by means of the examples.
References Cited (Backward Citations)
No citation records indexed.
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