Composition consisting of a dendrimer and an active substance

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

Dendrimer and an active substance occluded in the dendrimer : a process for the preparation thereof and a process for releasing the active substance

The invention relates to a dendrimer composition in which an effective number of the terminal functionalities are provided with blocking agents, and at least one active substance species is occluded in the dendrimer. A blocking agent is a sufficiently sterically sized compound which readily enters into a chemical bond with a terminal group of a dendrimer but which can also be split off from the dendrimer or can be modified without affecting the chemical structure of the dendrimer and the occluded active substance. The blocking agent can also be provided with a protecting group. The time and duration over which an active substance is released 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

Process for the preparation of a dendritic macromolecule

The invention relates to a process for the preparation of a dendritic macromolecule, wherein an amount of a core molecule comprising at least one functional group is dissolved in a solvent, after which alternatingly an addition reaction and a hydrogenation reaction are carried out, during the addition reaction vinyl cyanide units being added to the solution which react with the functional groups in such a manner that a dendritic macromolecule with terminal cyanide groups is formed, and during the hydrogenation reaction the cyanide groups being reduced in solution by means of hydrogen and a suitable catalyst in such a manner that functional amine groups are formed, wherein the solvent in which the hydrogenation reaction takes place is an alcohol which contains an amount of ammonia, the molar ratio between the amount of ammonia and the number of cyanide groups being higher than 0.8

Dendritic macromolecule and the preparation thereof

The invention relates to a dendritic macromolecule comprising a core and branches emanating from the core wherein the branches are based on vinyl cyanide and/or fumaryl dinatrile units. The invention also relates to processes for preparing these dendritic macromolecules. The dendritic macromolecules according to the invention are not sensitive to degradation through hydrolysis reactions and are also very stable at a high temperature. The processes are very suitable for large scale production of the dendritic macromolecules without requiring purification of reaction intermediates