Dendrimer and an active substance occluded in the dendrimer, a process for the preparation thereof and a process for releasing the active substance
First Claim
1. A composition comprising at least one dendrimer and at least one active substance occluded in said dendrimer, wherein the dendrimer has terminal groups, and wherein a sufficient number of said terminal groups are blocked with blocking agents whereby said active substance is occluded within said dendrimer.
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Accused Products
Abstract
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.
32 Citations
16 Claims
- 1. A composition comprising at least one dendrimer and at least one active substance occluded in said dendrimer, wherein the dendrimer has terminal groups, and wherein a sufficient number of said terminal groups are blocked with blocking agents whereby said active substance is occluded within said dendrimer.
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13. A process for the preparation of a dendrimer having at least one active substance occluded therein, which comprises adding an amount of an active substance to be occluded to a reaction mixture containing a dendrimers having terminal groups, and simultaneously or subsequently adding an amount of blocking agent provided with protective groups to block a sufficient number of said terminal groups to effect occlusion of said active substance in said dendrimer.
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14. A process for releasing an active substance from a dendrimer having at least one active substance occluded therein wherein said dendrimer has terminal groups, and a sufficient number of said terminal groups are blocked with a blocking agent, which comprises releasing said active substance by splitting off or modifying a blocking-effective amount of the blocking agent.
- 15. A process for releasing an active substance from a dendrimer having at least one active substance occluded therein wherein said dendrimer has terminal groups, and a sufficient number of said terminal groups are blocked with a blocking agent which is protected with a protective group, which process comprises the step of splitting off a sufficient number of said protecting groups.
Specification