A Spanish research group from the Department of Organic and Inorganic Chemistry of Alcala University has developed a highly branched macromolecules called dendrimers or dendrons, with carbosilane structure and functionalized on its periphery with anionic or cationic groups, providing the macromolecule a net negative or positive charge respectively. The invention also concerns the dendrimers’ procurement process and their biomedical applications, particularly as carriers of drugs or nucleic acids (such ODN, siRNA, dsRNA or DNA), or as therapeutic agents with antiviral or antibacterial activity. The group is looking for companies in the biomedical sector to reach licensing agreements, collaboration and commercial agreements with technical assistance.
New and innovative aspects
The procedure for preparing the compounds of the invention allows:
- Versatility in the synthesis of cationic or anionic nature, dendrimers and dendrons.
- Possibility to synthesize heterofunctionalized dendrimers or dendrons.
- Possibility of using carbosilane dendrons for the functionalization of other systems, such as nanoparticles, carbon nanotubes, etc.
Main advantages of its use
- The compounds play more than one role simultaneously.
-The compounds are stable and soluble in water in their ionic forms and can be isolated with a high performance.
The present invention provides highly branched macromolecules, dendrimers or dendrons, of carbosilane structure and its periphery functionalized with anionic groups (such carboxylate, sulfonate or sulfate), that give the macromolecule a net negative charge or cationic (ammonium) giving the dendrimer a net positive charge. Preferably the dendrimers have a polyphenol or silicon atom nucleus. The procedure for preparing the compounds of the invention allows, through a simple process, the versatility in the synthesis of dendrimers or dendrons, with anionic or cationic nature, and also the possibility of synthesizing dendrimers or dendrons heterofunctionalized which consists on the above molecules but with one or more of its branches replaced with different groups such as chromophore, targetting groups or others with therapeutic activity.
The present invention includes not only the compounds per se, but any of its salts, for example alkaline metal salts or alkaline earth metal. For example it may be selected from sodium, potassium or calcium salts. Therefore, the present invention provides dendritic compounds, dendrimers or dendrons, which also contain groups that provide a number of useful properties in biomedicine and can introduce in its outer layer at least one group with different functionality to produce a multifunctional compound with great versatility in their application.
In a preferred procedure, the compound of the invention may be a dendrimer or dendron of first, second, third or fourth subsequent generation. The term "generation" refers to the number of iterative ramifications that are necessary for the compound preparation. Another aspect of the present invention relates to a method of preparing the compounds of the invention which comprises a thiol-ene or thiol–ino reaction, between a precursor of that compound with olefins or terminal alkynes, respectively, and the thiol group.
- Pharmaceutical or biomedical companies
- Biomedical applications, particularly as carriers of drugs or nucleic acids (such ODN, siRNA, dsRNA or DNA), or as therapeutic agents with antiviral or antibacterial activity.