Carbosilane metallodendrimers containing ruthenium and copper ions coordinated to Schiff base ligands, their preparation and uses

Summary of the technology

The Research Group BIONANODEN "Dendritic Nanosystems for Biomedical Applications " of the University of Alcalá presents a new invention that refers to obtaining dendritic systems decorated with metalcomplexes with antitumour and antibacterial activity. The compoundscomprise a dendritic skeletonof different topology, mainly of carbosilane-based, and metal complexes, mainly copper(II) and ruthenium(II) complexes.The group seeks to reach collaboration agreements, licensing or commercial agreements with technical assistance, with companies fromthe biotechnology, pharmaceutical and biomedicine sectors in general.

Universidad de Alcalá-OTRI

Details of the Technology Offer

DESCRIPTION AND SPECIAL FEATURES

The present invention relates tothe preparation of metallodendrimers fortheiruse in thetreatment of various cancers, especially advanced prostate cancer, as well as infectious diseasescaused by bacteria and other biomedical applications.These systems are based oncarbosilanedendritic skeletonsfunctionalized on their periphery withSchiff bases capable of coordinating metal atoms, in this specific case the metals coordinated to thedendritic system are Cu(II) and Ru(II).

The preparation of the metallodendrimers is carried out by coordinating thecorrespondingmetalsalt to theSchiff base groups of the precursor dendrimers, through simple synthetic routes withhigh yields.In the metallodendrimers of the present invention, the dendrimer significantly increases thetherapeuticactivitywith respect to the isolated metal complexes. Its antitumor activity in a varietyof cell lines (derived from breast, cervix, prostate and colon tumours) is in the micromolar range andis selective, up to 16 times more active in tumourcelllines than in healthy ones. This antitumouractivity is reproducible inin vivoassays, reducingup to 36%the volume ofthesubcutaneoustumour in immunosuppressed mice. In addition, they show bacteriostatic and bactericidal activity inboth Gram+ and Gram-type bacteria.

Therefore, these compounds are an interesting alternative fortheuse in the pharmaceutical industry, and can be employedas new drugs or formulationscontaining them, for the treatment of tumour diseases and as antimicrobial drugs.Preferably this inventionaims forthe development of drugs forthe treatment of cancer, especiallyof prostatecancer, as well as for the treatment of bacterial diseases. However, other types ofcancers and microbial diseases are not excluded. Examples of pharmaceutical preparations includeany solid (tablets, pills,capsules, granules, etc.) or liquid (gels, solutions, suspensions or emulsions)composition for oral, nasal, topicalor parenteral administration.

INNOVATIVE ASPECTS

-Due to the lipophilic nature of the skeleton, even small generation systems have a high interactionwith biological membranes, resulting in high biological activity and synthetic cost savings.

-The preparation process is highly versatile and caneasilygenerate metallodendrimersbased ondifferent metals and on demand depending on the application.

-The dendritic nature gives these derivatives a nanoscopic size and a multivalence (capacity to hostmultiple groups on its surface) that can favour the properties of these compounds and differentfrom whatitwouldbe foundin these same groups if they were individually.

COMPETITIVE ADVANTAGES

-Biodistribution tests carried out by ICP, after severalin vivoassays, show that they are eliminatedby urine and faeces, presenting low cardiotoxicity and low-moderate liver damage .

-The necessary development, for the commercial exploitation of thispatent, does not involve ahigh technical difficulty.

COMMENTS

The research grouplooksforcompanies in the pharmaceutical or biotechnology, pharmaceuticaland healthsector to sign cooperation agreements, commercial agreements, licensing orpharmaceutical manufacturingagreementsof the compounds.The main application of the patented compounds lies in their antitumour activity, preferablyagainst advanced prostate cancer, as well as their antibacterial activity.

Intellectual property status

Granted Patent

Patent number : ES2735282

Where : Spain

Granted Patent

Patent number : WO2019239001

Where : International extension

Desired business relationship

Technology development

Other : Commercial agreement with technical assistance

Other : License Agreement

Other : Manufacturing agreement

Related Keywords

  • Light metals
  • Metals and Alloys
  • Cytology, Cancerology, Oncology
  • Virus, Virology / Antibiotics / Bacteriology
  • Biological Sciences
  • Biology / Biotechnology
  • Industrial Biotechnology
  • Speciality metals (including processes for working with metals)
  • Machine tools, other metal working equipment (excluding numeric control)
  • Industrial Products
  • Industrial Equipment and Machinery
  • metal
  • antibacterial
  • prostate
  • anticancer
  • carbosilane
  • dendrimer

About Universidad de Alcalá-OTRI

The Technology Transfer Office at Alcalá University serves as a liaison between the University and its socioeconomic environment in terms of research and innovation. It encorages collaboration between research groups from universities and companies/institutions, with the objective to promote and commercialize research results and scientific capabilities.

Some of the services offered by this office are specified in the following list:

- Promotion of R & D and improvement of the relationships with companies.
- Promote the participation in R & D projects applicants to public calls (regional, national and European).
- Advising, processing and monitoring of patents and other forms of industrial protection.
- Support in the negotiation of contracts and agreements for R&D&i

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