FIND A PARTNER

TRANSBIO SUDOE aims at fostering interregional partnerships in the project area.
To find a partner do not hesitate to consult our join our TRANSBIO SUDOE Network Group on LinkedIn.
FIND A TECHNOLOGY PLATFORM
FIND A TECHNOLOGY TRANSFER OFFER
Find a technology transfer offer
TRANSBIO SUDOE aims at setting up a network of technology platforms in order to expand, through collaboration, the existing possibilities within each region. Please find below a list of technology platforms and advanced instrumentation that belong to the TRANSBIO SUDOE network.
Enter keywords here :
Search type :
Search by location : All Toulouse Barcelona Lisboa Galicia Bordeaux Isles Baleares Montpellier Valencia

New process to obtain polysubstituted pyrrolidines as inhibitors of the hepatitis C virus

Title : New process to obtain polysubstituted pyrrolidines as inhibitors of the hepatitis C virus
Abstract : A research team has developed a new process to obtain polysubstituted pyrrolidines as inhibitors of the hepatitis C virus. This process allows the preparation of enantioenriched polysubstituted proline derivatives after a three-step sequence. High purity, high yields and high enantiomeric ratios are achieved. The process is patented and pharmaceutical laboratories or companies are sought for license agreements or technical cooperations.
Description :

---------------------------

The research team has developed a highly enantioselective process catalysed by small amounts

of a chiral complex formed by a silver(I) salt and a chiral phosphoramidite. This method allows the

preparation of enantioenriched polysubstituted proline derivatives after a three-step sequence.

These prolines are widely used for multiple purposes, but the most important activity is based on

the high efficiency against the hepatitis C virus.The process is based on two chiral complexes

prepared including phosphoramidite units. These chiral molecules are prepared at room

temperature and avoiding light exposure. After that, some chemical reactions are applied and the

final inhibitor is synthesized. It results in a solid which crystallises as colourless sheets using nhexane/

diethyl ether as solvent (mp 126-127ºC dec.), [?]D20= +95 (c1,

MeOH).Innovative Aspects:* The administration of these drugs in mammalians is beneficial

because the risks of the multiple side effects are reduced and the required dose is very small,

unlike the mixture of the pharmaceuticals employed in the current therapy. •The processes are

highly enantioselectives. The final antiviral agents are obtained with very good ee’s. •The

chemical yields are very good, and the purity of the compounds is very high.•The procedure is

efficient and reproducible.At this moment, this methodology is the unique dealing with the

production of these antiviral agents in an highly enantioselective manner. This enantioselective

synthesis is very reliable, reproducible and allows to react very bulky starting materials giving high

chemical yields. This method is a clear example of the atom economy. The efficiency and

biological potential has been demonstrated in infected mice IC50= 0.3-0.5 ?M, (even lower

according to the new structures published in the literature)

State of Development and IPR : demonstrator
patent applied
Intended collaboration : joint R&D
licensing

Application or research field :

Cancer
Drug design
Immunity
Infection
Microbiology
Public health
Key words technology :
Transbio Contact : osanchez@cipf.es
Search results : 0 offer(s)
Title Abstract View information
All the technology offers : 17 offer(s)
Title Abstract View information
Drug Screening Platform (USEF), University of Santiago de Compostela USEF is a High Throughput Screening (HTS) technology platform, for determining the pharmacological/biological activity of compounds produced by public groups, biotechnological companies and the pharmaceutical industry. It is a reference within the academic public sector in Spain in drug discovery that offers track record in early drug discovery research with pharmaceutical and biotechnological companies from 1998. Also apply its know-how to the public sector, facilitating translation of basic academic research ideas to drug discovery projects, thus adding value to academic projects it collaborates with international research groups. View information
Technology Platform for BioMedical Innovation: PTIB (Service Offer) The key focus of this transfer is the development of testing of diagnostic and therapeutic tools. The Platform conducts R&D work from the preparatory phase of a project through to its completion, as well as subsequent performance monitoring. The Platform offers methodological and technical scientific support at every stage of the transfer process, with respect for laboratory best practices as well as ethical and legal rules, and in line with the regulatory standards (CE marking, G-Med assessment, AFSSaPs). View information
New Biodegradable and Biocompatible Nanovesicle (Technology Offer) The basis of the technology is the formation of new vesicles by the self-assembly of biodegradable and biocompatible polypeptide-b-polysaccharide bloc copolymers. These nanostructures (100nm) allow the encapsulation and transportation of natural or synthetic molecules with or without therapeutic properties. View information
Screening Kit for Medicinal Molecules against Mitochondrial Diseases (Technology Offer) The basis for this technology is a kit allowing the user to screen libraries of chemical molecules using strains of yeast. View information
Bio-microelectronic insulin demand sensor (Technology Offer) To precisely measure the demand in insulin and not only glycemia, we have for the first time used recordings on microelectrode arrays of electrical signals, the frequency of action potentials. These signals provide the first integrative read-out at the cellular level of all nutrients, sugars and hormones. We are able to detect online the electrical activity testifying for the insulin need. View information
Device for stimulating living tissues by micro electrodes (Technology Offer) Here, we propose a new electrode configuration that improves the focality of electrical stimulation without the need to consider multipolar electrodes. In this configuration, we introduce a ground surface surrounding all the electrodes of the array. Stimulations are delivered between each electrode of the array and the ground surface. Using this configuration, stimulation is all the more focal that the surface conductance of the ground surface is high. View information
Calcemia and Response to Anticancer Drugs (Technology Offer) This invention is based on the original discovery that intracellular calcium ([Ca2+]i) negatively regulates the apoptotic signalling activated by Death Receptor engagement (Fas and DR4/DR5) (submitted to EMBO J). A decrease in [Ca2+]i results in a potentiation of the apoptotic effects of FasL, Rituximab and Trail killer, whereas an increase inhibits them. View information
New compounds with anti-herpes activity (Technology Offer) This invention concerns new family of C3-arylated-3-deazauridine with potent anti-HSV activities and negligible cytotoxicity against various cell lines. In the pool of the already tested compounds, two molecules showed enhanced activities (close to the one of the reference acyclovir). View information
Minigenome to cure HCV (Technology Offer) This invention concerns a suicide vector in the form of chimeric genomic RNA (negative strand). The negative single-strand RNA molecule is non coding. So, the sole replication complex of the virus can manage to transform it into a positive strand. The latter can then be traduced into a pathogenic compound which can destroy the contaminating virus. The infected hepatocyte returns by the way to a healthy state. View information
Gastro-intestinal Dynamic Simulator (GDS) A research centre has developed an artif icial in vitro digestive system. This model simulates the ow n conditions of in vivo human gastrointestinal tract allowing a good understanding of the food digestion matrix and its nutrient release during gastrointestinal passage. The centre seeks partners for a technical cooperation to assess the functionalities from functional food and ingredients. View information
New process to obtain polysubstituted pyrrolidines as inhibitors of the hepatitis C virus A research team has developed a new process to obtain polysubstituted pyrrolidines as inhibitors of the hepatitis C virus. This process allows the preparation of enantioenriched polysubstituted proline derivatives after a three-step sequence. High purity, high yields and high enantiomeric ratios are achieved. The process is patented and pharmaceutical laboratories or companies are sought for license agreements or technical cooperations. View information
Software support system for helping dermatologists in the diagnosis of the melanoma --------------------------- A Research Group has developed a software support system for helping dermatologists in the diagnosis of the melanoma (a type of skin cancer). This diagnosis can use images obtained with dermatoscopic techniques and also photographs taken by the patients themselves. This system can be used as an automated way to decide the urgency to refer a patient to the dermatologist. This software is fully developed and available for demonstration. The group is open to other kind of collaboration. View information
Diagnostic procedure to identify patients with Minimal Hepatic Encephalopathy MHE View information
ICEO platform : an high-throughput screening facility for Enzyme discovery The high-throughput screening facility ICEO (Ingénierie et Criblage d'Enzymes Originales) is dedicated to the screening of original enzymes, isolated from large libraries generated using techniques such as directed evolution or coming from genomic or metagenomic samples . Objectives are numerous and go from discovering new catalysts, to redesigning enzyme specificity as well as modifying catalytic properties of a potentially interesting enzyme (stability, efficiency, affinity,…) so that it can fit conditions of use different from the natural ones. Techniques focus on generating large variant libraries (104 à 1010 clones) which will be subsequently screened to isolate interesting variants for the desired property. These hits can then be re-used as templates for additional rounds of mutations, recombinations and screening so as to finally obtain an optimal clone, resulting from the cumulative effects of multiple mutations, which individual contributions are most often very difficult to predict rationally. The success of this approach depends on reliable robotic techniques allowing treating a very high number of clones with high-throughput. Internet site: http://iceo.genotoul.fr/ View information
Biaryl and heteroaryl scaffolds for fragment based drug design A structurally complex and diverse collection of small molecules can be used to explore cellular and organismic pathways in a processes analogous to genetics. In planning diversity oriented syntheses of compounds, branching reactions pathways are important because they increase the structural diversity of products by altering the skeletal array of connecting atoms. In that respect chemists continue to develop efficient and sustainable methods for the construction of much different kind of organic architectures. Among such architectures of interest our group is currently paying much attention to bioactive types of natural products-like architectures that are biaryl and aryl-heteroatomaryl containing systems. The biary moiety is an ubiquitous motif to a variety of biologically active compounds (some structures: steganone, steganacin, gallotannins, ellagitannins) with significant activities against different tumor cells. On the other hand aryl-heteroatom aryl systems are a molecular scaffold present in many natural compounds possessing antitumoral activities. By capitalizing on our knowledge in aromatic (phenolic, cinnamic, polyphenolic) chemistry, we use small highly substituted phenolic scaffolds (ex; vanilline) in order to create the necessary connections and generate libraries that can be used in the synthesis of natural products and analogues biologically active. The two main biological activities searched are: i) antioxidant derivatives with cytoprotective effects; ii) antitumoral compounds. View information
Phosphorus-based dendrimers for human immuno-modulation Dendrimers are a class of highly branched “tree-like” polymers. Due to their sequential process of synthesis, they are characterized by perfectly defined structure and molecular weight. As their multivalency enables polyvalent interactions with cellular and/or molecular targets, they received tremendous attention along the two past decades regarding their uses in biology: drug delivery, biological imaging and tissue engineering. They are now part in their own right of the nanobiology and nanomedicine landscape. Among dendrimers, phosphorus-containing dendrimers capped with phosphonate end groups display unprecedented immunological properties towards cells of the human immune system. In particular, we have reported that an azabisphosphonate-capped dendrimer activates anti-inflammatory and immunosuppressive responses of the human immune system. These properties have been confirmed in vivo in a mouse model of Rheumatoid Arthritis. View information
Evaluation of potential anti-inflammatory drugs The team has developed new technologies, human and murine experimental models that mimic the human diseases to assess :  The molecular mechanisms and the signalling pathways involved in the activation of macrophages by drugs or diet conditions  The anti-inflammatory or anti-infectious potentials of drugs developed by the Biopharmaceutical, Cosmetic, and Food & Beverage industries Identification of new biomarkers of inflammatory, infectious diseases and tissue repair :  bioactive lipids (prostaglandines, lipoxines, resolvines)  Cytokines and chemokines Phenotypics and functional markers of macrophages In vitro and in vivo evaluation of anti- infectious, anti-inflammatory and wound healing effectiveness of drugs View information