Reference number : GC-2017-Q4-01964, amendment number : , agreement type : G, recipient legal name : Yudin, Andrei (University of Toronto), recipient country : CA, recipient province : nan, recipient city : Ontario, recipient postal code : nan, program name english : Idea to Innovation, program name french : De l'idée à l'innovation, program purpose english : In 2016, we discovered a macrocyclization reaction that rapidly converts readily accessible linear peptides into macrocycles with well-defined conformation. (N-isocyanimino)triphenylphosphorane, instrumental to this reaction, was later named "Pinc" to identify the presence of phosphonium and isocyanide functionalities. This work was published in Nature Chemistry and was subsequently covered by The Chemical & Engineering News and Science. On the heels of this discovery, we applied for a patent application (PCT/CA2016/000234) that described the method of cyclizing peptides with simultaneous incorporation of an oxadiazole graft into the resulting macrocyclic structures. We also received market assessment funding from NSERC allowing us to retain the services of Adventus Research who carried out a thorough market assessment study (see the 85-page report attached)._x000D_
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The present I2I application considers the main messages from that report and focuses on two applications that will further de-risk our technology now that it is sufficiently mature. The first one is to develop an approach to the synthesis of improved derivatives of Pinc. The second one deals with peptide macrocycles produced using Pinc in order to further validate our approach to novel composition of matter. To move forward, we will engage in collaborative activity to produce Pinc (together with MilliporeSigma), initiate translational studies aimed at the use of Pinc toward heterocycle synthesis (together with Apotex), and evaluate the potential of Pinc-derived macrocycles in drug discovery (together with Encycle and Merck)._x000D_, program purpose french : In 2016, we discovered a macrocyclization reaction that rapidly converts readily accessible linear peptides into macrocycles with well-defined conformation. (N-isocyanimino)triphenylphosphorane, instrumental to this reaction, was later named "Pinc" to identify the presence of phosphonium and isocyanide functionalities. This work was published in Nature Chemistry and was subsequently covered by The Chemical & Engineering News and Science. On the heels of this discovery, we applied for a patent application (PCT/CA2016/000234) that described the method of cyclizing peptides with simultaneous incorporation of an oxadiazole graft into the resulting macrocyclic structures. We also received market assessment funding from NSERC allowing us to retain the services of Adventus Research who carried out a thorough market assessment study (see the 85-page report attached)._x000D_
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The present I2I application considers the main messages from that report and focuses on two applications that will further de-risk our technology now that it is sufficiently mature. The first one is to develop an approach to the synthesis of improved derivatives of Pinc. The second one deals with peptide macrocycles produced using Pinc in order to further validate our approach to novel composition of matter. To move forward, we will engage in collaborative activity to produce Pinc (together with MilliporeSigma), initiate translational studies aimed at the use of Pinc toward heterocycle synthesis (together with Apotex), and evaluate the potential of Pinc-derived macrocycles in drug discovery (together with Encycle and Merck)._x000D_, agreement title english : Oxadiazole grafts in peptide macrocycles, agreement title french : Oxadiazole grafts in peptide macrocycles, agreement number : I2IPJ, agreement value : 121000.0, agreement start date : 2018-02-07, agreement end date : nan, description english : nan, description french : nan, expected results english : nan, expected results french : nan, additional information english : Grant or Award spanning more than one fiscal year (2017-2018 to 2018-2019)., additional information french : Subvention ou bourse octroyée s'appliquant à plus d'un exercice financier (2017-2018 à 2018-2019)., owner organization : nserc-crsng, owner organization title : Natural Sciences and Engineering Research Council of Canada | Conseil de recherches en sciences naturelles et en génie du Canada