139729-28-5Relevant articles and documents
TARGETED BIFUNCTIONAL DEGRADERS
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, (2021/04/17)
The present invention provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In another aspect, the present invention provides bifunctional compounds that can be used to promote or enhance degradation of certain autoantibodies. In certain embodiments, treatment or management of a disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein or the autoantibody in the subject. Thus, in certain embodiments, administration of a compound of the invention to the subject removes or reduces the circulation concentration of the circulating protein or the autoantibody, thus treating, ameliorating, or preventing the disease and/or disorder. In certain embodiments, the circulating protein is TNF.
Optimization of IEDDA bioorthogonal system: Efficient process to improve trans-cyclooctene/tetrazine interaction
Béquignat, Jean-Baptiste,Boucheix, Claude,Canitrot, Damien,Chezal, Jean-Michel,Degoul, Fran?oise,Miot-Noirault, Elisabeth,Moreau, Emmanuel,Navarro-Teulon, Isabelle,Quintana, Mercedes,Rondon, Aurélie,Taiariol, Ludivine,Ty, Nancy
, (2020/07/21)
The antibody pretargeting approach for radioimmunotherapy (RIT) using inverse electron demand Diels-Alder cycloaddition (IEDDA) constitutes an emerging theranostic approach for solid cancers. However, IEDDA pretargeting has not reached clinical trial. The major limitation of the IEDDA strategy depends largely on trans-cyclooctene (TCO) stability. Indeed, TCO may isomerize into the more stable but unreactive cis-cyclooctene (CCO), leading to a drastic decrease of IEDDA efficiency. We have thus developed both efficient and reproducible synthetic pathways and analytical follow up for (PEGylated) TCO derivatives, providing high TCO isomeric purity for antibody modification. We have set up an original process to limit the isomerization of TCO to CCO before the mAbs’ functionalization to allow high TCO/tetrazine cycloaddition.
Preparation method of [2-[1-(Fmoc-amino)ethoxy]ethoxy]acetic acid
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Paragraph 0065; 0068; 0070, (2019/09/17)
The invention provides a preparation method of [2-[1-(Fmoc-amino)ethoxy]ethoxy]acetic acid. The preparation method comprises steps as follows: amino protection is performed on diglycolamine by use ofphthalic anhydride, an obtained intermediate and halo-acetic acid or halo-acetate are subjected to a reaction, deprotection or deprotection and hydrolysis are performed, a product reacts with a Fmoc-based amino protection reagent, and [2-[1-(Fmoc-amino)ethoxy]ethoxy]acetic acid is obtained. In the preparation method, phthalic anhydride and diglycolamine are taken as initial raw materials, short time is required by an amino protection reaction, an obtained intermediate compound has good stability, can be preserved for a long time and does not react with water, water-soluble impurities (such asthe raw material diglycolamine, a byproduct phthalic acid and the like) can be separated through extraction, so that an amino protection product with high purity is obtained, and the purity and the yield of the target product are also improved.
