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    MILD AND SITE-SELECTIVE 18F-LABELING OF SMALL MOLECULES AND/OR BIOMOLECULES VIA A THIOL-REACTIVE SYNTHON
    72.
    发明申请
    MILD AND SITE-SELECTIVE 18F-LABELING OF SMALL MOLECULES AND/OR BIOMOLECULES VIA A THIOL-REACTIVE SYNTHON 有权

    公开(公告)号：US20220072163A1

    公开(公告)日：2022-03-10

    申请号：US17253430

    申请日：2019-06-28

    申请人： The Regents of the University of California

    发明人： Jennifer M. Murphy ,  Gaoyuan Ma

    IPC分类号： A61K51/04 ,  C07B59/00 ,  A61K51/08 ,  C07D233/70

    摘要： Site-selective conjugation to biomolecules via thiol-based chemistry is superior to the unselective modification of lysine residues, which produce a mixed product and can potentially interfere with binding affinity of the biomolecule. However, in physiological environments, the maleimide-thiol conjugation product which is the current gold-standard for site-selective thiol-conjugation can be susceptible to hydrolysis or a retro-Michael reaction via exchange with reactive thiols such as those in albumin or glutathione residues yet the degradation is relatively slow. Therefore, for in vivo studies, the maleimide-thiol conjugation proposes instability issues. The compositions and methods disclosed herein provide an alternative thiol-based linkage, one that overcomes the instability issues with conventional reagents and methods. The compositions and methods disclosed herein are useful in various contexts, for example, for 18F-labeling of peptides/proteins in the preparation of positron emission tomography (PET) probes.

    Device for the synthesis of a radiotracer, facility comprising such a device, and method for producing a radiotracer by means of such a device
    76.
    发明授权
    Device for the synthesis of a radiotracer, facility comprising such a device, and method for producing a radiotracer by means of such a device 有权

    公开(公告)号：US11219875B2

    公开(公告)日：2022-01-11

    申请号：US15565740

    申请日：2016-04-14

    申请人： PMB

    发明人： Laurent Tanguy ,  Jerome Corneille ,  Bertrand Loubaton ,  Marc Delmas ,  Alain Perez Delaume

    IPC分类号： B01J19/00 ,  C07B59/00 ,  G21G4/08

    摘要： Disclosed is a device for the synthesis of a radiotracer, including a universal confined enclosure designed for the insertion of a specific synthesis cassette of the radiotracer and the removal of same. The synthesis cassette includes a synthesis module designed to receive reagents and a radioisotope for the synthesis of the radiotracer. An inner connector plate includes at least one inlet, designed to be connected to a radioisotope admission and also to the inlet of the cassette, and an outlet, designed to be connected to a syringe to be filled with the radiotracer and also to the outlet of the cassette. Such a synthesis device can be installed in a facility including, in a confined room, as well as such devices normally arranged in a storage area, a synthesis station, a radioisotope admission, at least one window for communication to the outside, and a manipulator robot.