COMPOUND HAVING AFFINITY SUBSTANCE TO ANTIBODY, CLEAVABLE PORTION, AND REACTIVE GROUP, OR SALT THEREOF

    公开(公告)号:US20210139549A1

    公开(公告)日:2021-05-13

    申请号:US17119786

    申请日:2020-12-11

    Abstract: Compounds having an affinity substance to an antibody, a cleavable portion, and a reactive group, represented by the following Formula (I): A-L-B-R  (I) wherein A is the affinity substance an antibody, L is a cleavable linker which is a divalent group comprising the cleavable portion, B is (a) a divalent group comprising a bioorthogonal functional group or (b) a divalent group comprising no bioorthogonal functional group, and R is the reactive group to the antibody, in which the affinity substance to an antibody is a certain peptide, or a salt thereof are useful for the modification of an antibody, particularly the regioselective modification of an antibody.

    CONJUGATE OF ANTIBODY AND FUNCTIONAL SUBSTANCE OR SALT THEREOF, AND ANTIBODY DERIVATIVE AND COMPOUND USED IN PRODUCTION OF THE SAME OR SALTS THEREOF

    公开(公告)号:US20240285788A1

    公开(公告)日:2024-08-29

    申请号:US18619910

    申请日:2024-03-28

    CPC classification number: A61K47/6811

    Abstract: A conjugate of an antibody and a functional substance, comprising a structural unit represented by the following Formula (1):






    wherein
    Ig represents an immunoglobulin unit comprising two heavy chains and two light chains, and is bonded to LA adjacent to Ig via a thiol group in side chains of a plurality of cysteine residues in the two heavy chains and the two light chains,
    HG represents a hydrophilic group or a monovalent group comprising a hydrophilic group,
    CS represents a divalent group comprising a cleavable site,
    ring A represents a divalent aromatic ring group optionally having a substituent wherein the divalent aromatic ring group constitutes a π electron conjugated system with the cleavable site,
    V represents an oxygen atom, a sulfur atom, or an amino group (NH),
    LA and LB each independently represent a divalent group,
    D represents a functional substance, and
    an average number n of the bonds per the immunoglobulin unit is 1.5 or more, or
    a salt thereof, and
    a substance associated therewith,

    is excellent in desired properties.

    COMPOUND OR SALT THEREOF, AND ANTIBODY OBTAINED BY USING THE SAME

    公开(公告)号:US20240115719A1

    公开(公告)日:2024-04-11

    申请号:US18463903

    申请日:2023-09-08

    CPC classification number: A61K47/68031 C07K16/2803

    Abstract: Compounds or salts thereof represented by formula (I):






    wherein
    X indicates a leaving group,
    Y indicates an affinity peptide having a binding region in a CH2 domain in an immunoglobulin unit comprising two heavy chains and two light chains,
    M indicates a trivalent group linking the carbon atom in C═O adjacent to M and the carbon atom in C═W via a main chain portion consisting of 3 to 5 carbon atoms,
    O indicates an oxygen atom,
    S indicates a sulfur atom,
    W indicates an oxygen atom or a sulfur atom,
    N3 indicates an azide group,
    La indicates a bond or a divalent group, and
    Lb indicates a bond or a divalent group; and antibodies or salts thereof which can be prepared using such a compound or salt thereof, are useful for controlling the bonding ratio of an antibody and a modifying group within a desired range.

    COMPOUND OR SALT THEREOF, AND ANTIBODY OBTAINED BY USING THE SAME

    公开(公告)号:US20240000965A1

    公开(公告)日:2024-01-04

    申请号:US18354436

    申请日:2023-07-18

    CPC classification number: A61K47/6889 A61K47/6811

    Abstract: Compounds and salts thereof represented by the following formula (I):






    wherein
    X indicates a leaving group,
    Y indicates an affinity peptide having a binding region to a CH2 domain in an immunoglobulin unit containing two heavy chains and two light chains,
    O indicates an oxygen atom,
    S indicates a sulfur atom,
    W indicates an oxygen atom or a sulfur atom,
    La indicates a first linker,
    Lb indicates a second linker, and
    the total number of atoms constituting a main chain in the first linker and atoms constituting a main chain in the second linker are 5 to 7, facilitate regioselective modification of an antibody with a functional substance and control of the bonding ratio of the antibody to the functional substance within a desired range.

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