公开(公告)号：US20240165260A1

公开(公告)日：2024-05-23

申请号：US18523499

申请日：2023-11-29

Applicant: Ajinomoto Co., Inc.

Inventor： Yutaka MATSUDA ,  Tomohiro FUJII ,  Ryusuke HIRAMA ,  Thomas MARKOTAN ,  Allan PRIOR ,  Christopher WONG ,  Konstantinos PLAKAS ,  Tomohiro WATANABE

IPC: A61K47/68 ,  C07K5/062

CPC classification number: A61K47/6889 ,  A61K47/68031 ,  A61K47/6855 ,  C07K5/06052

Abstract: A conjugate of an antibody and a functional substance or a salt thereof, which comprises a structural unit represented by the following formula (I):






wherein Ig represents an immunoglobulin unit comprising two heavy chains and two light chains, and regioselectively forms an amide bond with a carbonyl group adjacent to Ig via an amino group in side chains of lysine residues in the two heavy chains,
L1 and L2 each represent a divalent group,
R1 represents a monovalent group optionally comprising a hydrophilic group,
X represents a predetermined divalent group,
D represents a functional substance,
RA represents a side chain of a valine residue,
RB represents a side chain of a citrulline residue or an alanine residue,
n is 0 or 1, and
an average ratio r of the amide bonds per two heavy chains is 1.5 to 2.5, and
wherein at least one hydrophilic group is present in the structural unit are excellent in desired properties while controlling a binding ratio between the antibody and the functional substance within a desired range.

公开(公告)号：US20240285788A1

公开(公告)日：2024-08-29

申请号：US18619910

申请日：2024-03-28

Applicant: Ajinomoto Co., Inc.

Inventor： Yutaka MATSUDA ,  Tomohiro WATANABE ,  Noriko HATADA ,  Tomohiro FUJII

IPC: A61K47/68

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.

公开(公告)号：US20240269311A1

公开(公告)日：2024-08-15

申请号：US18619756

申请日：2024-03-28

Applicant: Ajinomoto Co., Inc.

Inventor： Yutaka MATSUDA ,  Tomohiro WATANABE ,  Noriko HATADA ,  Tomohiro FUJII

IPC: A61K47/68 ,  C07K5/08 ,  C07K16/46

CPC classification number: A61K47/6811 ,  C07K5/08 ,  C07K16/46

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






wherein
Ig represents an immunoglobulin unit comprising two heavy chains and two light chains, and is regioselectively bonded to L1 adjacent to Ig via an amino group in side chains of lysine residues in the two heavy chains,
HG represents a hydrophilic group,
RA represents a side chain of a valine residue,
RB represents a side chain of a citrulline residue or the like,
ring A represents a divalent aromatic ring group optionally having a substituent,
R1 and R2 each independently represent a hydrogen atom or a monovalent group,
L1 and L2 each independently represent a divalent
D represents a functional substance, and
r is 1.5 to 2.5, or
a salt thereof, and
substances related thereto,

is excellent in desired properties while controlling a bonding ratio between the antibody and the functional substance within a specific range.