Title:
REGIOSELECTIVE CONJUGATE OF FUNCTIONAL SUBSTANCE AND ANTIBODY OR SALT OF SAID CONJUGATE, AND ANTIBODY DERIVATIVE AND COMPOUND FOR USE IN PRODUCTION OF SAID CONJUGATE, OR SALT OF SAID ANTIBODY DERIVATIVE AND COMPOUND
Document Type and Number:
WIPO Patent Application WO/2023/054714
Kind Code:
A1
Abstract:
The present invention provides: a conjugate of a functional substance and an antibody, in which the binding ratio between the antibody and the functional substance is controlled to within a specific range, said conjugate being exceptional with respect to a desired property; or a salt of said conjugate. More specifically, the present invention provides: a regioselective conjugate of a functional substance and antibody or a salt of said conjugate, the conjugate including a structural unit represented by formula (I) (wherein Ig represents an immunoglobulin unit comprising two heavy chains and two light chains, and is regioselectively bound to L1 adjacent to the Ig via an amino group in the side chain of a lysine residue in the two heavy chains; HG represents a hydrophilic group, etc.; RA represents a side chain of a valine residue; RB represents a side chain of a citrulline residue, etc.; ring A represents a divalent aromatic ring group optionally having a substituent; R1 and R2 independently represent a hydrogen atom or a monovalent group; L1 and L2 independently represent a divalent group; D represents a functional substance; and r is 1.5 to 2.5); and a substance relating to the conjugate and the salt.
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Inventors:
MATSUDA YUTAKA (JP)
WATANABE TOMOHIRO (JP)
HATADA NORIKO (JP)
FUJII TOMOHIRO (JP)
WATANABE TOMOHIRO (JP)
HATADA NORIKO (JP)
FUJII TOMOHIRO (JP)
Application Number:
PCT/JP2022/036852
Publication Date:
April 06, 2023
Filing Date:
September 30, 2022
Export Citation:
Assignee:
AJINOMOTO KK (JP)
International Classes:
C07K16/00; A61K39/395; A61K47/68; A61K49/00; A61P35/00; C07K5/08; C07K7/06; C07K19/00
Domestic Patent References:
| WO2015038426A1 | 2015-03-19 | |||
| WO2014100762A1 | 2014-06-26 | |||
| WO2019231879A1 | 2019-12-05 | |||
| WO2022058548A1 | 2022-03-24 | |||
| WO2018199337A1 | 2018-11-01 | |||
| WO2019240288A1 | 2019-12-19 | |||
| WO2019240287A1 | 2019-12-19 | |||
| WO2020090979A1 | 2020-05-07 | |||
| WO2015038426A1 | 2015-03-19 | |||
| WO2004010957A2 | 2004-02-05 | |||
| WO2019240287A1 | 2019-12-19 |
Foreign References:
| US20060074008A1 | 2006-04-06 | |||
| US20050238649A1 | 2005-10-27 |
Other References:
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CHEMISTRY SELECT, vol. 5, 2020, pages 8435 - 8439
NATURE COMMUNICATIONS, vol. 9, 2018, pages 2512
DORYWALSKA ET AL., MOL CANCER THER., vol. 15, no. 5, 2016, pages 958 - 70
LYON ET AL., NAT BIOTECHNOL., vol. 33, no. 7, 2015, pages 733 - 5
SHARPLESS K.B., ANGEW. CHEM. INT. ED., vol. 40, 2015, pages 2004
BERTOZZI C. R. ET AL., SCIENCE, vol. 291, 2001, pages 2357
BERTOZZI C. R., NATURE CHEMICAL BIOLOGY, vol. 1, 2005, pages 13
G. LERICHEL. CHISHOLMA. WAGNER, BIOORGANIC MEDICINAL CHEMISTRY, vol. 20, 2012, pages 571
FENG P. ET AL., JOUNAL OF AMERICAN CHEMICAL SOCIETY, vol. 132, 2010, pages 1500
SCHOENMARKS, R. G., JOURNAL OF CONTROLLED RELEASE, vol. 95, 2004, pages 291
DESIMONE, J. M., JOURNAL OF AMERICAN CHEMICAL SOCIETY, vol. 132, 2010, pages 17928
THOMPSON, D. H., JOURNAL OF CONTROLLED RELEASE, vol. 91, 2003, pages 187
EXAMPLES AND CHEMISTRY SELECT, vol. 5, 2020, pages 8435 - 8439
G. J. L. BERNARDES ET AL., CHEM. REV., vol. 115, 2015, pages 2174 - 2195
G. J. L. BERNARDES ET AL., CHEM. ASIAN. J., vol. 4, 2009, pages 630
B. G. DAVIES ET AL., NAT. COMMUN., vol. 5, 2014, pages 4740
A. WAGNER ET AL., BIOCONJUGATE. CHEM., vol. 25, 2014, pages 825
ANAL. CHEM., vol. 91, no. 20, 2019, pages 12724 - 12732
CHEMISTRY SELECT, vol. 5, 2020, pages 8435 - 8439
NATURE COMMUNICATIONS, vol. 9, 2018, pages 2512
Attorney, Agent or Firm:
SAKAI INTERNATIONAL PATENT OFFICE (JP)
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