Title:
CONJUGATE AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/161452
Kind Code:
A1
Abstract:
A compound of formula (I), or a tautomer, a stereoisomer or a pharmaceutically acceptable salt thereof. The compound represented by formula (I) or the tautomer, the stereoisomer or the pharmaceutically acceptable salt thereof, as a novel linker compound, can be used for preparing an ADC medicament with a high DAR value. The present invention also relates to an ADC medicament prepared from the linker.
Inventors:
CHEN JIAN (CN)
ZHAO HAIBO (CN)
GU RONG (CN)
ZHAO HAIBO (CN)
GU RONG (CN)
Application Number:
PCT/CN2022/074523
Publication Date:
August 04, 2022
Filing Date:
January 28, 2022
Export Citation:
Assignee:
NANJING CHEMPION BIOTECHNOLOGY CO LTD (CN)
International Classes:
A61K47/68; A61K47/60; A61K47/66; A61P35/00
Domestic Patent References:
| WO2015105083A1 | 2015-07-16 | |||
| WO1990005144A1 | 1990-05-17 |
Foreign References:
| CN110234357A | 2019-09-13 | |||
| EP2913064A1 | 2015-09-02 | |||
| CN101541332A | 2009-09-23 | |||
| CN106061981A | 2016-10-26 | |||
| CN107109405A | 2017-08-29 | |||
| CN102006890A | 2011-04-06 | |||
| CN110520161A | 2019-11-29 | |||
| CN103491982A | 2014-01-01 | |||
| US20130317080A1 | 2013-11-28 | |||
| US5821337A | 1998-10-13 |
Other References:
CHI-HUI LIANG, SHENG-KAI WANG, CHIN-WEI LIN, CHENG-CHI WANG, CHI-HUEY WONG, AND CHUNG-YI WU: "Effects of Neighboring Glycans on Antibody-Carbohydrate Interaction,", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, 11 February 2011 (2011-02-11), pages 1608 - 1612, XP055633434, DOI: 10.1002/anie.201003482
REMON VAN GEEL, WIJDEVEN MARLOES A., HEESBEEN RYAN, VERKADE JORGE M. M., WASIEL ANNA A., VAN BERKEL SANDER S., VAN DELFT FLORIS L.: "Chemoenzymatic Conjugation of Toxic Payloads to the Globally Conserved N-Glycan of Native mAbs Provides Homogeneous and Highly Efficacious Antibody–Drug Conjugates", BIOCONJUGATE CHEMISTRY, vol. 26, no. 11, 18 November 2015 (2015-11-18), US , pages 2233 - 2242, XP055249394, ISSN: 1043-1802, DOI: 10.1021/acs.bioconjchem.5b00224
"McGraw-Hill Dictionary of Chemical Terms", 1984, MCGRAW-HILL BOOK COMPANY
POLJAK ET AL., STRUCTURE, vol. 2, 1994, pages 1121 - 3
JACQUES ET AL.: "Enantiomers, Racemates and Resolutions", 1981, WILEY INTERSCIENCE
"Principles of Asymmetric Synthesis", 2012, ELSEVIER
ELIEL, E.L.: "Stereochemistry of Carbon Compounds", 1962, MCGRAW-HILL
WILEN, S.H.: "Tables of Resolving Agents and Optical Resolutions", 1972, UNIV. OF NOTRE DAME PRESS, pages: 268
MICHAEL B. SMITHJERRY MARCH: "Chiral Separation Techniques: A Practical Approach", 2007, WILEY-VCH VERLAG GMBH & CO. KGAA
T W. GREENE: "Protective Groups in Organic Synthesis", 1991, JOHN WILEY&SONS
P. J. KOCIENSKI: "Protecting Groups", 2005, THIEME
S. M. BERGE ET AL., J. PHARMACEUTICAL SCIENCES, vol. 66, 1977, pages 1 - 19
WARD ET AL., NATURE, vol. 341, 1989, pages 544 - 6
BIRD ET AL., SCIENCE, vol. 242, 1988, pages 423 - 6
HUSTON ET AL., PROC. NATL. ACAD. SCI. USA, vol. 85, 1988, pages 5879 - 83
HE ET AL., J. NUCL. MED., vol. 51, 2010, pages 427 - 32
FITTING ET AL., MABS, vol. 7, 2015, pages 390 - 402
HOLLIGER ET AL., PROC. NATL. ACAD. SCI. USA, vol. 90, 1993, pages 6444 - 8
"Handbook of Chemistry and Physics", 1994
THOMAS SORRELL: "Organic Chemistry", 1999, UNIVERSITY SCIENCE BOOKS
REMON VAN GEEL, WIJDEVEN MARLOES A., HEESBEEN RYAN, VERKADE JORGE M. M., WASIEL ANNA A., VAN BERKEL SANDER S., VAN DELFT FLORIS L.: "Chemoenzymatic Conjugation of Toxic Payloads to the Globally Conserved N-Glycan of Native mAbs Provides Homogeneous and Highly Efficacious Antibody–Drug Conjugates", BIOCONJUGATE CHEMISTRY, vol. 26, no. 11, 18 November 2015 (2015-11-18), US , pages 2233 - 2242, XP055249394, ISSN: 1043-1802, DOI: 10.1021/acs.bioconjchem.5b00224
"McGraw-Hill Dictionary of Chemical Terms", 1984, MCGRAW-HILL BOOK COMPANY
POLJAK ET AL., STRUCTURE, vol. 2, 1994, pages 1121 - 3
JACQUES ET AL.: "Enantiomers, Racemates and Resolutions", 1981, WILEY INTERSCIENCE
"Principles of Asymmetric Synthesis", 2012, ELSEVIER
ELIEL, E.L.: "Stereochemistry of Carbon Compounds", 1962, MCGRAW-HILL
WILEN, S.H.: "Tables of Resolving Agents and Optical Resolutions", 1972, UNIV. OF NOTRE DAME PRESS, pages: 268
MICHAEL B. SMITHJERRY MARCH: "Chiral Separation Techniques: A Practical Approach", 2007, WILEY-VCH VERLAG GMBH & CO. KGAA
T W. GREENE: "Protective Groups in Organic Synthesis", 1991, JOHN WILEY&SONS
P. J. KOCIENSKI: "Protecting Groups", 2005, THIEME
S. M. BERGE ET AL., J. PHARMACEUTICAL SCIENCES, vol. 66, 1977, pages 1 - 19
WARD ET AL., NATURE, vol. 341, 1989, pages 544 - 6
BIRD ET AL., SCIENCE, vol. 242, 1988, pages 423 - 6
HUSTON ET AL., PROC. NATL. ACAD. SCI. USA, vol. 85, 1988, pages 5879 - 83
HE ET AL., J. NUCL. MED., vol. 51, 2010, pages 427 - 32
FITTING ET AL., MABS, vol. 7, 2015, pages 390 - 402
HOLLIGER ET AL., PROC. NATL. ACAD. SCI. USA, vol. 90, 1993, pages 6444 - 8
"Handbook of Chemistry and Physics", 1994
THOMAS SORRELL: "Organic Chemistry", 1999, UNIVERSITY SCIENCE BOOKS
Attorney, Agent or Firm:
LIU, SHEN & ASSOCIATES (CN)
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