Title:
BIOACTIVE CONJUGATE, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/114666
Kind Code:
A1
Abstract:
The present invention relates to a bioactive conjugate, a preparation method therefor, and use thereof. In particular, the present invention relates to a novel type of bioactive molecular conjugates obtained by improving the coupling of a drug to a targeted moiety in ADC or SMDC, a preparation method therefor, and use thereof in the preparation of drugs for treating diseases associated with abnormal cellular activity.
Inventors:
CAI JIAQIANG (CN)
SONG SHUAI (CN)
XUE TONGTONG (CN)
XIAO LIANG (CN)
DENG HANWEN (CN)
TIAN QIANG (CN)
WANG JING (CN)
LIU DENGNIAN (CN)
LIU LIPING (CN)
YU HAIMIN (CN)
YANG ZHOUNING (CN)
CAO XU (CN)
ZHONG GUOQING (CN)
WANG LICHUN (CN)
WANG JINGYI (CN)
SONG SHUAI (CN)
XUE TONGTONG (CN)
XIAO LIANG (CN)
DENG HANWEN (CN)
TIAN QIANG (CN)
WANG JING (CN)
LIU DENGNIAN (CN)
LIU LIPING (CN)
YU HAIMIN (CN)
YANG ZHOUNING (CN)
CAO XU (CN)
ZHONG GUOQING (CN)
WANG LICHUN (CN)
WANG JINGYI (CN)
Application Number:
PCT/CN2018/120125
Publication Date:
June 20, 2019
Filing Date:
December 10, 2018
Export Citation:
Assignee:
SICHUAN KELUN BIOTECH BIOPHARMACEUTICAL CO LTD (CN)
International Classes:
C07K7/02; A61K31/506; A61K45/00; A61P35/00; C07D491/22; C07K5/062
Domestic Patent References:
| WO2014144878A2 | 2014-09-18 | |||
| WO2016142049A1 | 2016-09-15 | |||
| WO2015012904A2 | 2015-01-29 | |||
| WO2018025168A1 | 2018-02-08 |
Foreign References:
| US4816567A | 1989-03-28 | |||
| CN103319599A | 2013-09-25 | |||
| US7560111B2 | 2009-07-14 | |||
| US7517964B2 | 2009-04-14 | |||
| US20120237518A1 | 2012-09-20 | |||
| CN103476941A | 2013-12-25 |
Other References:
TODA, N. ET AL.: "Rapid, Stable, Chemoselective Labeling of Thiols with Julia-Kocienski-Like Reagents: A Serum-Stable Alternative to Maleimide-Based Protein Conjugation", ANGEWANDTE CHEMI INTERNATIONAL EDITION, vol. 52, no. 48, 2 October 2013 (2013-10-02), pages 12592 - 12596, XP055416940, DOI: doi:10.1002/anie.201306241
LI, XIULING ET AL.: "Site-Specific Dual Antibody Conjugation via Engineered Cysteine and Selenocysteine Residues", BIOCONJUGATE CHEMISTRY, vol. 26, no. 11, 18 November 2015 (2015-11-18), pages 2243 - 2248, XP055416982, DOI: doi:10.1021/acs.bioconjchem.5b00244
PATTERSON, J.T. ET AL.: "Improving the Serum Stability of Site-Specific Antibody Conjugates with Sulfone Linkers", BIOCONJUGATE CHEMISTRY, vol. 25, no. 8, 20 August 2014 (2014-08-20), pages 1402 - 1407, XP055338868, DOI: doi:10.1021/bc500276m
LIANG, XIAOFEI ET AL.: "Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3- (trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL- ABL-053) as a Potent, Selective, and Orally Available BCR-ABUSRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, 31 December 2016 (2016-12-31), pages 1984 - 2004, XP055603365, DOI: doi:10.1021/acs.jmedchem.5b01618
CHOTHIALESK, J. MOL. BIOL., vol. 196, 1987, pages 901 - 917
CHOTHIA ET AL., NATURE, vol. 342, 1989, pages 878 - 883
DICK, L.W. ET AL., BIOTECHNOL. BIOENG., vol. 100, pages 1132 - 1143
MORRISON ET AL., PNAS, vol. 81, 1984, pages 6851 - 6855
YAMAMOTO ET AL., NATURE, vol. 319, 1986, pages 230 - 234
RIECHMANN ET AL., NATURE, vol. 332, 1988, pages 323 - 329
PRESTA, CURR OP STRUCT BWL, vol. 2, 1992, pages 593 - 596
KOHLER ET AL., NATURE, vol. 256, 1975, pages 495
CLACKSON ET AL., NATURE, vol. 352, 1991, pages 624 - 628
MARKS ET AL., JOURNAL OF MOLECULAR BIOLOGY, vol. 222, 1991, pages 581 - 597
"Genebank", Database accession no. X03363
SEMBA ET AL., PNAS, vol. 82, 1985, pages 6497 - 6501
See also references of EP 3725798A4
LI, XIULING ET AL.: "Site-Specific Dual Antibody Conjugation via Engineered Cysteine and Selenocysteine Residues", BIOCONJUGATE CHEMISTRY, vol. 26, no. 11, 18 November 2015 (2015-11-18), pages 2243 - 2248, XP055416982, DOI: doi:10.1021/acs.bioconjchem.5b00244
PATTERSON, J.T. ET AL.: "Improving the Serum Stability of Site-Specific Antibody Conjugates with Sulfone Linkers", BIOCONJUGATE CHEMISTRY, vol. 25, no. 8, 20 August 2014 (2014-08-20), pages 1402 - 1407, XP055338868, DOI: doi:10.1021/bc500276m
LIANG, XIAOFEI ET AL.: "Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3- (trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL- ABL-053) as a Potent, Selective, and Orally Available BCR-ABUSRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, 31 December 2016 (2016-12-31), pages 1984 - 2004, XP055603365, DOI: doi:10.1021/acs.jmedchem.5b01618
CHOTHIALESK, J. MOL. BIOL., vol. 196, 1987, pages 901 - 917
CHOTHIA ET AL., NATURE, vol. 342, 1989, pages 878 - 883
DICK, L.W. ET AL., BIOTECHNOL. BIOENG., vol. 100, pages 1132 - 1143
MORRISON ET AL., PNAS, vol. 81, 1984, pages 6851 - 6855
YAMAMOTO ET AL., NATURE, vol. 319, 1986, pages 230 - 234
RIECHMANN ET AL., NATURE, vol. 332, 1988, pages 323 - 329
PRESTA, CURR OP STRUCT BWL, vol. 2, 1992, pages 593 - 596
KOHLER ET AL., NATURE, vol. 256, 1975, pages 495
CLACKSON ET AL., NATURE, vol. 352, 1991, pages 624 - 628
MARKS ET AL., JOURNAL OF MOLECULAR BIOLOGY, vol. 222, 1991, pages 581 - 597
"Genebank", Database accession no. X03363
SEMBA ET AL., PNAS, vol. 82, 1985, pages 6497 - 6501
See also references of EP 3725798A4
Attorney, Agent or Firm:
CCPIT PATENT AND TRADEMARK LAW OFFICE (CN)
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