AU2015275248B2 - Legumain activated doxorubicin derivative as well as preparation method and application thereof - Google Patents

Legumain activated doxorubicin derivative as well as preparation method and application thereof

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Publication number
AU2015275248B2
AU2015275248B2 AU2015275248A AU2015275248A AU2015275248B2 AU 2015275248 B2 AU2015275248 B2 AU 2015275248B2 AU 2015275248 A AU2015275248 A AU 2015275248A AU 2015275248 A AU2015275248 A AU 2015275248A AU 2015275248 B2 AU2015275248 B2 AU 2015275248B2
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Prior art keywords
compound
group
preparation
doxorubicin
well
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AU2015275248A
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AU2015275248A1 (en
Inventor
Cheng Liu
Yuan Liu
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Yafei (shanghai) Biopharmaceutical Co Ltd
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Yafei Shanghai Biopharmaceutical Co Ltd
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Priority to AU2018203194A priority Critical patent/AU2018203194B2/en
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  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention discloses doxorubicin derivatives for targeted activation by legumain, its preparation method and use. The doxorubicin derivatives are obtained by condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: 0 OH 'OH 0 0 OH 0 ',N-R3- sn-R4-R5-RG o OH compounds A and B have the following structures, respectively: OCH30 OH 0 ,NH 2 R3-Asn-R 4-R5-R6 "'OH Compound A Compound B wherein R3 in compound B is Leu or absent; R4 is any one amino acid selected from the group consisting of Ala and Thr; R5 is any one amino acid selected from the group consisting of Ala, N ~ R7'O0 Thr and Asn; R 6 is 0 , wherein n=1-20; or 0 , wherein R 7 is substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be use to prepare an anti-tumor drug.
AU2015275248A 2012-12-26 2015-12-22 Legumain activated doxorubicin derivative as well as preparation method and application thereof Active AU2015275248B2 (en)

Priority Applications (1)

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AU2018203194A AU2018203194B2 (en) 2012-12-26 2018-05-08 Legumain activated doxorubicin derivative as well as preparation method and application thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201210573744.3A CN103044521B (en) 2012-12-26 2012-12-26 Aspartase-targeted activated adriamycin derivative as well as preparation method and application thereof
CN201210573744.3 2012-12-26

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AU2015275248A1 AU2015275248A1 (en) 2016-02-25
AU2015275248B2 true AU2015275248B2 (en) 2018-02-22

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Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104231047B (en) * 2014-08-22 2017-06-16 亚飞（上海）生物医药科技有限公司 The paclitaxel derivatives and its preparation and use of water-soluble targeted activation
CA2958495C (en) * 2014-08-22 2023-04-18 Yafei Shanghai Biolog Medicine Science & Technology Co., Ltd. Small molecule conjugates specifically activated in tumor microenvironment for targeting and use thereof
CN104262457A (en) * 2014-08-22 2015-01-07 亚飞（上海）生物医药科技有限公司 Water-soluble cancer targeted activation docetaxel derivatives and uses thereof
CN106344930B (en) * 2015-07-16 2021-08-17 亚飞（上海）生物医药科技有限公司 Preparation and application of molecular site-specific targeting and activating short peptide adriamycin
SG10201913521TA (en) * 2016-09-23 2020-03-30 Univ Nanyang Tech Methods for enzymatic peptide ligation
JP7051906B2 (en) * 2019-06-18 2022-04-11 四川瀛瑞医薬科技有限公司 Pectin-doxorubicin conjugated compound and its preparation method and application
CN113274507A (en) * 2020-02-20 2021-08-20 亚飞（上海）生物医药科技有限公司 Preparation and use of immunostimulatory conjugate complexes for targeted delivery and activation

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1781932A (en) * 2004-12-03 2006-06-07 成都南山药业有限公司 Adriamycin derivative and its preparing method and use

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1781932A (en) * 2004-12-03 2006-06-07 成都南山药业有限公司 Adriamycin derivative and its preparing method and use

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Andre Warnecke et al., Arch. Pharm. Chem.Life Sci., (20071231), vol. 340, PAGE 389 - 395 *

Also Published As

Publication number Publication date
CN103044521B (en) 2014-11-05
AU2015275248A1 (en) 2016-02-25
CN103044521A (en) 2013-04-17
AU2018203194A1 (en) 2018-05-24
AU2018203194B2 (en) 2019-07-18

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Legal Events

Date Code Title Description
NA Applications received for extensions of time, section 223

Free format text: AN APPLICATION TO EXTEND THE TIME FROM 26 DEC 2013 TO 26 DEC 2015 IN WHICH TO CLAIM THE CONVENTION PRIORITY DATE HAS BEEN FILED .

NB Applications allowed - extensions of time section 223(2)

Free format text: THE TIME IN WHICH TO CLAIM THE CONVENTION PRIORITY DATE HAS BEEN EXTENDED TO 26 DEC 2015 .

FGA Letters patent sealed or granted (standard patent)