WO2018124758A3 - 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물 - Google Patents

베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물 Download PDF

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Publication number
WO2018124758A3
WO2018124758A3 PCT/KR2017/015613 KR2017015613W WO2018124758A3 WO 2018124758 A3 WO2018124758 A3 WO 2018124758A3 KR 2017015613 W KR2017015613 W KR 2017015613W WO 2018124758 A3 WO2018124758 A3 WO 2018124758A3
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WO
WIPO (PCT)
Prior art keywords
galactoside
immolative linker
compound bearing
self
introduced self
Prior art date
Application number
PCT/KR2017/015613
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English (en)
French (fr)
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WO2018124758A2 (ko
Inventor
박태교
우성호
김선영
정두환
이상광
조종운
이재호
박수호
서동훈
이향숙
서범석
임지연
Original Assignee
주식회사 인투셀
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Priority claimed from KR1020170181411A external-priority patent/KR102085798B1/ko
Application filed by 주식회사 인투셀 filed Critical 주식회사 인투셀
Priority to CN201780081520.1A priority Critical patent/CN110167599B/zh
Priority to JP2019556777A priority patent/JP7256751B2/ja
Priority to US16/472,983 priority patent/US11065343B2/en
Publication of WO2018124758A2 publication Critical patent/WO2018124758A2/ko
Publication of WO2018124758A3 publication Critical patent/WO2018124758A3/ko

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 β-갈락토사이드(β-galactoside)가 도입된 자가-희생 기(self-immolative linker)를 포함하는 화합물에 관한 것으로, 보다 상세하게는 본 발명의 β-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물은 목적하는 표적에 대한 결합 특이성을 갖는 단백질(예: 올리고펩티드, 폴리펩티드, 항체 등) 또는 리간드, 특이적 기능 또는 활성을 갖는 활성제(예: 약물, 독소, 리간드, 검출용 탐침 등) 및 타겟 세포내에서 선택적으로 활성제가 방출될 수 있도록 글라이코사이드 결합(glycosidic bond)을 이루고 있는 자가-희생 기를 포함할 수 있다.
PCT/KR2017/015613 2016-12-28 2017-12-28 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물 WO2018124758A2 (ko)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN201780081520.1A CN110167599B (zh) 2016-12-28 2017-12-28 包含引入β-半乳糖苷的自我牺牲型连接基团的化合物
JP2019556777A JP7256751B2 (ja) 2016-12-28 2017-12-28 β－ガラクトシドが導入された自己犠牲リンカーを含む化合物
US16/472,983 US11065343B2 (en) 2016-12-28 2017-12-28 Compound bearing beta-galactoside-introduced self-immolative linker

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR20160180628 2016-12-28
KR10-2016-0180628 2016-12-28
KR1020170181411A KR102085798B1 (ko) 2016-12-28 2017-12-27 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물
KR10-2017-0181411 2017-12-27

Publications (2)

Publication Number Publication Date
WO2018124758A2 WO2018124758A2 (ko) 2018-07-05
WO2018124758A3 true WO2018124758A3 (ko) 2018-08-23

Family

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PCT/KR2017/015613 WO2018124758A2 (ko) 2016-12-28 2017-12-28 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물

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WO (1) WO2018124758A2 (ko)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020141460A2 (en) * 2019-01-03 2020-07-09 Intocell, Inc. Compounds comprising cleavable linker and uses thereof
AU2020205160A1 (en) * 2019-01-03 2021-06-24 Intocell, Inc. Compounds comprising cleavable linker and uses thereof
US20220226496A1 (en) * 2019-05-02 2022-07-21 Legochem Biosciences, Inc. Ligand-drug conjugate including linker having tris structure

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015095755A1 (en) * 2013-12-19 2015-06-25 Seattle Genetics, Inc. Methylene carbamate linkers for use with targeted-drug conjugates
KR20150137015A (ko) * 2014-05-28 2015-12-08 주식회사 레고켐 바이오사이언스 자가-희생 기를 포함하는 화합물
WO2016040684A1 (en) * 2014-09-11 2016-03-17 Seattle Genetics, Inc Targeted delivery of tertiary amine-containing drug substances

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015095755A1 (en) * 2013-12-19 2015-06-25 Seattle Genetics, Inc. Methylene carbamate linkers for use with targeted-drug conjugates
KR20150137015A (ko) * 2014-05-28 2015-12-08 주식회사 레고켐 바이오사이언스 자가-희생 기를 포함하는 화합물
WO2016040684A1 (en) * 2014-09-11 2016-03-17 Seattle Genetics, Inc Targeted delivery of tertiary amine-containing drug substances

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DEVALAPALLY, H.: "Beta-galactoside prodrugs of doxorubicin for application in antibody directed enzyme prodrug therapy/prodrug monotherapy", ARCHIVES OF PHARMACAL RESEARCH, vol. 30, 2007, pages 723 - 732, XP055535389 *
LEGIGAN, T. ET AL.: "The first generation of beta-galactosidase-responsive prodrugs designed for the selective treatment of solid tumors in prodrug monotherapy", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, vol. 51, no. 46, 20 September 2012 (2012-09-20), pages 11606 - 11610, XP002731989 *

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