WO2018124512A3 - 압타머-약물 콘쥬게이트 및 그 용도 - Google Patents

압타머-약물 콘쥬게이트 및 그 용도 Download PDF

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WO2018124512A3
WO2018124512A3 PCT/KR2017/014060 KR2017014060W WO2018124512A3 WO 2018124512 A3 WO2018124512 A3 WO 2018124512A3 KR 2017014060 W KR2017014060 W KR 2017014060W WO 2018124512 A3 WO2018124512 A3 WO 2018124512A3
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Prior art keywords
aptamer
drug conjugate
drug
derivative
monomethyl auristatin
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PCT/KR2017/014060
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English (en)
French (fr)
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WO2018124512A2 (ko
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이중환
임종훈
김종인
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이중환
인터올리고 주식회사
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Priority to EP17887935.9A priority Critical patent/EP3560517A4/en
Priority to JP2019555545A priority patent/JP7067802B2/ja
Priority to AU2017389094A priority patent/AU2017389094B2/en
Priority to US16/473,771 priority patent/US11458120B2/en
Priority to CN201780080822.7A priority patent/CN110167597A/zh
Publication of WO2018124512A2 publication Critical patent/WO2018124512A2/ko
Publication of WO2018124512A3 publication Critical patent/WO2018124512A3/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
    • A61K47/50—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
    • A61K47/54—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 organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • 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
    • A61K47/54—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 organic compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/115—Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith ; Nucleic acids binding to non-nucleic acids, e.g. aptamers
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/16—Aptamers

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  • Physics & Mathematics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

본 발명은 약물-링커-AS1411 구조를 포함하는 암 표적 치료제에 관한 것으로, 약물은 모노메틸 오리스타틴 E(MMAE), 모노메틸 오리스타틴 F(MMAF), 시타라빈, 젬시타빈, 메이탄시네, DM1, DM4, 칼리키아미신 및 그 유도체, 독소루비신, 듀오카르마이신 및 그 유도체, 피롤로벤조디아제핀(PBD), SN-38, α-아만틴, 및 투불루신 유사체(Tubulysin analog) 등으로부터 선택될 수 있다.
PCT/KR2017/014060 2016-12-26 2017-12-04 압타머-약물 콘쥬게이트 및 그 용도 WO2018124512A2 (ko)

Priority Applications (5)

Application Number Priority Date Filing Date Title
EP17887935.9A EP3560517A4 (en) 2016-12-26 2017-12-04 APTAMER INGREDIENT CONJUGATE AND USE OF IT
JP2019555545A JP7067802B2 (ja) 2016-12-26 2017-12-04 アプタマー－薬物コンジュゲート及びその用途
AU2017389094A AU2017389094B2 (en) 2016-12-26 2017-12-04 Aptamer-drug conjugate and use thereof
US16/473,771 US11458120B2 (en) 2016-12-26 2017-12-04 Aptamer-drug conjugate and use thereof
CN201780080822.7A CN110167597A (zh) 2016-12-26 2017-12-04 适配体-药物缀合物及其用途

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2016-0179111 2016-12-26
KR1020160179111A KR102015524B1 (ko) 2016-12-26 2016-12-26 압타머-약물 콘쥬게이트 및 그 용도

Publications (2)

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WO2018124512A2 WO2018124512A2 (ko) 2018-07-05
WO2018124512A3 true WO2018124512A3 (ko) 2018-08-23

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PCT/KR2017/014060 WO2018124512A2 (ko) 2016-12-26 2017-12-04 압타머-약물 콘쥬게이트 및 그 용도

Country Status (7)

Country Link
US (1) US11458120B2 (ko)
EP (1) EP3560517A4 (ko)
JP (1) JP7067802B2 (ko)
KR (1) KR102015524B1 (ko)
CN (1) CN110167597A (ko)
AU (1) AU2017389094B2 (ko)
WO (1) WO2018124512A2 (ko)

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Publication number Priority date Publication date Assignee Title
KR102280330B1 (ko) * 2018-10-19 2021-07-21 인터올리고 주식회사 치료 효능을 개선한 핵산 변형체 및 이를 포함하는 항암용 약학 조성물
US20210388361A1 (en) * 2018-10-19 2021-12-16 Interoligo Corporation Modified nucleic acid having improved treatment efficacy, and anticancer pharmaceutical composition containing same
KR20210061293A (ko) * 2019-11-19 2021-05-27 주식회사 바이오이즈 압타머 기반 표적화 복합 항암제
CN113941007B (zh) * 2020-07-16 2024-06-07 成都科岭源医药技术有限公司 一种串联的双药物链接组装单元及其应用
CN114053248B (zh) * 2020-08-10 2023-10-20 复旦大学 一种调控肿瘤代谢的核酸和小分子药物共递送纳米制剂及其制备方法
WO2022094609A1 (en) * 2020-10-30 2022-05-05 Speer Tod Oligonucleotide-based therapeutics and uses thereof
AU2022411618A1 (en) * 2021-12-16 2024-07-04 Interoligo Corporation. Modified oligonucleotide-drug conjugate and use thereof
CN115227829B (zh) * 2022-02-22 2023-10-13 成都中医药大学 酸敏感性适配体雷公藤甲素偶联物及应用

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Publication number Publication date
AU2017389094B2 (en) 2023-01-05
US20190358202A1 (en) 2019-11-28
US11458120B2 (en) 2022-10-04
EP3560517A4 (en) 2020-08-26
KR20180075133A (ko) 2018-07-04
CN110167597A (zh) 2019-08-23
WO2018124512A2 (ko) 2018-07-05
JP2020512393A (ja) 2020-04-23
KR102015524B1 (ko) 2019-08-29
JP7067802B2 (ja) 2022-05-16
AU2017389094A1 (en) 2019-07-11
EP3560517A2 (en) 2019-10-30

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