EA201992667A1 - Новые пептидные линкеры и конъюгаты на основе криптофицина, их получение и их терапевтическое применение - Google Patents

Новые пептидные линкеры и конъюгаты на основе криптофицина, их получение и их терапевтическое применение

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Publication number
EA201992667A1
EA201992667A1 EA201992667A EA201992667A EA201992667A1 EA 201992667 A1 EA201992667 A1 EA 201992667A1 EA 201992667 A EA201992667 A EA 201992667A EA 201992667 A EA201992667 A EA 201992667A EA 201992667 A1 EA201992667 A1 EA 201992667A1
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EA
Eurasian Patent Office
Prior art keywords
cryptophycin
therapeutic use
production
present
conjugates based
Prior art date
Application number
EA201992667A
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English (en)
Inventor
Эрве Бушар
Мари-Присцилл Брэн
Филипп Юбер
Original Assignee
Санофи
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Publication date
Application filed by Санофи filed Critical Санофи
Publication of EA201992667A1 publication Critical patent/EA201992667A1/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/15—Depsipeptides; Derivatives thereof
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • A61K47/6829—Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • 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
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Toxicology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I)где RCG1 представляет собой реакционноспособную химическую группу, которая является реакционноспособной в отношении химической группы, присутствующей на полипептиде, таком как антитело; P представляет собой H, OH или активированный O; и L представляет собой конкретный линкер. Настоящее изобретение также относится к полезным нагрузкам с криптофицином, а также к конъюгатам на основе криптофицина, к композициям, содержащим их, и к их терапевтическому применению, особенно в качестве противораковых средств. Настоящее изобретение также относится к способу получения таких конъюгатов.
EA201992667A 2017-05-10 2018-05-09 Новые пептидные линкеры и конъюгаты на основе криптофицина, их получение и их терапевтическое применение EA201992667A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17305531 2017-05-10
PCT/EP2018/061989 WO2018206635A1 (en) 2017-05-10 2018-05-09 Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation

Publications (1)

Publication Number Publication Date
EA201992667A1 true EA201992667A1 (ru) 2020-03-10

Family

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EA201992667A EA201992667A1 (ru) 2017-05-10 2018-05-09 Новые пептидные линкеры и конъюгаты на основе криптофицина, их получение и их терапевтическое применение

Country Status (20)

Country Link
US (4) US20200093934A1 (ru)
EP (1) EP3621658A1 (ru)
JP (2) JP2020519610A (ru)
KR (1) KR20200005580A (ru)
CN (1) CN110831633A (ru)
AR (1) AR111781A1 (ru)
AU (2) AU2018265333C1 (ru)
BR (1) BR112019023336A2 (ru)
CA (1) CA3062977A1 (ru)
CO (1) CO2019012108A2 (ru)
EA (1) EA201992667A1 (ru)
EC (1) ECSP19078277A (ru)
IL (1) IL270507B2 (ru)
MA (1) MA50764A (ru)
MX (1) MX2019013421A (ru)
PH (1) PH12019550230A1 (ru)
TN (1) TN2019000303A1 (ru)
TW (1) TWI778059B (ru)
UY (1) UY37728A (ru)
WO (1) WO2018206635A1 (ru)

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US11951165B2 (en) 2016-12-30 2024-04-09 Vaxcyte, Inc. Conjugated vaccine carrier proteins
CN111154133B (zh) * 2020-01-03 2022-07-12 万华化学集团股份有限公司 一种环氧树脂发泡剂，环氧树脂组合物及环氧发泡材料的制备方法和用途
CN114053426A (zh) * 2020-07-30 2022-02-18 成都科岭源医药技术有限公司 一种双药链接组装单元及双药靶向接头-药物偶联物
CN115105607A (zh) * 2021-03-22 2022-09-27 成都科岭源医药技术有限公司 一种用于adc的双药-接头的制备方法及其用途
WO2023161291A1 (en) 2022-02-22 2023-08-31 Araris Biotech Ag Peptide linkers comprising two or more payloads

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ATE328592T1 (de) * 1996-08-30 2006-06-15 Univ Hawaii Neue cryptophycin-derivate als antineoplastika
US20050175619A1 (en) 2004-02-05 2005-08-11 Robert Duffy Methods of producing antibody conjugates
ZA200900545B (en) 2006-07-18 2010-03-31 Sanofi Aventis Antagonist antibody against EPHA2 for the treatment of cancer
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WO2015057876A1 (en) * 2013-10-15 2015-04-23 Sorrento Therapeutics Inc. Drug-conjugates with a targeting molecule and two different drugs
KR102645430B1 (ko) 2013-10-15 2024-03-11 씨젠 인크. 개선된 리간드-약물 컨쥬게이트 약물동력학을 위한 peg화된 약물-링커
US10758636B2 (en) * 2013-11-12 2020-09-01 Centre For Probe Development And Commercialization Residualizing linkers and uses thereof
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TWI714661B (zh) * 2015-11-05 2021-01-01 法商賽諾菲公司 新穎念珠藻素化合物及接合物、其製備與其治療用途
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Also Published As

Publication number Publication date
TWI778059B (zh) 2022-09-21
CN110831633A (zh) 2020-02-21
AU2022204711A1 (en) 2022-07-21
MX2019013421A (es) 2020-02-05
PH12019550230A1 (en) 2020-07-06
BR112019023336A2 (pt) 2020-06-16
US20200093934A1 (en) 2020-03-26
TW201907957A (zh) 2019-03-01
AR111781A1 (es) 2019-08-21
AU2022204711B2 (en) 2024-01-04
IL270507A (ru) 2019-12-31
ECSP19078277A (es) 2019-11-30
KR20200005580A (ko) 2020-01-15
CA3062977A1 (en) 2018-11-15
EP3621658A1 (en) 2020-03-18
JP2023085475A (ja) 2023-06-20
US20180369401A1 (en) 2018-12-27
JP2020519610A (ja) 2020-07-02
US20200054760A1 (en) 2020-02-20
UY37728A (es) 2019-01-02
IL270507B1 (en) 2023-04-01
AU2018265333C1 (en) 2023-08-17
WO2018206635A1 (en) 2018-11-15
US11007275B2 (en) 2021-05-18
MA50764A (fr) 2020-03-18
AU2018265333B2 (en) 2022-07-21
IL270507B2 (en) 2023-08-01
CO2019012108A2 (es) 2020-02-28
TN2019000303A1 (en) 2021-05-07
AU2018265333A1 (en) 2019-11-28
US20210228726A1 (en) 2021-07-29

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