TN2019000303A1 - Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation - Google Patents

Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation

Info

Publication number
TN2019000303A1
TN2019000303A1 TNP/2019/000303A TN2019000303A TN2019000303A1 TN 2019000303 A1 TN2019000303 A1 TN 2019000303A1 TN 2019000303 A TN2019000303 A TN 2019000303A TN 2019000303 A1 TN2019000303 A1 TN 2019000303A1
Authority
TN
Tunisia
Prior art keywords
conjugates
therapy
useful
preparation
cryptophycin
Prior art date
Application number
TNP/2019/000303A
Other languages
English (en)
Inventor
Philippe Hubert
Hervé Bouchard
Marie-Priscille Brun
Original Assignee
Sanofi Sa
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.)
Filing date
Publication date
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of TN2019000303A1 publication Critical patent/TN2019000303A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/15Depsipeptides; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/64Drug-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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817Toxins
    • A61K47/6829Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6889Conjugates 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K11/00Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (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)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TNP/2019/000303A 2017-05-10 2018-05-09 Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation TN2019000303A1 (en)

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
TN2019000303A1 true TN2019000303A1 (en) 2021-05-07

Family

ID=58873750

Family Applications (1)

Application Number Title Priority Date Filing Date
TNP/2019/000303A TN2019000303A1 (en) 2017-05-10 2018-05-09 Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation

Country Status (21)

Country Link
US (5) US20180369401A1 (enExample)
EP (1) EP3621658A1 (enExample)
JP (2) JP2020519610A (enExample)
KR (1) KR102722886B1 (enExample)
CN (1) CN110831633A (enExample)
AR (1) AR111781A1 (enExample)
AU (2) AU2018265333C1 (enExample)
BR (1) BR112019023336A2 (enExample)
CA (1) CA3062977A1 (enExample)
CO (1) CO2019012108A2 (enExample)
EA (1) EA201992667A1 (enExample)
EC (1) ECSP19078277A (enExample)
IL (1) IL270507B2 (enExample)
MA (1) MA50764A (enExample)
MX (1) MX2019013421A (enExample)
MY (1) MY204075A (enExample)
PH (1) PH12019550230A1 (enExample)
TN (1) TN2019000303A1 (enExample)
TW (1) TWI778059B (enExample)
UY (1) UY37728A (enExample)
WO (1) WO2018206635A1 (enExample)

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US11951165B2 (en) 2016-12-30 2024-04-09 Vaxcyte, Inc. Conjugated vaccine carrier proteins
MX2019007910A (es) 2016-12-30 2019-12-05 Sutrovax Inc Conjugados de polipeptido-antigeno con aminoacidos no naturales.
US20180369401A1 (en) 2017-05-10 2018-12-27 Sanofi Novel peptidic linkers and cryptophycin conjugates, their preparation and their therapeutic use
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
CN114053426B (zh) * 2020-07-30 2024-06-18 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
CN115105607B (zh) * 2021-03-22 2024-12-20 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
EP4482529A1 (en) 2022-02-22 2025-01-01 Araris Biotech AG Peptide linkers comprising two or more payloads
CN115212315A (zh) * 2022-08-03 2022-10-21 联宁(苏州)生物制药有限公司 一种抗体偶联药物中间体及含有其的抗体偶联药物
WO2025082990A1 (en) 2023-10-15 2025-04-24 Araris Biotech Ag Antibody-drug conjugates using two different types of topoisomerase i inhibitors

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EP0735819B1 (en) 1993-12-21 2001-07-11 University Of Hawaii Cryptophycins
SI0934065T1 (sl) * 1996-08-30 2007-02-28 Univ Hawaii Novi kriptoficinski derivati kot anti-neoplasticna sredstva
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US20050175619A1 (en) 2004-02-05 2005-08-11 Robert Duffy Methods of producing antibody conjugates
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US20180369401A1 (en) 2017-05-10 2018-12-27 Sanofi Novel peptidic linkers and cryptophycin conjugates, their preparation and their therapeutic use

Also Published As

Publication number Publication date
JP2020519610A (ja) 2020-07-02
AR111781A1 (es) 2019-08-21
ECSP19078277A (es) 2019-11-30
AU2022204711C1 (en) 2025-04-24
EP3621658A1 (en) 2020-03-18
BR112019023336A2 (pt) 2020-06-16
US20200093934A1 (en) 2020-03-26
AU2018265333C1 (en) 2025-04-24
IL270507A (enExample) 2019-12-31
KR20200005580A (ko) 2020-01-15
UY37728A (es) 2019-01-02
JP2023085475A (ja) 2023-06-20
CO2019012108A2 (es) 2020-02-28
IL270507B1 (en) 2023-04-01
CN110831633A (zh) 2020-02-21
AU2022204711B9 (en) 2025-01-23
MX2019013421A (es) 2020-02-05
TWI778059B (zh) 2022-09-21
EA201992667A1 (ru) 2020-03-10
AU2022204711B2 (en) 2024-01-04
US20180369401A1 (en) 2018-12-27
TW201907957A (zh) 2019-03-01
CA3062977A1 (en) 2018-11-15
AU2022204711A1 (en) 2022-07-21
US20210228726A1 (en) 2021-07-29
MY204075A (en) 2024-08-06
US11998611B2 (en) 2024-06-04
US20250205348A1 (en) 2025-06-26
MA50764A (fr) 2020-03-18
IL270507B2 (en) 2023-08-01
AU2018265333A1 (en) 2019-11-28
KR102722886B1 (ko) 2024-10-29
PH12019550230A1 (en) 2020-07-06
AU2018265333B2 (en) 2022-07-21
WO2018206635A1 (en) 2018-11-15
US11007275B2 (en) 2021-05-18
US20200054760A1 (en) 2020-02-20

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