RU2722449C2 - Полилигандные лекарственные конъюгаты и их применения - Google Patents

Полилигандные лекарственные конъюгаты и их применения Download PDF

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RU2722449C2
RU2722449C2 RU2018104266A RU2018104266A RU2722449C2 RU 2722449 C2 RU2722449 C2 RU 2722449C2 RU 2018104266 A RU2018104266 A RU 2018104266A RU 2018104266 A RU2018104266 A RU 2018104266A RU 2722449 C2 RU2722449 C2 RU 2722449C2
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pharmaceutically acceptable
cells
acceptable salt
cancer
receptor
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RU2018104266A
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RU2018104266A3 (enExample
RU2018104266A (ru
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Баохуа Роберт ХУАН
Цзянь ДАЙ
Чжунбо ВАН
Сюэюань СЕ
Сяодун Лю
Синьли ХУ
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Кохерент Байофарма
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Priority claimed from CN201510489556.6A external-priority patent/CN106466485B/zh
Priority claimed from CN201510489560.2A external-priority patent/CN106466484B/zh
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    • 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/551Medicinal 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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/401Proline; Derivatives thereof, e.g. captopril
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
RU2018104266A 2015-08-11 2016-08-11 Полилигандные лекарственные конъюгаты и их применения RU2722449C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201510489560.2 2015-08-11
CN201510489556.6 2015-08-11
CN201510489556.6A CN106466485B (zh) 2015-08-11 2015-08-11 一种具有细胞内吞介导功能的靶向配体-药物偶联体
CN201510489560.2A CN106466484B (zh) 2015-08-11 2015-08-11 一种具有细胞内吞介导功能的多靶向配体-药物偶联体
PCT/CN2016/094704 WO2017025057A1 (en) 2015-08-11 2016-08-11 Multi-ligand drug conjugates and uses thereof

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RU2018104266A3 RU2018104266A3 (enExample) 2019-09-12
RU2018104266A RU2018104266A (ru) 2019-09-12
RU2722449C2 true RU2722449C2 (ru) 2020-06-01

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EP (1) EP3334500B1 (enExample)
JP (3) JP6772199B2 (enExample)
KR (2) KR102301596B1 (enExample)
CN (3) CN108135881B (enExample)
AU (2) AU2016305703B2 (enExample)
CA (1) CA2987322C (enExample)
DK (1) DK3334500T3 (enExample)
ES (1) ES2877409T3 (enExample)
MX (1) MX381031B (enExample)
RU (1) RU2722449C2 (enExample)
WO (1) WO2017025057A1 (enExample)
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CN116059392B (zh) * 2021-09-03 2025-02-28 同宜医药(苏州)有限公司 配体偶联物及其应用
CA3231134A1 (en) * 2021-09-08 2023-03-16 Coherent Biopharma (Suzhou) Limited Pharmaceutical preparation, preparation method therefor and use thereof
TW202327659A (zh) * 2021-10-19 2023-07-16 大陸商同宜醫藥(蘇州)有限公司 偶聯體藥物製劑及其製備方法和用途
CN116196408A (zh) * 2021-12-30 2023-06-02 思格(苏州)生物科技有限公司 一种新型免疫佐剂及其制备方法和应用
TW202404643A (zh) * 2022-04-20 2024-02-01 大陸商同宜醫藥(蘇州)有限公司 化合物及用途
TW202421200A (zh) * 2022-11-09 2024-06-01 大陸商同宜醫藥(蘇州)有限公司 透過施用配體-藥物偶聯體治療癌症
CN120813385A (zh) * 2023-03-23 2025-10-17 同宜医药(苏州)有限公司 通过施用配体-药物偶联体治疗卵巢癌
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AU2016305703B2 (en) 2019-07-25
JP6772199B2 (ja) 2020-10-21
CN111617250B (zh) 2022-07-01
KR20200071152A (ko) 2020-06-18
KR102301596B1 (ko) 2021-09-14
KR20180033513A (ko) 2018-04-03
MX381031B (es) 2025-03-12
JP2021006549A (ja) 2021-01-21
EP3334500A1 (en) 2018-06-20
HK1250634A1 (zh) 2019-01-11
CN108135881B (zh) 2020-11-13
RU2018104266A3 (enExample) 2019-09-12
AU2019240611B2 (en) 2021-09-09
KR102464778B1 (ko) 2022-11-07
RU2018104266A (ru) 2019-09-12
JP2018529632A (ja) 2018-10-11
CA2987322C (en) 2020-02-11
US20180200377A1 (en) 2018-07-19
JP2023025151A (ja) 2023-02-21
CN112263683A (zh) 2021-01-26
JP7573401B2 (ja) 2024-10-25
EP3334500A4 (en) 2019-04-03
DK3334500T3 (da) 2021-06-21
AU2019240611A1 (en) 2019-10-17
CN108135881A (zh) 2018-06-08
CN111617250A (zh) 2020-09-04
AU2016305703A1 (en) 2017-11-23
WO2017025057A1 (en) 2017-02-16
CA2987322A1 (en) 2017-02-16
US11571480B2 (en) 2023-02-07
ZA201707464B (en) 2021-05-26
ES2877409T3 (es) 2021-11-16
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US20240100175A1 (en) 2024-03-28
EP3334500B1 (en) 2021-04-07

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