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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compound
pharmaceutically acceptable
acceptable salt
cells
cancer
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RU2018104266A
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Russian (ru)
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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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    • 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
    • A61K47/55—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A61K47/551—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/62—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (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
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
CN201510489560.2 2015-08-11
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
CN201510489556.6 2015-08-11
PCT/CN2016/094704 WO2017025057A1 (en) 2015-08-11 2016-08-11 Multi-ligand drug conjugates and uses thereof

Publications (3)

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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) CN111617250B (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)
ZA (1) ZA201707464B (enExample)

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TW202317199A (zh) * 2021-06-25 2023-05-01 大陸商同宜醫藥（蘇州）有限公司 配體藥物偶聯物及其應用
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
AU2022344391B2 (en) * 2021-09-08 2026-02-05 Coherent Biopharma (Suzhou) Limited Pharmaceutical preparation, preparation method therefor and use thereof
WO2023066251A1 (zh) * 2021-10-19 2023-04-27 同宜医药（苏州）有限公司 偶联体药物制剂及其制备方法和用途
CN116196408B (zh) * 2021-12-30 2026-01-06 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
WO2024099387A1 (zh) * 2022-11-09 2024-05-16 同宜医药（苏州）有限公司 通过施用配体-药物偶联体治疗癌症
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
CN121001746A (zh) * 2023-04-26 2025-11-21 同宜医药（苏州）有限公司 一种配体-药物偶联体在治疗癌症中的用途

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JP7573401B2 (ja) 2024-10-25
AU2019240611A1 (en) 2019-10-17
HK1250634A1 (zh) 2019-01-11
JP6772199B2 (ja) 2020-10-21
KR102301596B1 (ko) 2021-09-14
CN108135881B (zh) 2020-11-13
MX381031B (es) 2025-03-12
ZA201707464B (en) 2021-05-26
CN111617250B (zh) 2022-07-01
KR20200071152A (ko) 2020-06-18
EP3334500A1 (en) 2018-06-20
ES2877409T3 (es) 2021-11-16
CN108135881A (zh) 2018-06-08
US20240100175A1 (en) 2024-03-28
JP2018529632A (ja) 2018-10-11
AU2016305703A1 (en) 2017-11-23
RU2018104266A3 (enExample) 2019-09-12
CN111617250A (zh) 2020-09-04
US11571480B2 (en) 2023-02-07
MX2018001723A (es) 2018-05-17
AU2019240611B2 (en) 2021-09-09
KR102464778B1 (ko) 2022-11-07
US20180200377A1 (en) 2018-07-19
JP2021006549A (ja) 2021-01-21
AU2016305703B2 (en) 2019-07-25
EP3334500B1 (en) 2021-04-07
KR20180033513A (ko) 2018-04-03
CA2987322A1 (en) 2017-02-16
DK3334500T3 (da) 2021-06-21
EP3334500A4 (en) 2019-04-03
CN112263683A (zh) 2021-01-26
RU2018104266A (ru) 2019-09-12
WO2017025057A1 (en) 2017-02-16
CA2987322C (en) 2020-02-11
JP2023025151A (ja) 2023-02-21

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