EA202091217A1 - Конъюгат аналога тубулизина с разветвленными линкерами - Google Patents

Конъюгат аналога тубулизина с разветвленными линкерами

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Publication number
EA202091217A1
EA202091217A1 EA202091217A EA202091217A EA202091217A1 EA 202091217 A1 EA202091217 A1 EA 202091217A1 EA 202091217 A EA202091217 A EA 202091217A EA 202091217 A EA202091217 A EA 202091217A EA 202091217 A1 EA202091217 A1 EA 202091217A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tubulisin
branched
conjugate
analogue conjugate
branched linkers
Prior art date
Application number
EA202091217A
Other languages
English (en)
Inventor
Роберт Юнсинь Чжао
Цинлян Ян
Юаньюань Хуан
Линьяо Чжао
Шунь Гай
Ханбо Е
Цзюнь Лэй
Ифан Сюй
Минцзюнь Цао
Хуэйхуэй Го
Цзюньсян Цзя
Цяньцянь Тун
Вэньцзюнь Ли
Сяомай Чжоу
Хуншэн Се
Лу Бай
Сян Цай
Сяотао Чжо
Сючжэн Чжан
Цзюнь Чжэн
Original Assignee
Ханчжоу Дак Байотек Ко. Лтд
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 Ханчжоу Дак Байотек Ко. Лтд filed Critical Ханчжоу Дак Байотек Ко. Лтд
Publication of EA202091217A1 publication Critical patent/EA202091217A1/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
    • A61K38/07—Tetrapeptides
    • 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
    • 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
    • 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
    • A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • 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
    • A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6855—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic

Landscapes

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

Abstract

Настоящее изобретение относится к конъюгации соединения аналога тубулизина со связывающейся с клеткой молекулой с разветвленными линкерами/линкерами боковой цепи для обеспечения лучшей доставки соединения конъюгата и точного целевого лечения аномальных клеток. Оно также относится к способу конъюгации молекулы аналога тубулизина и связывающегося с клеткой лиганда с помощью разветвленных связей, а также к способу применения конъюгата в целевом лечении онкологического, инфекционного и аутоиммунного заболевания.
EA202091217A 2017-12-31 2017-12-31 Конъюгат аналога тубулизина с разветвленными линкерами EA202091217A1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2017/120454 WO2019127607A1 (en) 2017-12-31 2017-12-31 A conjugate of a tubulysin analog with branched linkers

Publications (1)

Publication Number Publication Date
EA202091217A1 true EA202091217A1 (ru) 2020-09-18

Family

ID=67064953

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202091217A EA202091217A1 (ru) 2017-12-31 2017-12-31 Конъюгат аналога тубулизина с разветвленными линкерами

Country Status (17)

Country Link
US (3) US20230149502A1 (ru)
EP (1) EP3621652A4 (ru)
JP (2) JP7262817B2 (ru)
KR (2) KR102603344B1 (ru)
CN (1) CN111093707A (ru)
AU (2) AU2017445144A1 (ru)
BR (1) BR112020010405A2 (ru)
CA (1) CA3085634C (ru)
CL (1) CL2020001600A1 (ru)
EA (1) EA202091217A1 (ru)
IL (1) IL275274A (ru)
MX (1) MX2020006192A (ru)
NZ (1) NZ764814A (ru)
PH (1) PH12020550657A1 (ru)
SG (1) SG11202004801WA (ru)
WO (1) WO2019127607A1 (ru)
ZA (1) ZA202003211B (ru)

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* Cited by examiner, † Cited by third party
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PL2872157T3 (pl) 2012-07-12 2020-07-13 Hangzhou Dac Biotech Co., Ltd Koniugaty wiążących komórkę cząsteczek ze środkami cytotoksycznymi
US11873281B2 (en) 2012-07-12 2024-01-16 Hangzhou Dac Biotech Co., Ltd. Conjugates of cell binding molecules with cytotoxic agents
CN114040779A (zh) * 2019-06-24 2022-02-11 杭州多禧生物科技有限公司 含支链连接子的细胞结合分子与细胞毒性剂的偶联物
US20220249594A1 (en) * 2019-06-24 2022-08-11 Hangzhou Dac Biotech Co., Ltd A formulation of a conjugate of a tubulysin analog to a cell-binding molecule
EP3991752A4 (en) * 2019-06-29 2023-03-29 Hangzhou Dac Biotech Co., Ltd CELL BINDING MOLECULE-TUBULYSIN DERIVATIVE CONJUGATE AND METHOD OF PREPARATION THEREOF
US11596693B2 (en) 2019-08-07 2023-03-07 Mabplex International Co., Ltd Antibody-drug conjugates and uses thereof
CA3108168A1 (en) * 2020-02-05 2021-08-05 Yue Zhang Conjugates of cell-binding molecules with cytotoxic agents
US11045546B1 (en) 2020-03-30 2021-06-29 Cytodyn Inc. Methods of treating coronavirus infection
CN112755173B (zh) * 2020-12-31 2022-01-07 深圳市科达顺生物技术有限公司 用于治疗三阴性乳腺癌的Ii-Key/HER2杂交多肽药物及其制备方法
CN112961060B (zh) * 2021-02-09 2022-03-25 武汉大学 同位素标记的n,n-二甲基乙二胺及其制备方法和短链脂肪酸的分析方法
AU2022259314A1 (en) * 2021-04-14 2023-11-30 Genequantum Healthcare (Suzhou) Co., Ltd. Linkers, conjugates and applications thereof
WO2022078524A2 (en) * 2021-11-03 2022-04-21 Hangzhou Dac Biotech Co., Ltd. Specific conjugation of an antibody

Family Cites Families (12)

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EP1521769B1 (de) * 2002-07-09 2015-09-09 Dömling, Alexander Tubulysinkonjugate
CN101678124A (zh) * 2007-03-14 2010-03-24 恩多塞特公司 结合配体连接的微管溶素递药缀合物
CA2891280C (en) * 2012-11-24 2018-03-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
PT3122757T (pt) 2014-02-28 2023-11-03 Hangzhou Dac Biotech Co Ltd Ligantes carregados e as suas utilizações em conjugação
KR20160142392A (ko) * 2014-04-11 2016-12-12 메디뮨 엘엘씨 튜부리신 유도체
CN110279872A (zh) * 2014-11-11 2019-09-27 杭州多禧生物科技有限公司 细胞毒素分子同细胞结合受体分子的共轭体
WO2015151078A2 (en) 2015-06-15 2015-10-08 Suzhou M-Conj Biotech Co., Ltd Hydrophilic linkers for conjugation
CA2991975C (en) * 2015-08-10 2021-04-06 Suzhou M-Conj Biotech Co., Ltd. Novel linkers and their uses in specific conjugation of drugs to a biological molecule
AU2016202632B2 (en) * 2016-02-04 2021-09-09 Hangzhou Dac Biotech Co, Ltd Specific conjugation linkers, specific immunoconjugates thereof, methods of making and uses such conjugates thereof
BR112018071465A2 (pt) * 2016-04-20 2019-02-05 Hangzhou Dac Biotech Co Ltd derivados de toxinas de amanita e sua conjugação a uma molécula de ligação celular
JP7138350B2 (ja) * 2016-11-14 2022-09-16 ハンジョウ ディーエーシー バイオテック シーオー．，エルティディ． 共役連結体、該連結体を含有する細胞結合分子－薬物共役体、並びに該共役体及び連結体の使用及び製造方法
EA201992081A1 (ru) * 2017-04-06 2020-01-21 Ханчжоу Дэк Биотек Ко., Лтд Конъюгирование цитотоксических лекарственных средств посредством бис-связывания

Also Published As

Publication number Publication date
KR102641565B1 (ko) 2024-02-27
KR102603344B1 (ko) 2023-11-16
AU2017445144A1 (en) 2020-06-18
JP7262817B2 (ja) 2023-04-24
EP3621652A4 (en) 2021-01-13
EP3621652A1 (en) 2020-03-18
US20200276261A1 (en) 2020-09-03
IL275274A (en) 2020-07-30
CL2020001600A1 (es) 2021-03-19
ZA202003211B (en) 2024-04-24
NZ764814A (en) 2024-02-23
BR112020010405A2 (pt) 2020-11-24
KR20230075530A (ko) 2023-05-31
US20230165930A1 (en) 2023-06-01
MX2020006192A (es) 2020-08-20
CA3085634A1 (en) 2019-07-04
US20230165931A1 (en) 2023-06-01
JP2023093531A (ja) 2023-07-04
CA3085634C (en) 2023-11-14
JP2021507928A (ja) 2021-02-25
WO2019127607A1 (en) 2019-07-04
AU2022205269A1 (en) 2022-08-11
PH12020550657A1 (en) 2021-04-19
US20230149502A1 (en) 2023-05-18
SG11202004801WA (en) 2020-06-29
KR20200097295A (ko) 2020-08-18
CN111093707A (zh) 2020-05-01

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