CN118271394A - 药物接头化合物的制备方法 - Google Patents

药物接头化合物的制备方法 Download PDF

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Publication number
CN118271394A
CN118271394A CN202410349991.8A CN202410349991A CN118271394A CN 118271394 A CN118271394 A CN 118271394A CN 202410349991 A CN202410349991 A CN 202410349991A CN 118271394 A CN118271394 A CN 118271394A
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CN
China
Prior art keywords
compound
formula
alkyl
salt
aryl
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Pending
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CN202410349991.8A
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English (en)
Chinese (zh)
Inventor
S·布兰查德
J·寇茨
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Sijin Co
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Sijin Co
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Publication of CN118271394A publication Critical patent/CN118271394A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K47/6835—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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/10—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using coupling agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Analytical Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202410349991.8A 2017-11-30 2018-11-29 药物接头化合物的制备方法 Pending CN118271394A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201762593104P 2017-11-30 2017-11-30
US62/593,104 2017-11-30
PCT/US2018/063070 WO2019108797A1 (en) 2017-11-30 2018-11-29 Process for the preparation of drug linker compounds
CN201880077478.0A CN111417408B (zh) 2017-11-30 2018-11-29 药物接头化合物的制备方法

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201880077478.0A Division CN111417408B (zh) 2017-11-30 2018-11-29 药物接头化合物的制备方法

Publications (1)

Publication Number Publication Date
CN118271394A true CN118271394A (zh) 2024-07-02

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
CN202410349991.8A Pending CN118271394A (zh) 2017-11-30 2018-11-29 药物接头化合物的制备方法
CN201880077478.0A Active CN111417408B (zh) 2017-11-30 2018-11-29 药物接头化合物的制备方法

Family Applications After (1)

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CN201880077478.0A Active CN111417408B (zh) 2017-11-30 2018-11-29 药物接头化合物的制备方法

Country Status (15)

Country Link
US (2) US11612666B2 (https=)
EP (1) EP3717016A4 (https=)
JP (2) JP7402159B2 (https=)
KR (2) KR102762352B1 (https=)
CN (2) CN118271394A (https=)
AU (1) AU2018375412B2 (https=)
BR (1) BR112020010503A2 (https=)
CA (1) CA3082165A1 (https=)
EA (1) EA202091340A1 (https=)
IL (1) IL274757B2 (https=)
MA (1) MA51870A (https=)
MX (2) MX2020005565A (https=)
SG (1) SG11202004698RA (https=)
WO (1) WO2019108797A1 (https=)
ZA (1) ZA202003037B (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3085001C (en) * 2019-05-20 2021-10-05 Mabplex International, Ltd. One-pot process for preparing intermediate of antibody-drug conjugate
WO2021077317A1 (zh) * 2019-10-23 2021-04-29 烟台迈百瑞国际生物医药股份有限公司 一种寡肽连接子中间体及其制备方法
BR112023018676A2 (pt) 2021-03-18 2023-10-10 Seagen Inc Conjugado anticorpo-fármaco, composição farmacêutica, métodos de tratamento de uma doença ou condição e de um câncer, e, composição de conjugado ligante-fármaco
CN115873066A (zh) * 2022-07-27 2023-03-31 吉林省博大伟业制药有限公司 一种抗体偶联药物连接子的合成方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6214345B1 (en) * 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
EP2478912B1 (en) * 2003-11-06 2016-08-31 Seattle Genetics, Inc. Auristatin conjugates with anti-HER2 or anti-CD22 antibodies and their use in therapy
ES2382879T3 (es) * 2005-09-14 2012-06-14 Ucb Pharma, S.A. Conjugado de anticuerpo - polímero de peine.
JP2010503708A (ja) 2006-09-15 2010-02-04 エンゾン ファーマスーティカルズ インコーポレイテッド 多官能性リンカーを含む標的化ポリマープロドラッグ
EP2170805B1 (en) * 2007-06-21 2016-03-16 Amgen Inc. Methods of synthesizing cinacalcet and salts thereof
KR102356286B1 (ko) * 2011-05-27 2022-02-08 암브룩스, 인코포레이티드 비-천연 아미노산 연결된 돌라스타틴 유도체를 함유하는 조성물, 이를 수반하는 방법, 및 용도
CN104640572B (zh) 2012-05-15 2018-04-27 索伦托医疗有限公司 药物偶联物，偶联方法，及其用途
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
GB201309807D0 (en) 2013-05-31 2013-07-17 Pharma Mar Sau Antibody drug conjugates
GB201416960D0 (en) * 2014-09-25 2014-11-12 Antikor Biopharma Ltd Biological materials and uses thereof
US9533483B2 (en) 2014-09-26 2017-01-03 Kimberly-Clark Worldwide, Inc. Apparatus for and method of shaping and applying a segment to a moving web

Also Published As

Publication number Publication date
MX2020005565A (es) 2020-08-20
IL274757B1 (en) 2025-12-01
CN111417408B (zh) 2024-04-23
US20240042052A1 (en) 2024-02-08
AU2018375412B2 (en) 2025-01-02
JP2021505542A (ja) 2021-02-18
WO2019108797A1 (en) 2019-06-06
ZA202003037B (en) 2023-12-20
US20200360532A1 (en) 2020-11-19
EP3717016A1 (en) 2020-10-07
KR20200094185A (ko) 2020-08-06
KR20250024092A (ko) 2025-02-18
AU2018375412A1 (en) 2020-05-28
SG11202004698RA (en) 2020-06-29
JP2023164652A (ja) 2023-11-10
JP7402159B2 (ja) 2023-12-20
JP7787859B2 (ja) 2025-12-17
MX2023009372A (es) 2023-08-16
MA51870A (fr) 2020-10-07
IL274757B2 (en) 2026-04-01
BR112020010503A2 (pt) 2020-10-20
CA3082165A1 (en) 2019-06-06
IL274757A (en) 2020-07-30
EP3717016A4 (en) 2021-09-01
EA202091340A1 (ru) 2020-10-16
KR102762352B1 (ko) 2025-02-05
US11612666B2 (en) 2023-03-28
CN111417408A (zh) 2020-07-14

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