CL2025002018A1 - Conectores, conectores-fármaco, conjugados de los mismos y métodos para su uso. - Google Patents

Conectores, conectores-fármaco, conjugados de los mismos y métodos para su uso.

Info

Publication number
CL2025002018A1
CL2025002018A1 CL2025002018A CL2025002018A CL2025002018A1 CL 2025002018 A1 CL2025002018 A1 CL 2025002018A1 CL 2025002018 A CL2025002018 A CL 2025002018A CL 2025002018 A CL2025002018 A CL 2025002018A CL 2025002018 A1 CL2025002018 A1 CL 2025002018A1
Authority
CL
Chile
Prior art keywords
group
unit
binding site
drug
optionally
Prior art date
Application number
CL2025002018A
Other languages
English (en)
Inventor
Shang Xiao
Liu Haidong
Wang Guobao
Jiang Xiaolong
Original Assignee
Genmab As
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 Genmab As filed Critical Genmab As
Publication of CL2025002018A1 publication Critical patent/CL2025002018A1/es

Links

Classifications

    • 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
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • 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
    • A61K47/68037—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
    • 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
    • A61K47/6883—Polymer-drug antibody conjugates, e.g. mitomycin-dextran-Ab; DNA-polylysine-antibody complex or conjugate used for therapy
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)
  • Polyamides (AREA)
  • Polyethers (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Compuestos conectores, o estereoisómeros o sales de los mismos, que incluyen (a) una unidad conectora que tiene entre 1 y 4 sitios de unión a una unidad de fármaco y que presenta una de las siguientes estructuras (i) o (ii): (i) (ii) ; (b) por lo menos un grupo polar que contiene una unidad de polímero, opcionalmente una unidad sacárido, opcionalmente una unidad carboxilo y combinaciones de las mismas; y (c) opcionalmente un grupo extensor que tiene un sitio de unión a un grupo de direccionamiento, en donde a— es un sitio de unión a un grupo enzimáticamente escindible; ß— es un sitio de unión a dicho por lo menos un grupo polar; ?— es H, un sitio de unión a por lo menos una unidad de fármaco, o un sitio de unión a un grupo conector unido a dicha por lo menos una unidad de fármaco; y la unidad de polímero contiene una poliamida, un poliéter o una combinación de los mismos, en donde el poliéter contiene un grupo hidroxilo, un grupo polihidroxilo, un grupo sacárido, un grupo carboxilo o combinaciones de los mismos. También se divulgan compuestos de fármaco-conector y conjugados formados a partir de compuestos conectores, así como composiciones farmacéuticas y métodos relacionados
CL2025002018A 2023-01-11 2025-07-08 Conectores, conectores-fármaco, conjugados de los mismos y métodos para su uso. CL2025002018A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2023071778 2023-01-11

Publications (1)

Publication Number Publication Date
CL2025002018A1 true CL2025002018A1 (es) 2025-10-03

Family

ID=91897796

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2025002018A CL2025002018A1 (es) 2023-01-11 2025-07-08 Conectores, conectores-fármaco, conjugados de los mismos y métodos para su uso.

Country Status (13)

Country Link
US (1) US20260034238A1 (es)
EP (1) EP4648800A1 (es)
JP (1) JP2026504840A (es)
KR (1) KR20250133764A (es)
CN (1) CN120882431A (es)
AU (1) AU2024207684A1 (es)
CL (1) CL2025002018A1 (es)
CO (1) CO2025010841A2 (es)
IL (1) IL321864A (es)
MX (1) MX2025007838A (es)
PE (1) PE20252394A1 (es)
TW (1) TW202434223A (es)
WO (1) WO2024149345A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025064521A1 (en) 2023-09-18 2025-03-27 Profoundbio Us Co. Ultrafiltration / diafiltration purification methods
WO2026032411A1 (en) * 2024-08-09 2026-02-12 Beone Guangzhou Biologics Manufacturing Co., Ltd. Self-stabilizing linker conjugates

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015038426A1 (en) * 2013-09-13 2015-03-19 Asana Biosciences, Llc Self-immolative linkers containing mandelic acid derivatives, drug-ligand conjugates for targeted therapies and uses thereof
EP3230282A1 (en) * 2014-12-09 2017-10-18 AbbVie Inc. Bcl xl inhibitory compounds having low cell permeability and antibody drug conjugates including the same
US11135307B2 (en) * 2016-11-23 2021-10-05 Mersana Therapeutics, Inc. Peptide-containing linkers for antibody-drug conjugates
EP3717021A1 (en) * 2017-11-27 2020-10-07 Mersana Therapeutics, Inc. Pyrrolobenzodiazepine antibody conjugates
EP3727463A1 (en) * 2017-12-21 2020-10-28 Mersana Therapeutics, Inc. Pyrrolobenzodiazepine antibody conjugates
CA3101601A1 (en) * 2018-05-29 2019-12-05 Bristol-Myers Squibb Company Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making
CN113853219B (zh) * 2019-05-20 2025-01-07 诺华股份有限公司 具有包含亲水性基团的接头的抗体药物缀合物
WO2022207699A1 (en) * 2021-03-30 2022-10-06 Mablink Bioscience Enzyme-triggered self-reacting linker having improved physicochemical and pharmacological properties
JP2024522389A (ja) * 2021-04-29 2024-06-19 ハイスリンク セラピューティクス 抗体薬物複合体の調製方法および使用
TW202320857A (zh) * 2021-07-06 2023-06-01 美商普方生物製藥美國公司 連接子、藥物連接子及其結合物及其使用方法

Also Published As

Publication number Publication date
WO2024149345A1 (en) 2024-07-18
JP2026504840A (ja) 2026-02-10
PE20252394A1 (es) 2025-10-10
AU2024207684A1 (en) 2025-07-03
IL321864A (en) 2025-08-01
US20260034238A1 (en) 2026-02-05
TW202434223A (zh) 2024-09-01
CN120882431A (zh) 2025-10-31
CO2025010841A2 (es) 2025-11-19
MX2025007838A (es) 2025-08-01
KR20250133764A (ko) 2025-09-08
EP4648800A1 (en) 2025-11-19

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