CN116234582A - GalNAc和皂苷的缀合物、包含所述缀合物和GalNAc-寡核苷酸缀合物的治疗性组合物 - Google Patents

GalNAc和皂苷的缀合物、包含所述缀合物和GalNAc-寡核苷酸缀合物的治疗性组合物 Download PDF

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Publication number
CN116234582A
CN116234582A CN202180051254.4A CN202180051254A CN116234582A CN 116234582 A CN116234582 A CN 116234582A CN 202180051254 A CN202180051254 A CN 202180051254A CN 116234582 A CN116234582 A CN 116234582A
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saponin
galnac
conjugate
xyl
rha
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Pending
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CN202180051254.4A
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English (en)
Chinese (zh)
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鲁本·波斯特尔
盖伊·赫尔曼斯
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Saprami Technology Co ltd
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Saprami Technology Co ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=85176234&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN116234582(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Saprami Technology Co ltd filed Critical Saprami Technology Co ltd
Priority to CN202510833809.0A priority Critical patent/CN120586078A/zh
Priority claimed from PCT/NL2021/050384 external-priority patent/WO2021261992A1/en
Publication of CN116234582A publication Critical patent/CN116234582A/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
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • 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
    • 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
    • A61K47/554—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 a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Molecular Biology (AREA)
  • Biochemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
CN202180051254.4A 2020-06-24 2021-06-18 GalNAc和皂苷的缀合物、包含所述缀合物和GalNAc-寡核苷酸缀合物的治疗性组合物 Pending CN116234582A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202510833809.0A CN120586078A (zh) 2020-06-24 2021-06-18 GalNAc和皂苷的缀合物、包含所述缀合物和GalNAc-寡核苷酸缀合物的治疗性组合物

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
NL2025899 2020-06-24
NL2025899 2020-06-24
NL2026442 2020-09-10
NL2026442 2020-09-10
PCT/NL2021/050384 WO2021261992A1 (en) 2020-06-24 2021-06-18 Conjugate of galnac and saponin, therapeutic composition comprising said conjugate and a galnac-oligonucleotide conjugate

Related Child Applications (1)

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CN202510833809.0A Division CN120586078A (zh) 2020-06-24 2021-06-18 GalNAc和皂苷的缀合物、包含所述缀合物和GalNAc-寡核苷酸缀合物的治疗性组合物

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CN116234582A true CN116234582A (zh) 2023-06-06

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CN202180051254.4A Pending CN116234582A (zh) 2020-06-24 2021-06-18 GalNAc和皂苷的缀合物、包含所述缀合物和GalNAc-寡核苷酸缀合物的治疗性组合物
CN202510833809.0A Pending CN120586078A (zh) 2020-06-24 2021-06-18 GalNAc和皂苷的缀合物、包含所述缀合物和GalNAc-寡核苷酸缀合物的治疗性组合物

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US (1) US20230263897A1 (https=)
EP (2) EP4438125A3 (https=)
JP (1) JP2023532040A (https=)
KR (1) KR20230043114A (https=)
CN (2) CN116234582A (https=)
AU (1) AU2021295358B2 (https=)
CA (1) CA3183885A1 (https=)
ES (1) ES3002193T3 (https=)
IL (1) IL299357A (https=)
MX (1) MX2023000092A (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114072503A (zh) * 2019-07-02 2022-02-18 阿尔戈诺特Rna有限公司 载脂蛋白b拮抗剂
CN116655715A (zh) * 2023-07-27 2023-08-29 北京炫景瑞医药科技有限公司 一种GalNAc衍生物、缀合物、组合物以及它们的用途
CN116854754A (zh) * 2023-09-01 2023-10-10 北京悦康科创医药科技股份有限公司 一种含有核糖环或其衍生结构的GalNAc化合物及其寡核苷酸缀合物
WO2025016444A1 (en) * 2023-07-20 2025-01-23 Shanghai Argo Biopharmaceutical Co., Ltd. Compositions and methods for inhibiting expression of pd-l1

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025090612A1 (en) * 2023-10-27 2025-05-01 Wisconsin Alumni Research Foundation Lipid nanoparticles formed by lipidoids for efficient delivery of nucleotide drugs and biologics

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CN105378082A (zh) * 2013-05-01 2016-03-02 Isis制药公司 组合物和方法
WO2020126600A1 (en) * 2018-12-21 2020-06-25 Sapreme Technologies B.V. Antibody-drug conjugate with improved therapeutic window

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EP1623715B1 (en) * 2004-07-13 2012-09-19 Charité - Universitätsmedizin Berlin A composition comprising a pharmacologically active agent coupled to a target cell specific component, and a saponin
WO2008007941A1 (en) * 2006-07-10 2008-01-17 Vereniging Voor Christelijk Wetenschappelijk Onderwijs Gainac specific binding molecules and uses thereof
WO2011054811A1 (en) 2009-11-03 2011-05-12 Santaris Pharma A/S Rna antagonists targeting hsp27 combination therapy
WO2011141703A1 (en) * 2010-05-12 2011-11-17 Protiva Biotherapeutics Inc. Compositions and methods for silencing apolipoprotein b
CA2800911A1 (en) * 2010-06-11 2011-12-15 University Of Georgia Research Foundation, Inc. Immunogenic vaccine
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AR100516A1 (es) * 2014-05-19 2016-10-12 Pfizer Compuestos de 6,8-dioxabiciclo[3.2.1]octano-2,3-diol sustituidos como agentes de direccionamiento al asgpr
CN106795200B (zh) * 2014-10-10 2020-06-19 豪夫迈·罗氏有限公司 Galnac亚磷酰胺、其核酸缀合物及其用途
EP3514240A1 (en) * 2018-01-18 2019-07-24 Freie Universität Berlin Novel uses of a saponin and method for its isolation

Patent Citations (3)

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CN105378082A (zh) * 2013-05-01 2016-03-02 Isis制药公司 组合物和方法
WO2020126600A1 (en) * 2018-12-21 2020-06-25 Sapreme Technologies B.V. Antibody-drug conjugate with improved therapeutic window
CN113453722A (zh) * 2018-12-21 2021-09-28 萨普雷米科技有限公司 改良的细胞靶向结合分子

Non-Patent Citations (8)

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ALEXANDER WENG 等: "The toxin component of targeted anti-tumor toxins determines their efficacy increase by saponins", MOLECULAR ONCOLOGY, vol. 6, 31 December 2012 (2012-12-31), pages 323 - 332 *
BACHRAN CHRISTOPHER 等: "Saponins in Tumor Therapy", MINI REVIEWS IN MEDICINAL CHEMISTRY, vol. 8, no. 6, 31 December 2002 (2002-12-31), pages 575 - 584 *
CHEENU BHARGAVA 等: "Targeted dianthin is a powerful toxin to treat pancreatic carcinoma when applied in combination with the glycosylated triterpene SO1861", MOLECULAR ONCOLOGY, vol. 11, 31 December 2017 (2017-12-31), pages 1527 *
HENDRIK FUCHS 等: "Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies", BIOMEDICINES, vol. 5, no. 14, 29 March 2017 (2017-03-29), pages 1 - 25 *
ROGER GILABERT-ORIOL 等: "Combinatorial approach to increase efficacy of Cetuximab, Panitumumab and Trastuzumab by dianthin conjugation and co-application of SO1861", BIOCHEMICAL PHARMACOLOGY, vol. 97, 31 December 2015 (2015-12-31), pages 247 *
ROGER GILABERT-ORIOL 等: "Dianthin-30 or gelonin versus monomethyl auristatin E, each configured with an anti-calcitonin receptor antibody, are differentially potent in vitro in high-grade glioma cell lines derived from glioblastoma", CANCER IMMUNOLOGY, IMMUNOTHERAPY, vol. 66, 13 March 2017 (2017-03-13), pages 1217 *
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SABINE SEWING 等: "GalNAc Conjugation Attenuates the Cytotoxicity of Antisense Oligonucleotide Drugs in Renal Tubular Cells", MOLECULAR THERAPY: NUCLEIC ACIDS, vol. 14, 31 March 2019 (2019-03-31), pages 67 - 79 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114072503A (zh) * 2019-07-02 2022-02-18 阿尔戈诺特Rna有限公司 载脂蛋白b拮抗剂
WO2025016444A1 (en) * 2023-07-20 2025-01-23 Shanghai Argo Biopharmaceutical Co., Ltd. Compositions and methods for inhibiting expression of pd-l1
CN116655715A (zh) * 2023-07-27 2023-08-29 北京炫景瑞医药科技有限公司 一种GalNAc衍生物、缀合物、组合物以及它们的用途
CN116655715B (zh) * 2023-07-27 2023-10-20 北京炫景瑞医药科技有限公司 一种GalNAc衍生物、缀合物、组合物以及它们的用途
CN116854754A (zh) * 2023-09-01 2023-10-10 北京悦康科创医药科技股份有限公司 一种含有核糖环或其衍生结构的GalNAc化合物及其寡核苷酸缀合物
CN116854754B (zh) * 2023-09-01 2023-12-12 北京悦康科创医药科技股份有限公司 一种含有核糖环或其衍生结构的GalNAc化合物及其寡核苷酸缀合物

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ES3002193T3 (en) 2025-03-06
AU2021295358A9 (en) 2023-06-29
EP4171641A1 (en) 2023-05-03
EP4171641B1 (en) 2024-10-30
JP2023532040A (ja) 2023-07-26
EP4438125A3 (en) 2024-12-25
US20230263897A1 (en) 2023-08-24
AU2021295358A1 (en) 2023-02-16
IL299357A (en) 2023-02-01
EP4438125A2 (en) 2024-10-02
KR20230043114A (ko) 2023-03-30
AU2021295358B2 (en) 2026-01-22
CN120586078A (zh) 2025-09-05
CA3183885A1 (en) 2021-12-30
EP4171641C0 (en) 2024-10-30
MX2023000092A (es) 2023-04-20

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