CN109312004A - 包含赖氨酸-脲-谷氨酸药效团的改性右旋糖酐缀合物 - Google Patents

包含赖氨酸-脲-谷氨酸药效团的改性右旋糖酐缀合物 Download PDF

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Publication number
CN109312004A
CN109312004A CN201780038758.6A CN201780038758A CN109312004A CN 109312004 A CN109312004 A CN 109312004A CN 201780038758 A CN201780038758 A CN 201780038758A CN 109312004 A CN109312004 A CN 109312004A
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conjugate
modified dextrans
cancer
psma
dextran
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Chinese (zh)
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A.R.霍姆伯格
S.尼尔森
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Dextech Medical AB
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Dextech Medical AB
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/06—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
    • A61K51/065—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules conjugates with carriers being macromolecules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0491—Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • 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
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
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    • 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
    • A61K47/547—Chelates, e.g. Gd-DOTA or Zinc-amino acid chelates; Chelate-forming compounds, e.g. DOTA or ethylenediamine being covalently linked or complexed to the pharmacologically- or therapeutically-active agent
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61K47/6869—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 a cell of the reproductive system: ovaria, uterus, testes, prostate
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    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
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    • A61K51/06—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
    • A61K51/121—Solutions, i.e. homogeneous liquid formulation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/0006—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
    • C08B37/0009—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
    • C08B37/0021—Dextran, i.e. (alpha-1,4)-D-glucan; Derivatives thereof, e.g. Sephadex, i.e. crosslinked dextran

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Inorganic Chemistry (AREA)
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  • Reproductive Health (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
CN201780038758.6A 2016-06-22 2017-06-19 包含赖氨酸-脲-谷氨酸药效团的改性右旋糖酐缀合物 Pending CN109312004A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FI20165515A FI127538B (en) 2016-06-22 2016-06-22 MODIFIED Dextran Conjugates
FI20165515 2016-06-22
PCT/EP2017/064929 WO2017220488A1 (en) 2016-06-22 2017-06-19 Modified dextran conjugates comprising a lysine-urea-glutamate pharmacophore

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CN109312004A true CN109312004A (zh) 2019-02-05

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US (1) US20190175767A1 (enExample)
EP (1) EP3475311B1 (enExample)
JP (1) JP6944720B2 (enExample)
CN (1) CN109312004A (enExample)
AU (1) AU2017283151A1 (enExample)
CA (1) CA3027920C (enExample)
FI (1) FI127538B (enExample)
IL (1) IL263886B2 (enExample)
WO (1) WO2017220488A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112209970A (zh) * 2020-10-21 2021-01-12 北京师范大学 一种锝-99m标记含异腈的谷氨酸-脲衍生物的制备方法和应用
CN113573744A (zh) * 2019-03-19 2021-10-29 纳米疗法股份有限公司 制备螯合放射性同位素的且其表面被靶向psma受体的特异性分子修饰的聚合物纳米颗粒的方法及其用途
WO2024199442A1 (en) * 2023-03-30 2024-10-03 Genequantum Healthcare (Suzhou) Co., Ltd. Disaccharide linker, linker-payload containing the same and glycan chain-remodeled antibody-drug conjugate, preparation method and uses thereof

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PL240772B1 (pl) * 2018-06-11 2022-06-06 Nanothea Spolka Akcyjna Sposób wytwarzania nanocząstek polimerowych chelatujących izotopy promieniotwórcze do zastosowania w diagnostyce i terapii
EP3636635A1 (en) 2018-10-11 2020-04-15 Academisch Ziekenhuis Leiden h.o.d.n. LUMC Imaging agents
EP3923997A1 (en) * 2019-02-14 2021-12-22 Deutsches Krebsforschungszentrum Prostate specific membrane antigen (psma) ligands comprising an amylase cleavable linker

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CN101678121A (zh) * 2007-03-07 2010-03-24 德克斯特克医疗公司 对肿瘤细胞具有杀伤作用的改性羟基聚合物共轭物
CN101778910A (zh) * 2006-11-08 2010-07-14 分子制药洞察公司 谷氨酸的异质二聚体
CN101990442A (zh) * 2008-04-07 2011-03-23 德克斯特克医疗公司 具有亲骨部分和肿瘤杀伤部分的改性羟基聚合物缀合物
WO2014127365A1 (en) * 2013-02-15 2014-08-21 Case Western Reserve University Psma ligands and uses thereof
CN104203942A (zh) * 2011-11-30 2014-12-10 约翰霍普金斯大学 前列腺特异性膜抗原(psma)的同源多价抑制剂和异源多价抑制剂以及其用途
WO2015058151A2 (en) * 2013-10-18 2015-04-23 Molecular Insight Pharmaceuticals, Inc. Methods of using spect/ct analysis for staging cancer
CN104797247A (zh) * 2012-11-15 2015-07-22 恩多塞特公司 用于治疗由psma表达细胞引起的疾病的共轭物
EP3011976A1 (en) * 2014-10-20 2016-04-27 Deutsches Krebsforschungszentrum 18F-tagged inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents

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SE9803482D0 (sv) 1998-10-13 1998-10-13 Anders Holmberg Ion exchange tumor targeting (IETT)
EP2921482B1 (en) * 2007-06-26 2018-09-05 The Johns Hopkins University Labeled inhibitors of prostate-specific membrane antigen (psma), biological evaluation, and use as imaging agents
JP5843338B2 (ja) * 2011-08-05 2016-01-13 モレキュラ インサイト ファーマシューティカルズ インコーポレイテッド 放射標識された前立腺特異的膜抗原阻害剤
CN106660943B (zh) * 2014-05-06 2020-03-17 约翰霍普金斯大学 用于psma靶向的成像和放射疗法的金属/放射性金属标记的psma抑制物

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US4822594A (en) * 1987-01-27 1989-04-18 Gibby Wendell A Contrast enhancing agents for magnetic resonance images
CN101778910A (zh) * 2006-11-08 2010-07-14 分子制药洞察公司 谷氨酸的异质二聚体
CN101678121A (zh) * 2007-03-07 2010-03-24 德克斯特克医疗公司 对肿瘤细胞具有杀伤作用的改性羟基聚合物共轭物
CN101990442A (zh) * 2008-04-07 2011-03-23 德克斯特克医疗公司 具有亲骨部分和肿瘤杀伤部分的改性羟基聚合物缀合物
CN104203942A (zh) * 2011-11-30 2014-12-10 约翰霍普金斯大学 前列腺特异性膜抗原(psma)的同源多价抑制剂和异源多价抑制剂以及其用途
CN104797247A (zh) * 2012-11-15 2015-07-22 恩多塞特公司 用于治疗由psma表达细胞引起的疾病的共轭物
WO2014127365A1 (en) * 2013-02-15 2014-08-21 Case Western Reserve University Psma ligands and uses thereof
WO2015058151A2 (en) * 2013-10-18 2015-04-23 Molecular Insight Pharmaceuticals, Inc. Methods of using spect/ct analysis for staging cancer
EP3011976A1 (en) * 2014-10-20 2016-04-27 Deutsches Krebsforschungszentrum 18F-tagged inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113573744A (zh) * 2019-03-19 2021-10-29 纳米疗法股份有限公司 制备螯合放射性同位素的且其表面被靶向psma受体的特异性分子修饰的聚合物纳米颗粒的方法及其用途
CN112209970A (zh) * 2020-10-21 2021-01-12 北京师范大学 一种锝-99m标记含异腈的谷氨酸-脲衍生物的制备方法和应用
WO2024199442A1 (en) * 2023-03-30 2024-10-03 Genequantum Healthcare (Suzhou) Co., Ltd. Disaccharide linker, linker-payload containing the same and glycan chain-remodeled antibody-drug conjugate, preparation method and uses thereof

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IL263886A (en) 2019-01-31
JP6944720B2 (ja) 2021-10-06
WO2017220488A1 (en) 2017-12-28
IL263886B2 (en) 2023-09-01
EP3475311A1 (en) 2019-05-01
EP3475311B1 (en) 2020-05-13
CA3027920C (en) 2023-10-17
IL263886B1 (en) 2023-05-01
FI127538B (en) 2018-08-31
JP2019527740A (ja) 2019-10-03
US20190175767A1 (en) 2019-06-13
AU2017283151A1 (en) 2018-12-06
CA3027920A1 (en) 2017-12-28
FI20165515A7 (fi) 2017-12-23

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