EA201400237A1 - Фолатные конъюгаты альбуминсвязывающих частиц - Google Patents

Фолатные конъюгаты альбуминсвязывающих частиц

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Publication number
EA201400237A1
EA201400237A1 EA201400237A EA201400237A EA201400237A1 EA 201400237 A1 EA201400237 A1 EA 201400237A1 EA 201400237 A EA201400237 A EA 201400237A EA 201400237 A EA201400237 A EA 201400237A EA 201400237 A1 EA201400237 A1 EA 201400237A1
Authority
EA
Eurasian Patent Office
Prior art keywords
folated
albumins
conjugates
radionuclide
diagnostic
Prior art date
Application number
EA201400237A
Other languages
English (en)
Inventor
Роже Шибли
Рудольф Мозер
Кристина Магдалена Мюллер
Харриет Стратерз
Виола Грён
Симон Менсах Аметамей
Синди Рамона Фишер
Original Assignee
Мерк Э Сие
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 Мерк Э Сие filed Critical Мерк Э Сие
Publication of EA201400237A1 publication Critical patent/EA201400237A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • 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
    • A61K47/551—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 one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • 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
    • A61K51/041—Heterocyclic compounds
    • A61K51/0472—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • C07K5/0215—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing natural amino acids, forming a peptide bond via their side chain functional group, e.g. epsilon-Lys, gamma-Glu
    • 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
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/569—Immunoassay; Biospecific binding assay; Materials therefor for microorganisms, e.g. protozoa, bacteria, viruses
    • G01N33/56966—Animal cells
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Optics & Photonics (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Cell Biology (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Pathology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Zoology (AREA)
  • Virology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)

Abstract

Настоящее изобретение относится к новым трехфункциональным фолатным конъюгатам, содержащим фолат, альбуминовое связующее и терапевтическую или диагностическую часть на основе радионуклида, а также к их фармацевтическим композициям, к способу их получения и к их применению для диагностических и терапевтических применений в медицине, таких как диагностическая радионуклидная визуализация и радионуклидная терапия.
EA201400237A 2011-08-17 2012-08-10 Фолатные конъюгаты альбуминсвязывающих частиц EA201400237A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11177732 2011-08-17
PCT/EP2012/065702 WO2013024035A1 (en) 2011-08-17 2012-08-10 Folate conjugates of albumin-binding entities

Publications (1)

Publication Number Publication Date
EA201400237A1 true EA201400237A1 (ru) 2014-08-29

Family

ID=46650547

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201400237A EA201400237A1 (ru) 2011-08-17 2012-08-10 Фолатные конъюгаты альбуминсвязывающих частиц

Country Status (17)

Country Link
US (1) US9295739B2 (ru)
EP (1) EP2766364B1 (ru)
JP (1) JP6152104B2 (ru)
KR (1) KR102036199B1 (ru)
CN (1) CN103732595B (ru)
AU (1) AU2012296937B2 (ru)
CA (1) CA2839647C (ru)
DK (1) DK2766364T3 (ru)
EA (1) EA201400237A1 (ru)
ES (1) ES2990974T3 (ru)
FI (1) FI2766364T3 (ru)
HU (1) HUE068833T2 (ru)
IL (1) IL230758B (ru)
PL (1) PL2766364T3 (ru)
PT (1) PT2766364T (ru)
WO (1) WO2013024035A1 (ru)
ZA (1) ZA201400174B (ru)

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PT2776382T (pt) * 2011-08-22 2018-12-24 Merck & Cie Folatos de 18f-sacárido
GB201417067D0 (en) * 2014-09-26 2014-11-12 South African Nuclear Energy Radiopharmaceutical conjugate
CN104897627B (zh) * 2015-02-04 2017-07-11 浙江工商大学 一种基于分子识别的荧光检测叶酸的方法
US20180110871A1 (en) * 2015-04-17 2018-04-26 Endocyte, Inc. Dual disulfide drug conjugates
AR105911A1 (es) 2015-09-03 2017-11-22 Forma Therapeutics Inc Inhibidores de hdac8 bicíclicos fusionados [6,6]
AU2017234676A1 (en) 2016-03-16 2018-09-20 Purdue Research Foundation Carbonic anhydrase IX targeting agents and methods
WO2017161144A1 (en) * 2016-03-16 2017-09-21 Endocyte, Inc. Carbonic anhydrase ix inhibitor conjugates and uses thereof
US10806806B2 (en) 2016-06-23 2020-10-20 Cornell University Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies
CN109843339B (zh) 2016-06-23 2023-07-07 康奈尔大学 影响肿瘤杀伤的双重靶向构建体
AU2017311510B2 (en) 2016-08-10 2021-11-18 Cancer Targeted Technology Llc Chelated PSMA inhibitors
EP3609541A4 (en) * 2017-04-05 2021-04-07 Cornell University Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies
WO2018233798A1 (en) 2017-06-20 2018-12-27 ITM Isotopen Technologien München AG Novel psma-binding agents and uses thereof
CA3060143A1 (en) 2017-05-24 2018-11-29 Itm Isotopen Technologien Munchen Ag Novel psma-binding agents and uses thereof
CN111372940A (zh) * 2017-09-19 2020-07-03 阿尔伯塔大学理事会 生物还原活化的化合物、其前药、放射性药物、组合物及其在包括癌症在内的低氧疾病的多模式治疗控制中的应用
CN112409436B (zh) * 2020-11-06 2022-02-18 厦门大学 一种放射性核素标记的雌激素受体分子靶向化合物及其应用
WO2024025845A1 (en) * 2022-07-25 2024-02-01 Sorrento Therapeutics, Inc. Folate-conjugated drugs and uses thereof
CN119855612A (zh) * 2022-09-09 2025-04-18 同宜医药（苏州）有限公司 放射性核素偶联药物及其药物组合物和应用
WO2025171887A1 (en) 2024-02-16 2025-08-21 Paul Scherrer Institut Radiolabeled complexes and pharmaceutical compositions including the same

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4136159A (en) 1977-02-28 1979-01-23 New England Nuclear Corporation Radioassay of folates
US5688488A (en) 1989-04-03 1997-11-18 Purdue Research Foundation Composition and method for tumor imaging
US5919934A (en) 1997-02-19 1999-07-06 The George Washington University Compounds, compositions, and methods for cancer imaging and therapy
US6093382A (en) 1998-05-16 2000-07-25 Bracco Research Usa Inc. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
US7067111B1 (en) 1999-10-25 2006-06-27 Board Of Regents, University Of Texas System Ethylenedicysteine (EC)-drug conjugates, compositions and methods for tissue specific disease imaging
JP4801348B2 (ja) 2002-05-06 2011-10-26 エンドサイト，インコーポレイテッド ビタミンを標的とした造影剤
JP4638225B2 (ja) 2002-05-30 2011-02-23 ザ スクリプス リサーチ インスティテュート 銅を触媒とするアジドとアセチレンのライゲーション
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US8926945B2 (en) * 2005-10-07 2015-01-06 Guerbet Compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium
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WO2008125618A1 (en) * 2007-04-11 2008-10-23 Merck Eprova Ag Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy
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Also Published As

Publication number Publication date
JP6152104B2 (ja) 2017-06-21
IL230758A0 (en) 2014-03-31
IL230758B (en) 2020-11-30
PT2766364T (pt) 2024-09-24
JP2014531407A (ja) 2014-11-27
EP2766364B1 (en) 2024-07-31
KR102036199B1 (ko) 2019-10-24
US20140234216A1 (en) 2014-08-21
CA2839647C (en) 2022-08-16
PL2766364T3 (pl) 2024-12-16
KR20140052027A (ko) 2014-05-02
ES2990974T3 (es) 2024-12-02
AU2012296937B2 (en) 2017-10-12
FI2766364T3 (fi) 2024-10-23
WO2013024035A1 (en) 2013-02-21
CN103732595A (zh) 2014-04-16
CA2839647A1 (en) 2013-02-21
AU2012296937A1 (en) 2014-02-20
EP2766364A1 (en) 2014-08-20
DK2766364T3 (da) 2024-09-30
CN103732595B (zh) 2017-02-08
ZA201400174B (en) 2015-09-30
HUE068833T2 (hu) 2025-01-28
US9295739B2 (en) 2016-03-29

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