AU2012252024B2 - Pretargeting kit for imaging or therapy comprising a trans - cyclooctene dienophile and a diene - Google Patents

Pretargeting kit for imaging or therapy comprising a trans - cyclooctene dienophile and a diene Download PDF

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Publication number
AU2012252024B2
AU2012252024B2 AU2012252024A AU2012252024A AU2012252024B2 AU 2012252024 B2 AU2012252024 B2 AU 2012252024B2 AU 2012252024 A AU2012252024 A AU 2012252024A AU 2012252024 A AU2012252024 A AU 2012252024A AU 2012252024 B2 AU2012252024 B2 AU 2012252024B2
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Australia
Prior art keywords
alkyl
aryl
group
probe
independently
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AU2012252024A
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AU2012252024A1 (en
Inventor
Johan Lub
Marc Stefan Robillard
Raffaella Rossin
Sandra Martina Van Den Bosch
Ronny Mathieu Versteegen
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Tagworks Pharmaceuticals BV
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Tagworks Pharmaceuticals BV
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Classifications

    • 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
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • 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
    • A61K47/6891—Pre-targeting systems involving an antibody for targeting specific cells
    • A61K47/6897—Pre-targeting systems with two or three steps using antibody conjugates; Ligand-antiligand therapies
    • 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
    • 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
    • A61K51/0495—Pretargeting
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/02—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • A61K49/101—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals
    • A61K49/106—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals the complex-forming compound being cyclic, e.g. DOTA

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Nanotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nuclear Medicine (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
AU2012252024A 2011-05-09 2012-05-07 Pretargeting kit for imaging or therapy comprising a trans - cyclooctene dienophile and a diene Active AU2012252024B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11165267A EP2522369A1 (en) 2011-05-09 2011-05-09 Pretargeting kit, method and agents used therein
EP11165267.3 2011-05-09
PCT/IB2012/052260 WO2012153254A1 (en) 2011-05-09 2012-05-07 Pretargeting kit for imaging or therapy comprising a trans - cyclooctene dienophile and a diene

Publications (2)

Publication Number Publication Date
AU2012252024A1 AU2012252024A1 (en) 2014-01-09
AU2012252024B2 true AU2012252024B2 (en) 2017-06-29

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012252024A Active AU2012252024B2 (en) 2011-05-09 2012-05-07 Pretargeting kit for imaging or therapy comprising a trans - cyclooctene dienophile and a diene

Country Status (7)

Country Link
US (1) US9913921B2 (enExample)
EP (2) EP2522369A1 (enExample)
JP (1) JP6223962B2 (enExample)
CN (1) CN103648533B (enExample)
AU (1) AU2012252024B2 (enExample)
CA (1) CA2835298C (enExample)
WO (1) WO2012153254A1 (enExample)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6215194B2 (ja) 2011-05-16 2017-10-18 コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． 生体直交型薬物活性化
EP2948186A4 (en) * 2013-01-25 2016-10-05 Sloan Kettering Inst Cancer TETRAZINE / TRANSCYCLOOKTENE IN SOLID PHASE SYNTHESIS MARKED PEPTIDE
CN105611914B (zh) * 2013-06-19 2020-09-08 加利福尼亚大学董事会 局部递送治疗剂的化学构造物
US20160346409A1 (en) * 2014-02-10 2016-12-01 Mcmaster University Targeted molecular imaging contrast agents
CN106659796B (zh) * 2014-03-14 2021-04-30 加利福尼亚大学董事会 Tco缀合物和治疗剂递送方法
EP3125866B1 (en) * 2014-04-04 2021-03-03 President and Fellows of Harvard College Refillable drug delivery devices and methods of use thereof
US10179775B2 (en) 2014-08-11 2019-01-15 The General Hospital Corporation Cyclooctenes for bioorthogonol reactions
WO2016164565A1 (en) * 2015-04-08 2016-10-13 University Of Delaware Trans-cycloheptenes and hetero-trans-cycloheptenes for bioorthogonal coupling
WO2017031084A1 (en) 2015-08-14 2017-02-23 The Regents Of The University Of California Poly(vinyl alcohol) nanocarriers
CN117567535A (zh) 2015-09-10 2024-02-20 坦伯公司 生物正交组合物
US11690825B2 (en) 2016-03-09 2023-07-04 Board Of Regents, The University Of Texas System 20-HETE receptor (GPR75) antagonists and methods of use
WO2018004338A1 (en) 2016-06-27 2018-01-04 Tagworks Pharmaceuticals B.V. Cleavable tetrazine used in bio-orthogonal drug activation
ES2983582T3 (es) 2017-04-07 2024-10-23 Tambo Inc Composiciones bioortogonales
US11560384B2 (en) 2017-05-04 2023-01-24 University Of Utah Research Foundation Benzonorbornadiene derivatives and reactions thereof
CN107746367B (zh) * 2017-11-07 2020-05-26 清华大学 β-石竹烯衍生物及其制备方法与应用
WO2019227490A1 (en) 2018-06-01 2019-12-05 Tayu Huaxia Biotech Medical Group Co., Ltd. Compositions and methods for imaging
JP7554178B2 (ja) * 2018-07-26 2024-09-19 タユー ファシャ バイオテック メディカル グループ カンパニー， リミテッド イメージングのための組成物および方法
EP3853234B1 (en) 2018-09-18 2025-04-23 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
CN119823023A (zh) 2018-10-10 2025-04-15 坦博公司 制备官能化环辛烯的工艺
IL289095A (en) 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Activating components to cleave labels from biomolecules in vivo
CN110954514B (zh) * 2019-12-02 2022-06-21 上海交通大学 适用于研究脂质体体内外分布的荧光示踪系统和方法
WO2022038183A1 (en) 2020-08-18 2022-02-24 Rigshospitalet Extracorporeal clearing traps based on inverse electron demand diels-alder cycloaddition for (pre)-targeted therapy and diagnostics
CA3239713A1 (en) * 2021-12-08 2023-06-15 Edward A. LEMKE Hydrophilic tetrazine-functionalized payloads for preparation of targeting conjugates
KR20250141267A (ko) * 2023-02-15 2025-09-26 태그웍스 파마슈티컬스 비.브이. 개선된 특성을 가지는 테트라진
CN118546131B (zh) * 2024-05-10 2025-02-28 四川大学华西医院 四嗪聚集诱导发光探针前体、探针及其制备方法、应用
CN119746111A (zh) * 2024-12-04 2025-04-04 苏州大学 一种体内放射性标记降低肝脏辐射剂量的试剂及其应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010051530A2 (en) * 2008-10-31 2010-05-06 The General Hospital Corporation Compositions and methods for delivering a substance to a biological target
WO2010119389A2 (en) * 2009-04-16 2010-10-21 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
WO2011095336A2 (en) * 2010-02-03 2011-08-11 Deutsches Krebsforschungszentrum Post-synthetic modification of nucleic acids by inverse diels-alder reaction
WO2012049624A1 (en) * 2010-10-14 2012-04-19 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
US20130266512A1 (en) * 2010-07-23 2013-10-10 University Of Southern California Tetrazine-trans-cyclooctene Ligation for the Rapid Construction of Radionuclide Labeled Probes

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3143578A (en) * 1962-12-28 1964-08-04 Union Carbide Corp Preparation of tricyclo [8.2.1.02.9] trideca-5, 11-diene
US4741900A (en) 1982-11-16 1988-05-03 Cytogen Corporation Antibody-metal ion complexes
US5326856A (en) 1992-04-09 1994-07-05 Cytogen Corporation Bifunctional isothiocyanate derived thiocarbonyls as ligands for metal binding
US20030129191A1 (en) 1992-12-23 2003-07-10 Neorx Corporation Pretargeting methods and compounds
ATE391713T1 (de) * 2001-12-05 2008-04-15 California Inst Of Techn Enantioseletive umwandlung von alpha,beta- ungesättigten ketonen unter verwendung chiraler organischer katalysatoren
US8236949B2 (en) * 2007-07-17 2012-08-07 University Of Delaware Tetrazine-based bio-orthogonal coupling reagents and methods
RU2011146362A (ru) * 2009-04-16 2013-05-27 Конинклейке Филипс Электроникс Н.В. Набор для предварительного таргетинга, способ и средства, используемые в нем

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010051530A2 (en) * 2008-10-31 2010-05-06 The General Hospital Corporation Compositions and methods for delivering a substance to a biological target
WO2010119389A2 (en) * 2009-04-16 2010-10-21 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
WO2011095336A2 (en) * 2010-02-03 2011-08-11 Deutsches Krebsforschungszentrum Post-synthetic modification of nucleic acids by inverse diels-alder reaction
US20130266512A1 (en) * 2010-07-23 2013-10-10 University Of Southern California Tetrazine-trans-cyclooctene Ligation for the Rapid Construction of Radionuclide Labeled Probes
WO2012049624A1 (en) * 2010-10-14 2012-04-19 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
BLACKMAN, M.L. et al. "The Tetrazine Ligation: Fast Bioconjugation based on Inverse-electron-demand Diels-Alder Reactivity", J. American Chemical Society,2008, 130, 13518-13519 *
KELIHER, E. J. et al., "High-Yielding, Two-Step 18F Labeling Strategy for 18F-PARP1 Inhibitors", CHEMMEDCHEM vol. 6, no. 3, 7 March 2011, pages 424-427 *
ROSSIN, R. et al. "In vivo chemistry for pretargeted tumor imaging in live mice", Angewandte Chemie International Edition, 2010, 49, 3375-33 *
SELVARAJ, R. et al., Bioorganic & Medicinal Chemistry Letters, vol. 21, no. 17, 2011, pages 5011-5014 *
TAYLOR, M.T. et al., "Design and Synthesis of Highly Reactive Dienophiles for the Tetrazine-trans-Cyclooctene Ligation", Journal Of The American Chemical Society, vol. 133, no. 25, 29 June 2011, pages 9646-9649 *

Also Published As

Publication number Publication date
US20140093450A1 (en) 2014-04-03
EP2707035B1 (en) 2020-04-01
US9913921B2 (en) 2018-03-13
EP2522369A1 (en) 2012-11-14
EP2707035A1 (en) 2014-03-19
JP2014518861A (ja) 2014-08-07
CA2835298C (en) 2019-06-18
WO2012153254A1 (en) 2012-11-15
CN103648533A (zh) 2014-03-19
JP6223962B2 (ja) 2017-11-01
CA2835298A1 (en) 2012-11-15
AU2012252024A1 (en) 2014-01-09
CN103648533B (zh) 2017-09-08

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Owner name: TAGWORKS PHARMACEUTICALS B.V.

Free format text: FORMER OWNER(S): KONINKLIJKE PHILIPS N.V.