DK2721045T3 - Compositions, methods of synthesis and use of carbohydrate targeted agents - Google Patents

Compositions, methods of synthesis and use of carbohydrate targeted agents Download PDF

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Publication number
DK2721045T3
DK2721045T3 DK12803364.4T DK12803364T DK2721045T3 DK 2721045 T3 DK2721045 T3 DK 2721045T3 DK 12803364 T DK12803364 T DK 12803364T DK 2721045 T3 DK2721045 T3 DK 2721045T3
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cells
compound
glucose
media
linker
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DK12803364.4T
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English (en)
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Izabela Tworowska
Ebrahim S Delpassand
Jennifer Sims-Mourtada
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Radiomedix Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/0472Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/06Benzopyran radicals
    • C07H17/065Benzo[b]pyrans
    • C07H17/07Benzo[b]pyran-4-ones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0491Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0497Organic compounds conjugates with a carrier being an organic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/04Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04Heterocyclic radicals containing only oxygen as ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00Compounds containing boron, silicon, or a metal, e.g. chelates, vitamin B12
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0474Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Saccharide Compounds (AREA)

Claims (8)

1
1. Sammensætning omfattende et D02S-derivat konjugeret til en monosaccharidligand direkte eller gennem en linker og valgfrit chelateret til et metal, hvori D02S-derivatet har den følgende struktur:
hvori Ri', R2' hver uafhængigt er -OH eller -O-alkyl; Rx er et hydrogen, en linker eller en ligand; R3 er en linker og/eller en ligand; og n er et helt tal fra 1 til 10; linkeren er en aminosyre, et peptid, en aminoalkohol, en polyethylylenglycol, en alkyl, en alkenyl, en alkynyl, et azid, en aromatisk forbindelse, en carboxylsyre eller en ester, idet alkyl, alkenyl eller alkynyl valgfrit er substitueret med en alkyl, et halogen, en nitrogruppe, en hydroxylgruppe, en aminogruppe eller en carboxylgruppe; liganden er en GLUTl-targeteringsdel, hvori GLUT1-targeteringsdelen er en l'-aminosukker, en 2'-aminosukker, en l',2'-diaminosukker eller scutellarin.
2. Sammensætning ifølge krav 1 , hvori linkeren omfatter -(CH2)m-X, hvori X er en hydroxyl-, en amino- eller en carboxylgruppe, og m er et helt tal fra 1 til 10, og hvori linkeren valgfrit kan være substitueret med en alkyl, et halogen, en nitrogruppe, en hydroxylgruppe, en aminogruppe eller en carboxylgruppe.
3. Sammensætning ifølge krav 1, hvori D02S-derivatet har den følgende struktur:
4. Sammensætning ifølge krav 1, hvori D02S-derivatet yderligere omfatter et radioaktivt metal.
5. Sammensætning ifølge krav 4, hvori det radioaktive metal er 68Ga eller 177Lu.
6. Fremgangsmåde til syntese af D02S-derivatet ifølge krav 1, hvilken fremgangsmåde omfatter tilknytning af en forbindelse med den følgende struktur til en fast bærer, direkte eller gennem en linker:
hvori Ri' er -OH og R2 er -O-alkyl.
7. Fremgangsmåde ifølge krav 6, yderligere omfattende radioaktiv mærkning af D02S-derivatet med et radioaktivt metal, hvori det radioaktive metal er 68Ga eller 177Lu.
8. Sammensætning ifølge krav 1, hvori D02S-derivatet er valgt blandt de følgende:
eller
DK12803364.4T 2011-06-20 2012-06-20 Compositions, methods of synthesis and use of carbohydrate targeted agents DK2721045T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161498950P 2011-06-20 2011-06-20
PCT/US2012/043255 WO2012177701A2 (en) 2011-06-20 2012-06-20 Compositions, methods of synthesis and use of carbohydrate targeted agents

Publications (1)

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DK2721045T3 true DK2721045T3 (da) 2017-07-24

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US (1) US9550001B2 (da)
EP (1) EP2721045B1 (da)
CA (1) CA2843313C (da)
DK (1) DK2721045T3 (da)
PL (1) PL2721045T3 (da)
WO (1) WO2012177701A2 (da)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2155262A4 (en) * 2007-03-27 2012-12-19 Radiomedix Inc COMPOSITIONS FOR TARGETED THERAPIES AND IMAGERY
EP2721045B1 (en) 2011-06-20 2017-04-12 Radiomedix Inc. Compositions, methods of synthesis and use of carbohydrate targeted agents
GB201300707D0 (en) * 2013-01-15 2013-02-27 Novartis Ag Compounds and processes
US11207429B2 (en) * 2014-05-09 2021-12-28 Arizona Board Of Regents On Behalf Of The University Of Arizona Method and compositions for orally administered contrast agents for MR imaging
BR112018074716A2 (pt) 2016-06-02 2019-03-12 Sanofi conjugados de um agente farmacêutico e porção capaz de ligar-se a uma proteína sensível à glicose
GB201610738D0 (en) * 2016-06-20 2016-08-03 Ge Healthcare As Chelate compounds
EP3568205B1 (en) 2017-01-12 2023-08-16 Radiomedix Inc. Treatment of cancer cells overexpressing somatostatin receptors using ocreotide derivatives chelated to radioisotopes
CN117603148A (zh) 2017-05-05 2024-02-27 探针技术开发及商业化中心 双官能螯合物的药代动力学增强及其用途
RU2019139434A (ru) 2017-05-05 2021-06-07 Сентр фор Проуб Девелопмент энд Коммерсиализэйшн Моноклональные антитела против igf-1r и их применение
US10093741B1 (en) 2017-05-05 2018-10-09 Fusion Pharmaceuticals Inc. IGF-1R monoclonal antibodies and uses thereof
KR20200095507A (ko) 2017-12-01 2020-08-10 사노피 글루코오스 감지 단백질에 결합할 수 있는 모이어티 및 약제의 신규 접합체
RU2730507C1 (ru) * 2019-08-27 2020-08-24 Федеральное государственное бюджетное образовательное учреждение высшего образования "Московский государственный университет имени М.В. Ломоносова" (МГУ) Соединение для диагностики опухолей, экспрессирующих псма, и композиция на его основе
CN114853827B (zh) * 2022-06-02 2023-11-24 南京江原安迪科正电子研究发展有限公司 一种葡萄糖衍生配体化合物及其制备方法和应用
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

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4141654A (en) 1977-05-23 1979-02-27 James V. Massey, III Standard for calibrating and/or verifying instrument accuracy
US5648063A (en) 1981-07-24 1997-07-15 Schering Aktiengesellschaft Sterile composition comprising a chelate complex for magnetic resonance imaging
US5242679A (en) 1985-01-14 1993-09-07 Neorx Corporation Metal radionuclide labeled proteins for diagnosis and therapy
US5175343A (en) 1985-01-14 1992-12-29 Neorx Corporation Metal radionuclide labeled proteins for diagnosis and therapy
US4988496A (en) 1988-05-31 1991-01-29 Neorx Corporation Metal radionuclide chelating compounds for improved chelation kinetics
CN1033030C (zh) 1988-06-24 1996-10-16 唐化学原料公司 大环双官能螯合剂及其配合物和抗体共轭物的制备方法
US5364613A (en) 1989-04-07 1994-11-15 Sieving Paul F Polychelants containing macrocyclic chelant moieties
US5605672A (en) 1993-06-09 1997-02-25 The General Hospital Corporation Blood pool imaging composition and method of its use
FR2725382B1 (fr) * 1994-10-05 1997-01-03 Commissariat Energie Atomique Polyazacycloalcanes, complexes tri-, tetra- ou pentaazamacrocycliques, procede de fabrication de ces polyazacycloalcanes substitues ou non et greffes sur un support et utilisations des polyazacycloalcanes
US6770261B2 (en) 1995-06-02 2004-08-03 Research Corporation Technologies Magnetic resonance imaging agents for the detection of physiological agents
US5707605A (en) 1995-06-02 1998-01-13 Research Corporation Technologies Magnetic resonance imaging agents for the detection of physiological agents
US6713045B1 (en) 1995-06-02 2004-03-30 Research Corporation Technologies, Inc. Targeted magnetic resonance imaging agents for the detection of physiological processes
US5980862A (en) 1995-06-02 1999-11-09 Research Corporation Technologies Magnetic resonance imaging agents for the detection of physiological agents
US5739313A (en) 1995-11-13 1998-04-14 Regents Of The University Of Minnesota Radionuclide labeling of vitamin B12 and coenzymes thereof
IT1284046B1 (it) 1996-06-21 1998-05-08 Bracco Spa Processo per la preparazione di tetraazamacrocicli
US20040170563A1 (en) 1997-10-27 2004-09-02 Meade Thomas J. Magnetic resonance imaging agents for the delivery of therapeutic agents
CA2309749A1 (en) 1997-11-17 1999-05-27 Research Corporation Technologies, Inc. Magnetic resonance imaging agents for the detection of physiological agents
US6071490A (en) 1998-05-07 2000-06-06 Immunomedics, Inc. Position emission tomography using gallium-68 chelates
EP1148878A4 (en) 1999-01-26 2003-04-02 Fox Chase Cancer Ct 1,4,8,11-TETRAAZA-CYCLOTETRADECANE DERIVATIVES AS RADIODIAGNOSTICS AND THE USE THEREOF FOR DETERMINING HYPOXIA AND RADIOR RESISTANCE OF TUMORS
US6692724B1 (en) 1999-10-25 2004-02-17 Board Of Regents, The University Of Texas System Ethylenedicysteine (EC)-drug conjugates, compositions and methods for tissue specific disease imaging
US6565828B2 (en) 2000-04-07 2003-05-20 Bristol-Myers Squibb Company Macrocyclic chelants for metallopharmaceuticals
US6673333B1 (en) 2000-05-04 2004-01-06 Research Corporation Technologies, Inc. Functional MRI agents for cancer imaging
EP1286704B1 (en) * 2000-06-02 2014-07-23 Board of Regents, The University of Texas System ETHYLENEDICYSTEINE (EC)-glucose analog CONJUGATES
US6641797B2 (en) * 2000-08-11 2003-11-04 Schering Aktiengesellschaft Perfluoroalkyl-containing complexes with sugar radicals, process for their production and their use
EP1326523A4 (en) 2000-10-19 2005-01-05 Gen Hospital Corp VISUALIZATION OF THE ENZYMATIC ACTIVITY
JP2004537573A (ja) * 2001-08-08 2004-12-16 ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー 心臓灌流およびビトロネクチン受容体を標的とするイメージング剤の同時イメージング
WO2003082301A1 (en) 2002-03-29 2003-10-09 Threshold Pharmaceuticals, Inc. Compositions and methods for treating cancer
US20050232866A1 (en) 2004-03-26 2005-10-20 Alerion Biomedical Inc. Biochemically-activated contrast agents for magnetic resonance imaging
EP1797106A1 (en) 2004-09-07 2007-06-20 Triumf, operating as a joint venture by the Governors of the Universities of Alberta, Synthesis of radiolabeled sugar metal complexes
CA2593256A1 (en) 2005-01-05 2006-07-13 Board Of Regents, The University Of Texas System Conjugates for dual imaging and radiochemotherapy: composition, manufacturing, and applications
US20060275217A1 (en) 2005-05-06 2006-12-07 Caravan Peter D Chemical exchange saturation transfer contrast agents
WO2006127842A2 (en) 2005-05-23 2006-11-30 The Regents Of The University Of California Tracers for monitoring the activity of sodium/glucose cotransporters in health and disease
US8097237B2 (en) 2005-08-23 2012-01-17 Stc.Unm Non-invasive diagnostic agents of cancer and methods of diagnosing cancer, especially leukemia and lymphoma
US8758723B2 (en) 2006-04-19 2014-06-24 The Board Of Regents Of The University Of Texas System Compositions and methods for cellular imaging and therapy
US7586102B2 (en) 2006-08-14 2009-09-08 Board Of Regents The University Of Texas System Automated system for formulating radiopharmaceuticals
US7842280B2 (en) 2006-09-06 2010-11-30 Case Western Reserve University Flexibly labeling peptides
EP2155262A4 (en) * 2007-03-27 2012-12-19 Radiomedix Inc COMPOSITIONS FOR TARGETED THERAPIES AND IMAGERY
WO2009054327A1 (ja) 2007-10-22 2009-04-30 Osaka Foundation For Trade And Industry Mri用プローブ
US20100316566A1 (en) * 2008-02-27 2010-12-16 Radiomedix Inc. Radiolabeled hedgehog derivatives for imaging and therapy
CA2738786C (en) * 2008-09-30 2017-12-19 Mallinckrodt Inc. A version of fdg detectable by single-photon emission computed tomography
US10413621B2 (en) 2009-10-19 2019-09-17 Case Western Reserve University Composition and methods for imaging cells
EP2721045B1 (en) 2011-06-20 2017-04-12 Radiomedix Inc. Compositions, methods of synthesis and use of carbohydrate targeted agents
EP2968335B1 (en) 2013-03-15 2019-03-27 Purdue Research Foundation Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors

Also Published As

Publication number Publication date
US20140228551A1 (en) 2014-08-14
EP2721045A2 (en) 2014-04-23
CA2843313C (en) 2018-02-13
US9550001B2 (en) 2017-01-24
EP2721045B1 (en) 2017-04-12
EP2721045A4 (en) 2014-11-12
CA2843313A1 (en) 2012-12-27
WO2012177701A2 (en) 2012-12-27
WO2012177701A3 (en) 2013-05-10
PL2721045T3 (pl) 2017-11-30

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