ECSP18091468A - Complejos radio-farmacéuticos - Google Patents

Complejos radio-farmacéuticos

Info

Publication number
ECSP18091468A
ECSP18091468A ECSENADI201891468A ECDI201891468A ECSP18091468A EC SP18091468 A ECSP18091468 A EC SP18091468A EC SENADI201891468 A ECSENADI201891468 A EC SENADI201891468A EC DI201891468 A ECDI201891468 A EC DI201891468A EC SP18091468 A ECSP18091468 A EC SP18091468A
Authority
EC
Ecuador
Prior art keywords
tissue
targets
thorium
complex
coupling
Prior art date
Application number
ECSENADI201891468A
Other languages
English (en)
Inventor
Alan Cuthbertson
Jenny Karlsson
Ernst Weber
Stefanie Hammer
Mark Trautwein
Original Assignee
Bayer As
Bayer Pharma AG
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 Bayer As, Bayer Pharma AG filed Critical Bayer As
Publication of ECSP18091468A publication Critical patent/ECSP18091468A/es

Links

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
    • A61K51/0474—Organic 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
    • A61K51/0478—Organic 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 complexes from non-cyclic ligands, e.g. EDTA, MAG3
    • 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
    • A61K51/0474—Organic 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
    • A61K51/0482—Organic 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
    • 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
    • A61K51/1075—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 the antibody being against an enzyme
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La invención proporciona un método para la formación de un complejo de torio que se dirige al tejido, comprendiendo dicho método; a) formar un quelante octadentado que comprende cuatro restos hidroxipiridinona (HOPO), sustituidos en la posición N con un grupo metilo, y un resto de acoplamiento que termina en un grupo ácido carboxílico; b) acoplar dicho quelante octadentado a por lo menos un resto que se dirige al tejido que se dirige a prolil endopeptidasa FAP; y c) contactar dicho agente quelante que se dirige al tejido con una solución acuosa que comprende un ion de por lo menos un isótopo de torio emisor de radiaciones alfa. Se proporciona un método para el tratamiento de una enfermedad neoplásica o hiperplásica que comprende la administración de un complejo de torio que se dirige al tejido de ese tipo, así como también se provee el complejo y formulaciones farmacéuticas correspondientes.
ECSENADI201891468A 2016-06-10 2018-12-10 Complejos radio-farmacéuticos ECSP18091468A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP16173874 2016-06-10

Publications (1)

Publication Number Publication Date
ECSP18091468A true ECSP18091468A (es) 2018-12-31

Family

ID=56132786

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI201891468A ECSP18091468A (es) 2016-06-10 2018-12-10 Complejos radio-farmacéuticos

Country Status (26)

Country Link
US (1) US20190298865A1 (es)
EP (1) EP3468619A1 (es)
JP (1) JP2019517547A (es)
KR (1) KR20190016544A (es)
CN (1) CN109689115A (es)
AR (1) AR110466A1 (es)
AU (1) AU2017277463A1 (es)
BR (1) BR112018075554A2 (es)
CA (1) CA3026900A1 (es)
CL (1) CL2018003550A1 (es)
CO (1) CO2018013359A2 (es)
CR (1) CR20180581A (es)
CU (1) CU20180149A7 (es)
DO (1) DOP2018000277A (es)
EA (1) EA201892814A1 (es)
EC (1) ECSP18091468A (es)
IL (1) IL263538A (es)
MA (1) MA45225A (es)
MX (1) MX2018015340A (es)
NI (1) NI201800136A (es)
PE (1) PE20190327A1 (es)
PH (1) PH12018502605A1 (es)
SG (1) SG11201810967VA (es)
TW (1) TW201805025A (es)
UY (1) UY37286A (es)
WO (1) WO2017211809A1 (es)

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WO2016183266A1 (en) 2015-05-13 2016-11-17 Enanta Pharmaceuticals, Inc. Ehpatitis b antiviral agents
ES2938341T3 (es) 2016-03-07 2023-04-10 Enanta Pharm Inc Agentes antivirales contra la hepatitis B
CA3073986A1 (en) 2017-08-28 2019-03-07 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
US11058678B2 (en) 2018-01-22 2021-07-13 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
CN112955142A (zh) 2018-09-21 2021-06-11 英安塔制药有限公司 官能化杂环化合物作为抗病毒剂
UY38483A (es) 2018-11-21 2020-06-30 Enanta Pharm Inc Heterociclos funcionalizados como agentes antivirales
US11236111B2 (en) 2019-06-03 2022-02-01 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
WO2020247575A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
WO2020247561A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
EP3763726A1 (en) 2019-07-08 2021-01-13 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
CN118406106A (zh) 2019-07-08 2024-07-30 3B制药有限公司 包含成纤维细胞活化蛋白配体的化合物及其用途
CN114341158B (zh) 2019-07-08 2024-08-06 3B制药有限公司 包含成纤维细胞活化蛋白配体的化合物及其用途
WO2021007488A1 (en) 2019-07-11 2021-01-14 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
TW202116733A (zh) 2019-07-25 2021-05-01 挪威商拜耳公司 用於癌症診斷及治療之靶向放射性藥品
WO2021055425A2 (en) 2019-09-17 2021-03-25 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
US11802125B2 (en) 2020-03-16 2023-10-31 Enanta Pharmaceuticals, Inc. Functionalized heterocyclic compounds as antiviral agents
KR20230093251A (ko) 2020-09-10 2023-06-27 프리시릭스 엔.브이. Fap에 대한 항체 단편
IL303925A (en) 2021-01-07 2023-08-01 3B Pharmaceuticals Gmbh Compounds comprising a protein ligand for fibroblast activation and its use
EP4050018A1 (en) 2021-01-07 2022-08-31 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting

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US5179017A (en) 1980-02-25 1993-01-12 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
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GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
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Also Published As

Publication number Publication date
EP3468619A1 (en) 2019-04-17
CR20180581A (es) 2019-02-11
US20190298865A1 (en) 2019-10-03
SG11201810967VA (en) 2019-01-30
AR110466A1 (es) 2019-04-03
DOP2018000277A (es) 2018-12-31
IL263538A (en) 2019-01-31
MA45225A (fr) 2019-04-17
NI201800136A (es) 2019-04-29
KR20190016544A (ko) 2019-02-18
CO2018013359A2 (es) 2018-12-14
CU20180149A7 (es) 2019-07-04
AU2017277463A1 (en) 2019-01-03
EA201892814A1 (ru) 2019-06-28
CA3026900A1 (en) 2017-12-14
MX2018015340A (es) 2019-03-28
PE20190327A1 (es) 2019-03-05
BR112018075554A2 (pt) 2019-10-01
TW201805025A (zh) 2018-02-16
WO2017211809A1 (en) 2017-12-14
CL2018003550A1 (es) 2019-02-01
UY37286A (es) 2018-01-31
PH12018502605A1 (en) 2019-10-21
JP2019517547A (ja) 2019-06-24
CN109689115A (zh) 2019-04-26

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