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PE20220935A1 - Quelantes macrociclicos y metodos de uso de estos - Google Patents

Quelantes macrociclicos y metodos de uso de estos

Info

Publication number
PE20220935A1
PE20220935A1 PE2021001868A PE2021001868A PE20220935A1 PE 20220935 A1 PE20220935 A1 PE 20220935A1 PE 2021001868 A PE2021001868 A PE 2021001868A PE 2021001868 A PE2021001868 A PE 2021001868A PE 20220935 A1 PE20220935 A1 PE 20220935A1
Authority
PE
Peru
Prior art keywords
ring
alkyl
hydrogen
independently
chelator
Prior art date
Application number
PE2021001868A
Other languages
English (en)
Inventor
Rhys Salter
Vadim Dudkin
Fengbin Song
Wei Zhang
Shalom Goldberg
John Keith
Original Assignee
Janssen Biotech Inc
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 Janssen Biotech Inc filed Critical Janssen Biotech Inc
Publication of PE20220935A1 publication Critical patent/PE20220935A1/es

Links

Classifications

    • 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
    • A61K51/025Preparations 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 inorganic Tc complexes or compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies 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
    • A61K51/1027Antibodies 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 against receptors, cell-surface antigens or cell-surface determinants
    • 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
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies 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
    • A61K51/1093Antibodies 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

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

Abstract

La presente invencion se refiere a un compuesto quelante de formula (I), donde: cada uno del anillo A y el anillo B es independientemente un arilo de 6-10 miembros o un heteroarilo de 5-10 miembros, en donde cada uno del anillo A y el anillo B se sustituye opcionalmente con uno o mas sustituyentes seleccionados independientemente del grupo que consiste en halo, alquilo, entre otros; Z1 y Z2 son independientemente -(C(R12)2)m- o -(CH2)n-C(R12)(X)-(CH2)n-, donde X es -L1-R11, n es 0 a 5, m es 1 a 5, L1 esta ausente o es un enlazador, R11 es una entidad nucleofilica o una entidad electrofilica, R12 es hidrogeno, alquilo, cicloalquilo, entre otros; R14 a R17 son independientemente hidrogeno, alquilo, entre otros, o alternativamente R14 y R15 y/o R16 y R17 se toman juntos con los atomos de carbono a los cuales se acoplan para formar un anillo cicloalquilo de 5 o 6 miembros opcionalmente sustituido con X, siempre que el quelante comprenda al menos un X, y cuando X esta presente en el anillo A o anillo B, L1 es un enlazador o al menos uno de R12 y R14-R17 no es hidrogeno. Tambien se refiere a un complejo de radiometal de formula (I-m) que comprende un quelante unido a un ion de radiometal emisor alfa a traves de un enlace coordinado, donde M es un ion de radiometal, preferentemente un ion emisor alfa de actinio-225 (225Ac) y a un inmunoconjugado, donde el anticuerpo o fragmento de union al antigeno de este se une especificamente a un antigeno tumoral, el cual puede ser pertuzumab, cetuximab, panitumumab, entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de produccion. Los radioinmunoconjugados producidos mediante conjugacion del quelante de la invencion con un ligando dirigido son utiles en el tratamiento de una enfermedad o trastorno neoplasico, tal como el cancer.
PE2021001868A 2019-05-10 2020-05-08 Quelantes macrociclicos y metodos de uso de estos PE20220935A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962846044P 2019-05-10 2019-05-10
PCT/IB2020/054381 WO2020229974A1 (en) 2019-05-10 2020-05-08 Macrocyclic chelators and methods of use thereof

Publications (1)

Publication Number Publication Date
PE20220935A1 true PE20220935A1 (es) 2022-05-31

Family

ID=70804855

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2021001868A PE20220935A1 (es) 2019-05-10 2020-05-08 Quelantes macrociclicos y metodos de uso de estos

Country Status (22)

Country Link
US (2) US11576986B2 (es)
EP (1) EP3966211A1 (es)
JP (2) JP7734078B2 (es)
KR (1) KR20220006613A (es)
CN (1) CN114127059B (es)
AU (1) AU2020273654A1 (es)
BR (1) BR112021022237A2 (es)
CA (1) CA3139806A1 (es)
CL (1) CL2021002960A1 (es)
CO (1) CO2021015713A2 (es)
CR (1) CR20210556A (es)
DO (1) DOP2021000233A (es)
EA (1) EA202193076A1 (es)
EC (1) ECSP21089217A (es)
IL (1) IL287909A (es)
MA (1) MA55885A (es)
MX (1) MX2021013667A (es)
PE (1) PE20220935A1 (es)
PH (1) PH12021552791A1 (es)
SG (1) SG11202112100PA (es)
UA (1) UA129220C2 (es)
WO (1) WO2020229974A1 (es)

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EP3883610A4 (en) 2018-11-20 2022-11-02 Cornell University MACROCYCLIC COMPLEXES OF RADIONUCLIDES AND THEIR USE IN CANCER RADIATION THERAPY
EA202193076A1 (ru) 2019-05-10 2022-02-16 Янссен Байотек, Инк. Макроциклические хелаторы и способы их применения
HUE064465T2 (hu) 2019-05-10 2024-04-28 Deciphera Pharmaceuticals Llc Heteroarilaminopirimidin amid autophagia inhibitorok és azok felhasználási eljárásai
SMT202300469T1 (it) 2019-05-10 2024-01-10 Deciphera Pharmaceuticals Llc Inibitori dell'autofagia a base di fenilamminopirimidinammidi, e metodi di loro utilizzo
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US20250009917A1 (en) * 2021-09-29 2025-01-09 The University Of Melbourne Macrocycle containing compounds and radiolabelled complexes thereof, as ligands in targeted radiotherapy applications
EP4429718A1 (en) * 2021-11-09 2024-09-18 Janssen Biotech, Inc. Macrocyclic compounds and diagnostic uses thereof
EP4430040A1 (en) * 2021-11-09 2024-09-18 Janssen Biotech, Inc. Macrocyclic compounds and methods of making the same
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JP2023135733A (ja) * 2022-03-16 2023-09-29 Jfeエンジニアリング株式会社 ジルコニウム錯体およびその合成方法
CN114656422B (zh) * 2022-04-22 2023-05-23 重庆理工大学 一种新型氮杂冠醚化合物及其阳离子脂质体、制备方法与应用
CN114874214B (zh) * 2022-05-31 2023-03-21 南京航空航天大学 可偶联巯基的双功能大环螯合剂衍生物及其制备方法
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MX2023005462A (es) 2020-11-10 2023-05-22 Janssen Biotech Inc Compuestos macrociclicos y metodos para usarlos.
CA3205707A1 (en) 2021-01-27 2022-08-04 Fei Shen Immunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses
EP4429718A1 (en) 2021-11-09 2024-09-18 Janssen Biotech, Inc. Macrocyclic compounds and diagnostic uses thereof
EP4430040A1 (en) 2021-11-09 2024-09-18 Janssen Biotech, Inc. Macrocyclic compounds and methods of making the same

Also Published As

Publication number Publication date
JP2025176045A (ja) 2025-12-03
MA55885A (fr) 2022-03-16
EP3966211A1 (en) 2022-03-16
IL287909A (en) 2022-01-01
CN114127059B (zh) 2024-09-24
JP2022532157A (ja) 2022-07-13
SG11202112100PA (en) 2021-11-29
CA3139806A1 (en) 2020-11-19
US11576986B2 (en) 2023-02-14
WO2020229974A1 (en) 2020-11-19
CO2021015713A2 (es) 2021-11-30
CR20210556A (es) 2021-12-17
AU2020273654A1 (en) 2021-11-25
ECSP21089217A (es) 2022-01-31
US12453785B2 (en) 2025-10-28
MX2021013667A (es) 2022-01-31
DOP2021000233A (es) 2022-07-31
US20200353105A1 (en) 2020-11-12
CN114127059A (zh) 2022-03-01
EA202193076A1 (ru) 2022-02-16
BR112021022237A2 (pt) 2022-03-29
UA129220C2 (uk) 2025-02-12
JP7734078B2 (ja) 2025-09-04
PH12021552791A1 (en) 2022-09-05
KR20220006613A (ko) 2022-01-17
US20230110178A1 (en) 2023-04-13
CL2021002960A1 (es) 2022-06-24

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