CA2982269C - Heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same - Google Patents

Heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same Download PDF

Info

Publication number
CA2982269C
CA2982269C CA2982269A CA2982269A CA2982269C CA 2982269 C CA2982269 C CA 2982269C CA 2982269 A CA2982269 A CA 2982269A CA 2982269 A CA2982269 A CA 2982269A CA 2982269 C CA2982269 C CA 2982269C
Authority
CA
Canada
Prior art keywords
groups
compound
group
optionally substituted
nwc
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CA2982269A
Other languages
English (en)
French (fr)
Other versions
CA2982269A1 (en
Inventor
Christopher Martin Waldmann
Anton A. Toutov
Jennifer Marie Murphy
Robert H. Grubbs
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
California Institute of Technology
University of California, San Diego
Original Assignee
California Institute of Technology
University of California, San Diego
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 California Institute of Technology, University of California, San Diego filed Critical California Institute of Technology
Publication of CA2982269A1 publication Critical patent/CA2982269A1/en
Application granted granted Critical
Publication of CA2982269C publication Critical patent/CA2982269C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/12—Organo silicon halides
    • 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
    • C07B59/004—Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium
    • 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
    • A61K51/1027—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 against receptors, cell-surface antigens or cell-surface determinants
    • 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
    • A61K51/1045—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 against animal or human tumor cells or tumor cell determinants
    • A61K51/1072—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 against animal or human tumor cells or tumor cell determinants the tumor cell being from the reproductive system, e.g. ovaria, uterus, testes or prostate
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Reproductive Health (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2982269A 2015-05-26 2016-05-24 Heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same Active CA2982269C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562166240P 2015-05-26 2015-05-26
US62/166,240 2015-05-26
PCT/US2016/033923 WO2016191424A2 (en) 2015-05-26 2016-05-24 Novel heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same

Publications (2)

Publication Number Publication Date
CA2982269A1 CA2982269A1 (en) 2016-12-01
CA2982269C true CA2982269C (en) 2023-12-05

Family

ID=57394170

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2982269A Active CA2982269C (en) 2015-05-26 2016-05-24 Heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same

Country Status (6)

Country Link
US (4) US10800797B2 (enExample)
EP (1) EP3303349B1 (enExample)
JP (2) JP7266365B2 (enExample)
CN (1) CN107667109B (enExample)
CA (1) CA2982269C (enExample)
WO (1) WO2016191424A2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3303349B1 (en) 2015-05-26 2022-07-06 The Regents of the University of California Novel heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same
KR20240027896A (ko) * 2017-07-28 2024-03-04 테크니쉐 우니베르지테트 뮌헨 이중 모드 방사성 트레이서 및 치료법
WO2019055825A1 (en) 2017-09-15 2019-03-21 The Regents Of The University Of California INHIBITION OF AMINOACYLASE 3 (AA3) IN THE TREATMENT OF CANCER
BR112021012110A2 (pt) * 2019-01-30 2021-09-08 Technische Universität München Radiofarmacêuticos substituídos por aceptor de fluoreto de silício
WO2020220020A1 (en) * 2019-04-26 2020-10-29 The Regents Of The University Of California Silicon-fluoride heteroaromatic systems for applications in positron emission tomography (pet) molecular imaging
KR102899941B1 (ko) * 2019-05-24 2025-12-16 듀크 유니버시티 18f-방사선 표지된 생체 분자
US20230202944A1 (en) * 2020-05-29 2023-06-29 Fuzionaire, Inc. Methods for Rapid Formation of Chemicals Including Positron Emission Tomography Biomarkers
WO2023205755A2 (en) * 2022-04-20 2023-10-26 Fuzionaire Diagnostics, Inc. Theranostic silicon-fluoride heteroaromatic systems and methods thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6972336B2 (en) * 2002-07-18 2005-12-06 Novartis Ag N-alkylation of indole derivatives
KR20090085599A (ko) 2006-10-02 2009-08-07 바이엘 쉐링 파마 악티엔게젤샤프트 Ｐｅｔ 영상화용 규소 유도체
US20120046242A1 (en) * 2008-12-24 2012-02-23 Massachusetts Institute Of Technology Molecular activators of the wnt/beta-catenin pathway
EP2654803B1 (en) 2010-12-22 2021-08-18 General Electric Company Radiolabeled her2-binding peptide conjugates
EP3303349B1 (en) * 2015-05-26 2022-07-06 The Regents of the University of California Novel heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same

Also Published As

Publication number Publication date
US20200377529A1 (en) 2020-12-03
US20180346491A1 (en) 2018-12-06
EP3303349A2 (en) 2018-04-11
WO2016191424A3 (en) 2016-12-29
JP2018521956A (ja) 2018-08-09
CN107667109A (zh) 2018-02-06
JP7266365B2 (ja) 2023-04-28
EP3303349A4 (en) 2019-03-13
US11447508B2 (en) 2022-09-20
CA2982269A1 (en) 2016-12-01
JP2021073293A (ja) 2021-05-13
CN107667109B (zh) 2021-08-03
US12371445B2 (en) 2025-07-29
WO2016191424A2 (en) 2016-12-01
US20250333425A1 (en) 2025-10-30
US20230114064A1 (en) 2023-04-13
EP3303349B1 (en) 2022-07-06
US10800797B2 (en) 2020-10-13

Similar Documents

Publication Publication Date Title
EP3303349B1 (en) Novel heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same
JP7290638B2 (ja) Ｗｅｅ１阻害剤としての大環状化合物及びその使用
JP7168149B2 (ja) Ｆｇｆｒ阻害剤としてのピラジン－２（１ｈ）－オン系化合物
ES2955132T3 (es) Compuestos heterocíclicos sustituidos con amina como inhibidores de EHMT2 y métodos de uso de los mismos
EP2693876B1 (en) Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds
AU2018227417A1 (en) Inhibitors of (alpha-v)(beta-6) integrin
CA2808678C (en) Fused ring compound for use as mineralocorticoid receptor antagonist
US12139492B2 (en) Substituted pyrimidines for the targeted degradation of Bruton's tyrosine kinase
ES3062921T3 (en) Preparation method for novel rho-related protein kinase inhibitor and intermediate in preparation method
ES2899694T3 (es) Compuestos novedosos, su síntesis y sus usos
US20220274961A1 (en) Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors
US20230106083A1 (en) Silicon-fluoride heteroaromatic systems for applications in positron emission tomography (pet) molecular imaging
WO2015166289A1 (en) Pyrrolobenzodiazepine compounds
CA3197470A1 (en) Bicyclic compounds
WO2007007054A1 (en) Phthalamides, succinimides and related compounds and their use as pharmaceuticals
JP6491214B2 (ja) 放射性標識のための方法および試薬
ES2906868T3 (es) Intermedio farmacéutico para preparar pimavanserina
AU2018205277B2 (en) Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) for the treatment of neurodegenerative diseases
Wuest et al. Fluorine-and rhenium-containing geldanamycin derivatives as leads for the development of molecular probes for imaging Hsp90
EP3758696B1 (en) [1,2,4]triazolo[1,5-a]pyrimidine compounds and use in stabilizing microtubules
CN120230029A (zh) 整合素α4β7拮抗剂化合物及其制备方法与应用
JP2025507308A (ja) 化学療法剤および組織結合小分子のコンジュゲート、組成物、ならびにその方法
Blass et al. Increased rigidity and bioisosteric replacement in the design, synthesis and preliminary evaluation of novel, functionalized 3, 3-dialkyl-γ-butyrolactones as sigma-2 ligands
EP3968994A1 (en) Abhd12 inhibitors and methods of making and using same
WO2017196544A1 (en) Novel compositions for labeling biomolecules and methods using same

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20210521

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 9TH ANNIV.) - STANDARD

Year of fee payment: 9

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250508

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250508

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 10TH ANNIV.) - STANDARD

Year of fee payment: 10

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20260519

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20260519