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MX2021005089A - Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos. - Google Patents

Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos.

Info

Publication number
MX2021005089A
MX2021005089A MX2021005089A MX2021005089A MX2021005089A MX 2021005089 A MX2021005089 A MX 2021005089A MX 2021005089 A MX2021005089 A MX 2021005089A MX 2021005089 A MX2021005089 A MX 2021005089A MX 2021005089 A MX2021005089 A MX 2021005089A
Authority
MX
Mexico
Prior art keywords
ifap
hynic
99mtc
activation protein
novel
Prior art date
Application number
MX2021005089A
Other languages
English (en)
Inventor
García Blanca Elí Ocampo
Vega Erika Patricia Azorín
Mancilla Nallely Patricia Jiménez
Flores Guillermina Ferro
Gutiérrez Myrna Alejandra Luna
Cuevas Clara Leticia Santos
Original Assignee
Instituto Nac De Investigaciones Nucleares
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 Instituto Nac De Investigaciones Nucleares filed Critical Instituto Nac De Investigaciones Nucleares
Priority to MX2021005089A priority Critical patent/MX2021005089A/es
Priority to EP21939473.1A priority patent/EP4331624A1/en
Priority to US18/288,838 priority patent/US20240216551A1/en
Priority to CA3217281A priority patent/CA3217281A1/en
Priority to CN202180100141.9A priority patent/CN117642188A/zh
Priority to PCT/MX2021/050055 priority patent/WO2022231410A1/es
Priority to BR112023022726A priority patent/BR112023022726A2/pt
Priority to KR1020237041332A priority patent/KR20240027585A/ko
Priority to AU2021443407A priority patent/AU2021443407A1/en
Priority to IL308084A priority patent/IL308084A/en
Priority to JP2023567111A priority patent/JP7741893B2/ja
Publication of MX2021005089A publication Critical patent/MX2021005089A/es
Priority to CL2023003230A priority patent/CL2023003230A1/es
Priority to ZA2024/01715A priority patent/ZA202401715B/en
Priority to JP2025146943A priority patent/JP2025172921A/ja

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07F13/00—Compounds containing elements of Groups 7 or 17 of the Periodic Table
    • C07F13/005—Compounds without a metal-carbon linkage
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo
    • 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

Landscapes

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

Abstract

Esta invención se refiere a nuevos radiofármacos inhibidores de la proteína de activación de fibroblastos (iFAP) basados en la molécula ácido ((R)-1-((6-hidrazinilnicotinoil)-D-alanil)pirrolidi n-2-il)borónico (HYNIC-iFAP), donde los nitrógenos de la hidracina del HYNIC actúan como grupos químicos favorables para la interacción de la molécula HYNIC-iFAP con la fenilalanina (Phe-350 y Phe-351), el ácido glutámico (Glu-203 y Glu-204) y con la serina (Ser-624) en el centro activo de la proteína de activación de fibroblastos (FAP), aunado al uso convencional del HYNIC como un agente quelante para el radiometal 99mTc, donde el ácido etilendiaminodiacético (EDDA) es usado para completar la esfera de coordinación del radiometal. El nuevo radiofármaco de 99mTc-EDDA/HYNIC-iFAP (99mTc-HYNlC-iFAP) detecta, con alta afinidad in vivo, a la FAP expresada en el microambiente de tumores malignos de origen epitelial mediante técnicas de imagen molecular SPECT en medicina nuclear. El objeto de esta invención es proporcionar un nuevo radiofármaco específico de SPECT con alta sensibilidad para la detección de la expresión de la proteína FAP en el microambiente tumoral, basado en inhibidores tipo boroPro (radiofármaco de blancos moleculares).
MX2021005089A 2021-04-30 2021-04-30 Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos. MX2021005089A (es)

Priority Applications (14)

Application Number Priority Date Filing Date Title
MX2021005089A MX2021005089A (es) 2021-04-30 2021-04-30 Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos.
KR1020237041332A KR20240027585A (ko) 2021-04-30 2021-10-14 섬유아세포 활성화 단백질의 과발현을 검출하기 위한 ((r)-1-((6-히드라지닐니코티노일)-d-알라닐)피롤리딘-2-일)보론산(hynic-ifap) 기반 방사성 의약품
AU2021443407A AU2021443407A1 (en) 2021-04-30 2021-10-14 Radiopharmaceuticals based on ((r)-1-((6-hydrazinylnicotinoyl)-d-alanyl)pyrrolidin-2-yl)boronic acid (hynic-ifap) for detecting the overexpression of fibroblast activation protein
CA3217281A CA3217281A1 (en) 2021-04-30 2021-10-14 Radiopharmaceuticals based on ((r)-1-((6-hydrazinylnicotinoyl)-d-alanyl)pyrrolidin-2-yl)boronic acid (hynic-ifap) for detecting the overexpression of fibroblast activation protein
CN202180100141.9A CN117642188A (zh) 2021-04-30 2021-10-14 用于检测成纤维细胞激活蛋白过表达的基于((r)-1-((6-肼基烟酰基)-d-丙氨酰基)吡咯烷-2-基)硼酸(hynic-ifap)的放射性药物
PCT/MX2021/050055 WO2022231410A1 (es) 2021-04-30 2021-10-14 Radiofármacos basados en el ácido ((R)‑1‑((6‑hidrazinilnicotinoil)‑D‑alanil)pirrolidin-2-il)borónico (HYNIC-iFAP) para la detección de la sobreexpresión de la proteína de activación de fibroblastos
BR112023022726A BR112023022726A2 (pt) 2021-04-30 2021-10-14 Radiofármacos à base de ácido ((r)-1-((6- hidrazinilnicotinoil)-d-alanil)pirrolidin-2-il)borônico (hynic-ifap) para detecção da superexpressão da proteínas de ativação de fibroblastos
EP21939473.1A EP4331624A1 (en) 2021-04-30 2021-10-14 Radiopharmaceuticals based on ((r)-1-((6-hydrazinylnicotinoyl)-d-alanyl)pyrrolidin-2-yl)boronic acid (hynic-ifap) for detecting the overexpression of fibroblast activation protein
US18/288,838 US20240216551A1 (en) 2021-04-30 2021-10-14 Radiopharmaceuticals based on ((r)-1-((6-hydrazinylnicotinoyl)-d-alanyl)pyrrolidin-2-yl)boronic acid (hynic-ifap) for detecting the overexpression of fibroblast activation protein
IL308084A IL308084A (en) 2021-04-30 2021-10-14 Radiopharmaceuticals based on R -1 6 hydrazinylnicotinoyl d alanylpyrrolidin-2-y hynic acid-IFAP for fibrob detection
JP2023567111A JP7741893B2 (ja) 2021-04-30 2021-10-14 線維芽細胞活性化タンパク質の過剰発現を検出するための（（ｒ）－１－（（６－ヒドラジニルニコチノイル）－ｄ－アラニル）ピロリジン－２－イル）ボロン酸（ｈｙｎｉｃ－ｉｆａｐ）をベースとする放射性医薬品
CL2023003230A CL2023003230A1 (es) 2021-04-30 2023-10-30 Radiofármacos basados en el ácido ((r) 1 ((6 hidrazinilnicotinoil) d alanil)pirrolidin-2-il)borónico (hynic-ifap) para la detección de la sobreexpresión de la proteína de activación de fibroblastos.
ZA2024/01715A ZA202401715B (en) 2021-04-30 2024-02-28 Radiopharmaceuticals based on ((r)-1-((6-hydrazinylnicotinoyl)-dalanyl) pyrrolidin-2-yl)boronic acid (hynic-ifap) for detecting the overexpression of fibroblast activation protein
JP2025146943A JP2025172921A (ja) 2021-04-30 2025-09-04 線維芽細胞活性化タンパク質の過剰発現を検出するための（（ｒ）－１－（（６－ヒドラジニルニコチノイル）－ｄ－アラニル）ピロリジン－２－イル）ボロン酸（ｈｙｎｉｃ－ｉｆａｐ）をベースとする放射性医薬品

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
MX2021005089A MX2021005089A (es) 2021-04-30 2021-04-30 Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos.

Publications (1)

Publication Number Publication Date
MX2021005089A true MX2021005089A (es) 2022-11-01

Family

ID=83847159

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2021005089A MX2021005089A (es) 2021-04-30 2021-04-30 Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos.

Country Status (13)

Country Link
US (1) US20240216551A1 (es)
EP (1) EP4331624A1 (es)
JP (2) JP7741893B2 (es)
KR (1) KR20240027585A (es)
CN (1) CN117642188A (es)
AU (1) AU2021443407A1 (es)
BR (1) BR112023022726A2 (es)
CA (1) CA3217281A1 (es)
CL (1) CL2023003230A1 (es)
IL (1) IL308084A (es)
MX (1) MX2021005089A (es)
WO (1) WO2022231410A1 (es)
ZA (1) ZA202401715B (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117143080B (zh) * 2023-08-30 2025-12-05 北京师范大学 一种含肼基尼古酰胺基的fapi-46衍生物及其应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002055544A2 (en) 2000-12-23 2002-07-18 Dyax Corp Fibrin binding polypeptides useful inter alia in medical imaging processes
JP2015526402A (ja) 2012-06-29 2015-09-10 ジーイー・ヘルスケア・リミテッド 線維症のイメージング
PL3433238T3 (pl) 2016-03-22 2021-12-13 The Johns Hopkins University Środki o wysokim powinowactwie ukierunkowane na antygen błonowy specyficzny dla gruczołu krokowego do endoradioterapii raka gruczołu krokowego
JP7166512B2 (ja) 2016-05-03 2022-11-08 インスティチュート ナショナル デ ラ サンテ エ デ ラ ルシェルシュ メディカル （インセルム） 炎症のイメージングのための分子標識としてのＣＤ３１ｓｈｅｄ
MX2016008466A (es) * 2016-06-24 2017-12-25 Instituto Nac De Investigaciones Nucleares 99mtc-edda/hynic-ipsma como un radiofarmaco para la deteccion de la sobre-expresion del antigeno prostatico de membrana.
PH12020551205A1 (en) * 2018-02-06 2021-04-19 Univ Heidelberg Fap inhibitors
KR20220158038A (ko) * 2020-03-24 2022-11-29 트러스티즈 오브 터프츠 칼리지 Fap-표적화된 방사성약제 및 영상화제 및 이와 관련된 용도
CN112625065A (zh) 2020-12-22 2021-04-09 北京师范大学 锝-99m标记含肼基尼古酰胺基的FAPI衍生物及制备方法和应用

Also Published As

Publication number Publication date
CL2023003230A1 (es) 2024-09-13
AU2021443407A1 (en) 2023-12-14
JP2025172921A (ja) 2025-11-26
US20240216551A1 (en) 2024-07-04
IL308084A (en) 2023-12-01
EP4331624A1 (en) 2024-03-06
CA3217281A1 (en) 2022-11-03
JP7741893B2 (ja) 2025-09-18
JP2024516687A (ja) 2024-04-16
ZA202401715B (en) 2025-03-26
KR20240027585A (ko) 2024-03-04
CN117642188A (zh) 2024-03-01
WO2022231410A1 (es) 2022-11-03
BR112023022726A2 (pt) 2024-01-02

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