CN111511408A - 靶向成纤维细胞活化蛋白-α(FAP-α)的成像剂及放射治疗剂 - Google Patents

靶向成纤维细胞活化蛋白-α(FAP-α)的成像剂及放射治疗剂 Download PDF

Info

Publication number
CN111511408A
CN111511408A CN201880083520.XA CN201880083520A CN111511408A CN 111511408 A CN111511408 A CN 111511408A CN 201880083520 A CN201880083520 A CN 201880083520A CN 111511408 A CN111511408 A CN 111511408A
Authority
CN
China
Prior art keywords
group
alkyl
compound
fibroblast activation
activation protein
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.)
Pending
Application number
CN201880083520.XA
Other languages
English (en)
Chinese (zh)
Inventor
杨兴
斯里达尔·尼玛加达
史蒂文·罗韦
斯蒂芬妮·斯莱尼亚
马丁·G·庞培
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.)
Johns Hopkins University
Original Assignee
Johns Hopkins University
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=66247306&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN111511408(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Johns Hopkins University filed Critical Johns Hopkins University
Priority to CN202310498227.2A priority Critical patent/CN116617420A/zh
Publication of CN111511408A publication Critical patent/CN111511408A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K51/0485—Porphyrins, texaphyrins wherein the nitrogen atoms forming the central ring system complex the radioactive metal
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0032—Methine dyes, e.g. cyanine dyes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0052—Small organic molecules
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07B2200/07—Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicinal Preparation (AREA)
CN201880083520.XA 2017-10-23 2018-10-23 靶向成纤维细胞活化蛋白-α(FAP-α)的成像剂及放射治疗剂 Pending CN111511408A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202310498227.2A CN116617420A (zh) 2017-10-23 2018-10-23 靶向成纤维细胞活化蛋白α的化合物、药物组合物及用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762575607P 2017-10-23 2017-10-23
US62/575,607 2017-10-23
PCT/US2018/057086 WO2019083990A2 (en) 2017-10-23 2018-10-23 IMAGING AND RADIATION THERAPY AGENTS TARGETING α-FIBROBLAST ACTIVATION PROTEIN α (FAP-α)

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202310498227.2A Division CN116617420A (zh) 2017-10-23 2018-10-23 靶向成纤维细胞活化蛋白α的化合物、药物组合物及用途

Publications (1)

Publication Number Publication Date
CN111511408A true CN111511408A (zh) 2020-08-07

Family

ID=66247306

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201880083520.XA Pending CN111511408A (zh) 2017-10-23 2018-10-23 靶向成纤维细胞活化蛋白-α(FAP-α)的成像剂及放射治疗剂
CN202310498227.2A Pending CN116617420A (zh) 2017-10-23 2018-10-23 靶向成纤维细胞活化蛋白α的化合物、药物组合物及用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202310498227.2A Pending CN116617420A (zh) 2017-10-23 2018-10-23 靶向成纤维细胞活化蛋白α的化合物、药物组合物及用途

Country Status (12)

Country Link
US (5) US20200330624A1 (enExample)
EP (1) EP3700580A4 (enExample)
JP (2) JP2021500373A (enExample)
KR (2) KR102764076B1 (enExample)
CN (2) CN111511408A (enExample)
AU (2) AU2018355222B2 (enExample)
BR (1) BR112020008011A2 (enExample)
CA (1) CA3088138A1 (enExample)
EA (1) EA202090776A1 (enExample)
IL (1) IL274088A (enExample)
MX (2) MX2020004807A (enExample)
WO (1) WO2019083990A2 (enExample)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111699181A (zh) * 2018-02-06 2020-09-22 海德堡大学 Fap抑制剂
CN112138175A (zh) * 2020-09-01 2020-12-29 上海市质子重离子临床技术研发中心 一种放射性核素99mTc标记FAPI的化合物的制备方法
CN113105432A (zh) * 2021-03-30 2021-07-13 上海交通大学医学院附属仁济医院 一种碳-11（11c）放射性药物及其制备方法和应用
CN113277989A (zh) * 2021-04-27 2021-08-20 中南大学湘雅医院 一种68Ga标记的分子探针、制备方法及其应用
CN113527266A (zh) * 2021-06-23 2021-10-22 上海健康医学院 一种靶向fap的双氧水响应的前药及其制备方法与应用
CN113880810A (zh) * 2021-09-24 2022-01-04 厦门大学 一种核素标记的配合物及其制备方法和应用
CN114369084A (zh) * 2021-02-10 2022-04-19 上海蓝纳成生物技术有限公司 一种截短型伊文思蓝修饰的成纤维细胞活化蛋白抑制剂及其制备方法和应用
CN115368342A (zh) * 2022-08-24 2022-11-22 西南医科大学附属医院 成纤维细胞活性蛋白抑制剂、其放射性核素标记物及制备方法和应用
WO2024078592A1 (zh) * 2022-10-14 2024-04-18 无锡诺宇医药科技有限公司 靶向成纤维细胞活化蛋白的药物及其应用
CN118063689A (zh) * 2024-01-26 2024-05-24 锐康九域(厦门)医药科技有限公司 成纤维细胞激活蛋白-α响应水解致电荷翻转的聚合物-药物偶联物及其制备方法和应用
WO2024165072A1 (zh) * 2023-02-10 2024-08-15 成都纽瑞特医疗科技股份有限公司 一种多肽化合物及其应用
WO2024230728A1 (zh) * 2023-05-08 2024-11-14 江苏恒瑞医药股份有限公司 靶向成纤维细胞活化蛋白的配体

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110291401B (zh) 2016-12-14 2023-04-11 普渡研究基金会 成纤维细胞活化蛋白(fap)-靶向成像和治疗
KR102764076B1 (ko) * 2017-10-23 2025-02-05 더 존스 홉킨스 유니버시티 섬유아세포 활성 단백질-α(FAP-α)를 표적하는 영상화 및 방사선치료제
IL275333B2 (en) * 2017-12-15 2023-09-01 Praxis Biotech LLC Inhibitors of fibroblast activation protein
AU2019360944B2 (en) 2018-10-17 2022-09-29 Purdue Research Foundation Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis
US11504364B2 (en) 2018-12-21 2022-11-22 Praxis Biotech LLC Inhibitors of fibroblast activation protein
JP7608425B2 (ja) 2019-07-08 2025-01-06 ３ベー ファーマシューティカルズ ゲーエムベーハー 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用
EP3763726A1 (en) 2019-07-08 2021-01-13 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
EP3997104A1 (en) 2019-07-08 2022-05-18 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
US20220409747A1 (en) * 2019-09-17 2022-12-29 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases
US20240002408A1 (en) * 2020-01-31 2024-01-04 Purdue Research Foundation Fibroblast activation protein (fap) - targeted antifibrotic therapy
HUE058835T2 (hu) 2020-02-12 2022-09-28 Philochem Ag Fibroblaszt aktiváló protein ligandumok célzott szállítási alkalmazásokhoz
EP4147053A1 (en) 2020-05-07 2023-03-15 Institut Curie Antxr1 as a biomarker of immunosuppressive fibroblast populations and its use for predicting response to immunotherapy
WO2021234181A1 (en) * 2020-05-22 2021-11-25 Universität Heidelberg Use of fap inhibitor in a method of diagnosis
CN114790194B (zh) * 2020-12-21 2024-03-26 苏州药明博锐生物科技有限公司 成纤维细胞活化蛋白抑制剂
EP4050018A1 (en) * 2021-01-07 2022-08-31 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
JP2024503637A (ja) * 2021-01-07 2024-01-26 ３ベー ファーマシューティカルズ ゲーエムベーハー 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用
JP7651785B2 (ja) * 2021-02-10 2025-03-27 烟台藍納成生物技術股▲ふん▼有限公司 切断型エバンスブルー修飾線維芽細胞活性化タンパク質阻害剤及びその調製方法と応用
US20240148916A1 (en) 2021-02-12 2024-05-09 Philochem Ag Bivalent fibroblast activation protein ligands for targeted delivery applications
EP4043452A1 (en) 2021-02-12 2022-08-17 Philochem AG Bivalent fibroblast activation protein ligands for targeted delivery applications
MX2023011599A (es) * 2021-04-02 2024-02-02 Univ Johns Hopkins Agentes heterobivalentes y homobivalentes dirigidos a la proteína alfa de activación de fibroblastos y/o al antígeno de membrana específico de próstata.
AU2022275579C1 (en) * 2021-05-19 2024-08-22 Ferronova Pty Ltd Mapping nanoparticles
GB202109922D0 (en) 2021-07-09 2021-08-25 Blue Earth Diagnostics Ltd Radiotracers and therapeutics binding to fibroblast activation protein (fap)
EP4122499A1 (en) * 2021-07-23 2023-01-25 3B Pharmaceuticals GmbH Fibroblast activation protein inhibitors and use thereof
TW202320805A (zh) * 2021-08-18 2023-06-01 美商杜夫特學院信託管理公司 用於pet造影之選擇性靶向纖維母細胞活化蛋白之放射性氟標誌試劑
WO2023057457A1 (en) 2021-10-04 2023-04-13 Philochem Ag Radiolabelled fibroblast activation protein ligands
TW202317541A (zh) 2021-10-28 2023-05-01 行政院原子能委員會核能研究所 一種靶向成纖維細胞活化蛋白之化合物或其鹽，其製備方法及其用途
WO2023081301A1 (en) * 2021-11-05 2023-05-11 On Target Laboratories, LLC Fibroblast activation protein targeted dyes their related uses
WO2023144379A1 (en) 2022-01-30 2023-08-03 Philochem Ag High-affinity ligands of fibroblast activation protein for targeted delivery applications
WO2023162946A1 (ja) 2022-02-22 2023-08-31 国立大学法人大阪大学 放射標識されたＦＡＰα親和性化合物およびその用途
JP2025513317A (ja) * 2022-04-21 2025-04-24 シャンハイ シノタウ バイオテック． シーオー．， エルティーディー Ｆａｐ阻害剤
WO2023222558A1 (en) 2022-05-14 2023-11-23 Zounek Alexis Nikolai Precursor and theranostic radiotracer with improved tumor retention
CN115304582B (zh) * 2022-07-20 2023-05-12 北京法伯新天医药科技有限公司 FAP-α特异性肿瘤诊断显像剂
JP2025526460A (ja) * 2022-07-28 2025-08-13 レイシオ・セラピューティクス，インコーポレーテッド 線維芽細胞活性化タンパク質標的組成物およびその使用の方法
WO2024052333A1 (en) 2022-09-06 2024-03-14 Philochem Ag Multivalent fibroblast activation protein ligands for targeted delivery applications
EP4342890A1 (en) 2022-09-21 2024-03-27 Erasmus University Rotterdam Medical Center Platform and scaffold for fap targeting agents
CN120282804A (zh) * 2022-09-23 2025-07-08 核素迪姆股份公司 高纯度铜放射性药物组合物及其诊断和治疗用途
TW202426433A (zh) 2022-09-23 2024-07-01 瑞士商紐利迪姆股份公司 成纖維細胞活化蛋白（ｆａｐ）抑制劑、ｆａｐ結合物及其診斷與治療用途
WO2025029608A1 (en) * 2023-07-28 2025-02-06 Ratio Therapeutics, Inc. Fibroblast activation protein-targeted compositions and methods of use thereof
WO2025046043A1 (en) 2023-08-31 2025-03-06 Stichting Radboud Universitair Medisch Centrum Endometriosis tracer
WO2025063849A2 (en) 2023-09-21 2025-03-27 Erasmus University Medical Center Rotterdam Dimeric fap targeting agents
WO2025125335A1 (en) 2023-12-13 2025-06-19 Radiovaxx Gmbh Cytotoxic or radiopharmaceutical compound with sulfur fluoride exchange group
WO2025125621A1 (en) 2023-12-14 2025-06-19 Radiovaxx Gmbh Cancer-associated protein-targeted strong or covalently binding precursor compounds and radiotracers
WO2025146433A1 (en) 2024-01-05 2025-07-10 Radiovaxx Gmbh Precursor and theranostic radiotracer with prolonged tumor retention
CN118271393B (zh) * 2024-05-31 2024-09-03 中国药科大学 一种靶向fap的二聚化合物及其探针和应用

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101784192A (zh) * 2007-06-26 2010-07-21 约翰·霍普金斯大学 标记的前列腺特异性膜抗原(psma)的抑制子、生物学评估及作为成像试剂的用途
CN102203061A (zh) * 2008-09-25 2011-09-28 分子制药洞察公司 选择性seprase抑制剂
US20140357650A1 (en) * 2012-01-17 2014-12-04 Fox Chase Cancer Center Novel fap inhibitors
CN104379181A (zh) * 2012-06-29 2015-02-25 通用电气健康护理有限公司 对纤维变性成像
WO2015114166A2 (en) * 2014-02-03 2015-08-06 Philochem Ag Targeted drug conjugates
WO2016196628A1 (en) * 2015-06-01 2016-12-08 The Johns Hopkins University Nuclear imaging and radiotherapeutics agents targeting carbonic anhydrase ix and uses thereof
CN111699181A (zh) * 2018-02-06 2020-09-22 海德堡大学 Fap抑制剂

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008545661A (ja) * 2005-05-19 2008-12-18 ジェネンテック・インコーポレーテッド 線維芽細胞活性化タンパク質阻害剤化合物および
PL2318366T3 (pl) 2008-08-01 2017-10-31 Univ Johns Hopkins Środki wiążące PSMA i ich zastosowania
CA3257131A1 (en) * 2009-03-19 2025-04-15 The Johns Hopkins University PSMA-TARGETING COMPOUNDS AND RELATED USES
WO2016149188A1 (en) * 2015-03-13 2016-09-22 The Johns Hopkins University 68Ga-LABELED NOTA-CHELATED PSMA-TARGETED IMAGING AND THERAPEUTIC AGENTS
CA2882019C (en) * 2012-08-15 2021-02-09 Visen Medical, Inc. Prostate specific antigen agents and methods of using same for prostate cancer imaging
WO2016065142A2 (en) * 2014-10-22 2016-04-28 The Johns Hopkins University New scaffolds and multifunctional intermediates for imaging psma and cancer therapy
CN110291401B (zh) 2016-12-14 2023-04-11 普渡研究基金会 成纤维细胞活化蛋白(fap)-靶向成像和治疗
KR102764076B1 (ko) * 2017-10-23 2025-02-05 더 존스 홉킨스 유니버시티 섬유아세포 활성 단백질-α(FAP-α)를 표적하는 영상화 및 방사선치료제

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101784192A (zh) * 2007-06-26 2010-07-21 约翰·霍普金斯大学 标记的前列腺特异性膜抗原(psma)的抑制子、生物学评估及作为成像试剂的用途
CN102203061A (zh) * 2008-09-25 2011-09-28 分子制药洞察公司 选择性seprase抑制剂
US20140357650A1 (en) * 2012-01-17 2014-12-04 Fox Chase Cancer Center Novel fap inhibitors
CN104379181A (zh) * 2012-06-29 2015-02-25 通用电气健康护理有限公司 对纤维变性成像
WO2015114166A2 (en) * 2014-02-03 2015-08-06 Philochem Ag Targeted drug conjugates
WO2016196628A1 (en) * 2015-06-01 2016-12-08 The Johns Hopkins University Nuclear imaging and radiotherapeutics agents targeting carbonic anhydrase ix and uses thereof
CN111699181A (zh) * 2018-02-06 2020-09-22 海德堡大学 Fap抑制剂

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
PETRA DVOŘÁKOVÁ等: "Inhibitor-Decorated Polymer Conjugates Targeting Fibroblast", 《JOURNAL OF MEDICINAL CHEMISTRY》, vol. 60, no. 20, 27 September 2017 (2017-09-27), pages 8386 - 8387, XP055615512, DOI: 10.1021/acs.jmedchem.7b00767 *
王吉欣等: "《放射性药物学》", vol. 1, 原子能出版社, pages: 357 *

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111699181A (zh) * 2018-02-06 2020-09-22 海德堡大学 Fap抑制剂
CN112138175A (zh) * 2020-09-01 2020-12-29 上海市质子重离子临床技术研发中心 一种放射性核素99mTc标记FAPI的化合物的制备方法
CN114369084A (zh) * 2021-02-10 2022-04-19 上海蓝纳成生物技术有限公司 一种截短型伊文思蓝修饰的成纤维细胞活化蛋白抑制剂及其制备方法和应用
CN114369084B (zh) * 2021-02-10 2023-02-03 烟台蓝纳成生物技术有限公司 一种截短型伊文思蓝修饰的成纤维细胞活化蛋白抑制剂及其制备方法和应用
CN113105432A (zh) * 2021-03-30 2021-07-13 上海交通大学医学院附属仁济医院 一种碳-11（11c）放射性药物及其制备方法和应用
CN113105432B (zh) * 2021-03-30 2022-03-04 上海交通大学医学院附属仁济医院 一种碳-11（11c）放射性药物及其制备方法和应用
CN113277989A (zh) * 2021-04-27 2021-08-20 中南大学湘雅医院 一种68Ga标记的分子探针、制备方法及其应用
CN113527266A (zh) * 2021-06-23 2021-10-22 上海健康医学院 一种靶向fap的双氧水响应的前药及其制备方法与应用
CN113880810B (zh) * 2021-09-24 2023-02-28 厦门大学 一种核素标记的配合物及其制备方法和应用
CN113880810A (zh) * 2021-09-24 2022-01-04 厦门大学 一种核素标记的配合物及其制备方法和应用
CN115368342A (zh) * 2022-08-24 2022-11-22 西南医科大学附属医院 成纤维细胞活性蛋白抑制剂、其放射性核素标记物及制备方法和应用
CN115368342B (zh) * 2022-08-24 2024-01-23 西南医科大学附属医院 成纤维细胞活性蛋白抑制剂、其放射性核素标记物及制备方法和应用
WO2024078592A1 (zh) * 2022-10-14 2024-04-18 无锡诺宇医药科技有限公司 靶向成纤维细胞活化蛋白的药物及其应用
WO2024165072A1 (zh) * 2023-02-10 2024-08-15 成都纽瑞特医疗科技股份有限公司 一种多肽化合物及其应用
WO2024230728A1 (zh) * 2023-05-08 2024-11-14 江苏恒瑞医药股份有限公司 靶向成纤维细胞活化蛋白的配体
CN118063689A (zh) * 2024-01-26 2024-05-24 锐康九域(厦门)医药科技有限公司 成纤维细胞激活蛋白-α响应水解致电荷翻转的聚合物-药物偶联物及其制备方法和应用

Also Published As

Publication number Publication date
MX2023013164A (es) 2023-11-23
US20250235565A1 (en) 2025-07-24
KR102764076B1 (ko) 2025-02-05
AU2018355222B2 (en) 2024-10-03
IL274088A (en) 2020-06-30
US12115233B2 (en) 2024-10-15
US20250186628A1 (en) 2025-06-12
MX2020004807A (es) 2020-10-05
US20240293584A1 (en) 2024-09-05
BR112020008011A2 (pt) 2020-10-27
WO2019083990A2 (en) 2019-05-02
EP3700580A4 (en) 2021-06-23
AU2024203249A1 (en) 2024-06-06
US20200330624A1 (en) 2020-10-22
CA3088138A1 (en) 2019-05-02
JP2021500373A (ja) 2021-01-07
CN116617420A (zh) 2023-08-22
KR20200063230A (ko) 2020-06-04
KR20240162157A (ko) 2024-11-14
EA202090776A1 (ru) 2020-07-27
WO2019083990A3 (en) 2019-06-13
JP2024109682A (ja) 2024-08-14
EP3700580A2 (en) 2020-09-02
US11938201B2 (en) 2024-03-26
US20230364274A1 (en) 2023-11-16
AU2018355222A1 (en) 2020-04-30

Similar Documents

Publication Publication Date Title
CN111511408A (zh) 靶向成纤维细胞活化蛋白-α(FAP-α)的成像剂及放射治疗剂
US20240382629A1 (en) Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen
JP7449864B2 (ja) エバンスブルー誘導体の化学結合体ならびに前立腺癌を標的とするための放射線療法および造影剤としてのその使用
KR20180134918A (ko) 전립선 암의 내부방사선요법을 위한 전립선-특이적 막 항원 표적화된 고-친화성 제제
US20240148916A1 (en) Bivalent fibroblast activation protein ligands for targeted delivery applications
CN109476655B (zh) 靶向碳酸酐酶ix的核成像剂和放射治疗剂及其用途
US20220054659A1 (en) Psma-targeted pamam dendrimers for specific delivery of imaging, contrast and therapeutic agents
WO2023030509A1 (zh) 一种肽脲素衍生物、含其的药物组合物及其应用
WO2024183618A1 (zh) 一种含氮杂环类化合物及其制备方法与用途
JP2025530298A (ja) 腫瘍細胞の検出のための放射性核種組成物及びその使用方法
WO2025088200A2 (en) Acid phosphatase 3 ligands for targeted delivery applications
CN118164957A (zh) 一种靶向成纤维细胞活化蛋白显像剂
HK40029571A (en) Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents for targeting prostate cancer

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination