JP2021500373A - 線維芽細胞活性化タンパク質α（ＦＡＰ−α）を標的とする撮像剤および放射線療法用薬剤 - Google Patents

線維芽細胞活性化タンパク質α（ＦＡＰ−α）を標的とする撮像剤および放射線療法用薬剤 Download PDF

Info

Publication number
JP2021500373A
JP2021500373A JP2020523010A JP2020523010A JP2021500373A JP 2021500373 A JP2021500373 A JP 2021500373A JP 2020523010 A JP2020523010 A JP 2020523010A JP 2020523010 A JP2020523010 A JP 2020523010A JP 2021500373 A JP2021500373 A JP 2021500373A
Authority
JP
Japan
Prior art keywords
group
alkyl
fap
compound according
substituted
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
JP2020523010A
Other languages
English (en)
Japanese (ja)
Other versions
JP2021500373A5 (https=
Inventor
ヤン シン
ヤン シン
ニマガダ シュリダール
ニマガダ シュリダール
ロー スティーブン
ロー スティーブン
スラニア ステファニー
スラニア ステファニー
ジー ポンパー マーティン
ジー ポンパー マーティン
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=JP2021500373(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
Publication of JP2021500373A publication Critical patent/JP2021500373A/ja
Publication of JP2021500373A5 publication Critical patent/JP2021500373A5/ja
Priority to JP2024078640A priority Critical patent/JP2024109682A/ja
Pending legal-status Critical Current

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
    • A61K51/0485—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
    • 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
    • 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
    • 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
    • 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
    • A61K49/005—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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (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)
JP2020523010A 2017-10-23 2018-10-23 線維芽細胞活性化タンパク質α（ＦＡＰ−α）を標的とする撮像剤および放射線療法用薬剤 Pending JP2021500373A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024078640A JP2024109682A (ja) 2017-10-23 2024-05-14 線維芽細胞活性化タンパク質α（ＦＡＰ－α）を標的とする撮像剤および放射線療法用薬剤

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
JP2024078640A Division JP2024109682A (ja) 2017-10-23 2024-05-14 線維芽細胞活性化タンパク質α（ＦＡＰ－α）を標的とする撮像剤および放射線療法用薬剤

Publications (2)

Publication Number Publication Date
JP2021500373A true JP2021500373A (ja) 2021-01-07
JP2021500373A5 JP2021500373A5 (https=) 2021-12-02

Family

ID=66247306

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2020523010A Pending JP2021500373A (ja) 2017-10-23 2018-10-23 線維芽細胞活性化タンパク質α（ＦＡＰ−α）を標的とする撮像剤および放射線療法用薬剤
JP2024078640A Pending JP2024109682A (ja) 2017-10-23 2024-05-14 線維芽細胞活性化タンパク質α（ＦＡＰ－α）を標的とする撮像剤および放射線療法用薬剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2024078640A Pending JP2024109682A (ja) 2017-10-23 2024-05-14 線維芽細胞活性化タンパク質α（ＦＡＰ－α）を標的とする撮像剤および放射線療法用薬剤

Country Status (12)

Country Link
US (5) US20200330624A1 (https=)
EP (1) EP3700580A4 (https=)
JP (2) JP2021500373A (https=)
KR (2) KR102764076B1 (https=)
CN (2) CN116617420A (https=)
AU (2) AU2018355222B2 (https=)
BR (1) BR112020008011A2 (https=)
CA (1) CA3088138A1 (https=)
EA (1) EA202090776A1 (https=)
IL (1) IL274088A (https=)
MX (2) MX2020004807A (https=)
WO (1) WO2019083990A2 (https=)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021512949A (ja) * 2018-02-06 2021-05-20 ウニベルジテート ハイデルベルク Ｆａｐ阻害物質
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
JP2023545213A (ja) * 2021-02-10 2023-10-26 烟台藍納成生物技術有限公司 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
JP2024527627A (ja) * 2021-07-23 2024-07-25 スリービー・ファーマシューティカルズ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 線維芽細胞活性化タンパク質阻害剤及びその使用
JP2024109682A (ja) * 2017-10-23 2024-08-14 ザ・ジョンズ・ホプキンス・ユニバーシティ 線維芽細胞活性化タンパク質α（ＦＡＰ－α）を標的とする撮像剤および放射線療法用薬剤
JP2025503541A (ja) * 2022-07-20 2025-02-04 嘉興法伯新天医薬科技有限公司 ＦＡＰ－α特異的腫瘍診断イメージング剤

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116474108A (zh) 2016-12-14 2023-07-25 普渡研究基金会 成纤维细胞活化蛋白(fap)-靶向成像和治疗
JP2021506972A (ja) 2017-12-15 2021-02-22 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤
US11426472B2 (en) 2018-10-17 2022-08-30 Purdue Research Foundation Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis
CN113811529A (zh) 2018-12-21 2021-12-17 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂
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
EP3763726A1 (en) 2019-07-08 2021-01-13 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
IL289673B2 (en) 2019-07-08 2026-04-01 3B Pharmaceuticals Gmbh Compounds comprising a protein ligand for fibroblast activation and their use
WO2021055641A1 (en) * 2019-09-17 2021-03-25 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases
WO2021155292A1 (en) * 2020-01-31 2021-08-05 Philip Stewart Low Fibroblast activation protein (fap) - targeted antifibrotic therapy
EP3891138B1 (en) 2020-02-12 2022-01-12 Philochem AG Fibroblast activation protein ligands for targeted delivery applications
CA3176497A1 (en) 2020-05-07 2021-11-11 Fatima MECHTA-GRIGORIOU 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
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
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
KR20230129261A (ko) 2021-01-07 2023-09-07 쓰리비 파마슈티컬스 게엠베하 섬유모세포 활성화 단백질 리간드를 포함하는 화합물및 그의 용도
EP4050018A1 (en) 2021-01-07 2022-08-31 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
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
JP2024506644A (ja) 2021-02-12 2024-02-14 フィロケム・アーゲー 標的送達に適用するための二価線維芽細胞活性化タンパク質リガンド
EP4043452A1 (en) 2021-02-12 2022-08-17 Philochem AG Bivalent fibroblast activation protein ligands for targeted delivery applications
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
BR112023020123A2 (pt) * 2021-04-02 2024-01-23 Univ Johns Hopkins Agentes heterobivalentes e homobivalentes que alvejam proteína alfa de ativação de fibroblasto alfa e/ou antígeno de membrana específico da próstata
CN113277989B (zh) * 2021-04-27 2022-05-31 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
AU2022275579C1 (en) 2021-05-19 2024-08-22 Ferronova Pty Ltd Mapping nanoparticles
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
GB202109922D0 (en) 2021-07-09 2021-08-25 Blue Earth Diagnostics Ltd Radiotracers and therapeutics binding to fibroblast activation protein (fap)
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
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
MX2024004077A (es) 2021-10-04 2024-04-18 Philochem Ag Ligandos de proteina de activacion de fibroblastos radioetiquetados.
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
US20250177582A1 (en) 2022-01-30 2025-06-05 Philochem Ag High-affinity ligands of fibroblast activation protein for targeted delivery applications
WO2023202655A1 (en) * 2022-04-21 2023-10-26 Shanghai Sinotau Biotech. Co., Ltd Fap inhibitors
WO2023222558A1 (en) 2022-05-14 2023-11-23 Zounek Alexis Nikolai Precursor and theranostic radiotracer with improved tumor retention
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
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
CN119816493A (zh) 2022-09-06 2025-04-11 菲罗化学股份公司 用于靶向递送应用的多价成纤维细胞激活蛋白配体
EP4342890A1 (en) * 2022-09-21 2024-03-27 Erasmus University Rotterdam Medical Center Platform and scaffold for fap targeting agents
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
AU2023347470A1 (en) * 2022-09-23 2025-04-10 Nuclidium Ag High-purity copper radiopharmaceutical compositions and diagnostic and therapeutic uses thereof
CN117883585A (zh) * 2022-10-14 2024-04-16 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
KR20250143347A (ko) * 2023-02-10 2025-10-01 청두 뉴 라디오메디슨 테크놀로지 컴퍼니 리미티드 폴리펩타이드 화합물 및 이의 용도
KR20260006628A (ko) 2023-05-08 2026-01-13 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 섬유아세포 활성화 단백질을 표적화하는 리간드
AU2024316927A1 (en) * 2023-07-28 2026-02-26 Ratio Therapeutics, Inc. Fibroblast activation protein-targeted compositions and methods of use thereof
CN117164557A (zh) * 2023-08-30 2023-12-05 上海交通大学医学院附属仁济医院 靶向成纤维细胞激活蛋白的放射性药物标记前体及其放射性标记化合物与应用
CN121752300A (zh) 2023-08-31 2026-03-27 荷兰拉德堡德大学学术医学中心 子宫内膜异位症示踪剂
WO2025063849A2 (en) 2023-09-21 2025-03-27 Erasmus University Medical Center Rotterdam Dimeric fap targeting agents
US20250186630A1 (en) * 2023-12-12 2025-06-12 Viewpoint Molecular Targeting, Inc. Fibroblast activation protein targeting peptides
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
CN118063689B (zh) * 2024-01-26 2025-01-28 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
WO2025250709A1 (en) * 2024-05-28 2025-12-04 Actithera, Inc. Bifunctional compounds for cancer treatment
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
WO2026007968A1 (zh) * 2024-07-01 2026-01-08 杭州景嘉航生物医药科技有限公司 一种靶向结合成纤维细胞活化蛋白的化合物及应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010014933A2 (en) * 2008-08-01 2010-02-04 The Johns Hopkins University Psma-binding agents and uses thereof
WO2010108125A2 (en) * 2009-03-19 2010-09-23 The Johns Hopkins University Psma-targeting compounds and uses thereof
JP2010532754A (ja) * 2007-06-26 2010-10-14 ジョンズ ホプキンス ユニバーシティ 前立腺特異膜抗原（ｐｓｍａ）の標識阻害剤、生物学的評価およびイメージング剤としての使用
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
JP2015532641A (ja) * 2012-08-15 2015-11-12 ビセン メディカル， インコーポレイテッド 前立腺がんイメージングのための前立腺特異的抗原薬剤およびその使用方法
WO2016065142A2 (en) * 2014-10-22 2016-04-28 The Johns Hopkins University New scaffolds and multifunctional intermediates for imaging psma and cancer therapy
WO2016149188A1 (en) * 2015-03-13 2016-09-22 The Johns Hopkins University 68Ga-LABELED NOTA-CHELATED PSMA-TARGETED IMAGING AND THERAPEUTIC AGENTS
WO2016196628A1 (en) * 2015-06-01 2016-12-08 The Johns Hopkins University Nuclear imaging and radiotherapeutics agents targeting carbonic anhydrase ix and uses thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1943257A2 (en) * 2005-05-19 2008-07-16 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
WO2010036814A1 (en) * 2008-09-25 2010-04-01 Molecular Insight Pharmaceuticals, Inc. Selective seprase inhibitors
US20150320892A1 (en) * 2012-06-29 2015-11-12 Ge Healthcare Limited Imaging fibrosis
EP3102242A2 (en) * 2014-02-03 2016-12-14 Philochem AG Targeted drug conjugates
CN116474108A (zh) 2016-12-14 2023-07-25 普渡研究基金会 成纤维细胞活化蛋白(fap)-靶向成像和治疗
EA202090776A1 (ru) * 2017-10-23 2020-07-27 Дзе Джонс Хопкинс Юниверсити Визуализирующие и радиотерапевтические агенты, нацеленные на фибробласт-активирующий белок-альфа (fapalpha)
SG11202007180QA (en) 2018-02-06 2020-08-28 Univ Heidelberg Fap inhibitor

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010532754A (ja) * 2007-06-26 2010-10-14 ジョンズ ホプキンス ユニバーシティ 前立腺特異膜抗原（ｐｓｍａ）の標識阻害剤、生物学的評価およびイメージング剤としての使用
WO2010014933A2 (en) * 2008-08-01 2010-02-04 The Johns Hopkins University Psma-binding agents and uses thereof
WO2010108125A2 (en) * 2009-03-19 2010-09-23 The Johns Hopkins University Psma-targeting compounds and uses thereof
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
JP2015532641A (ja) * 2012-08-15 2015-11-12 ビセン メディカル， インコーポレイテッド 前立腺がんイメージングのための前立腺特異的抗原薬剤およびその使用方法
WO2016065142A2 (en) * 2014-10-22 2016-04-28 The Johns Hopkins University New scaffolds and multifunctional intermediates for imaging psma and cancer therapy
WO2016149188A1 (en) * 2015-03-13 2016-09-22 The Johns Hopkins University 68Ga-LABELED NOTA-CHELATED PSMA-TARGETED IMAGING AND THERAPEUTIC AGENTS
WO2016196628A1 (en) * 2015-06-01 2016-12-08 The Johns Hopkins University Nuclear imaging and radiotherapeutics agents targeting carbonic anhydrase ix and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J. MED. CHEM., vol. 60, JPN6022045724, 2017, pages 8385 - 8393, ISSN: 0005058498 *

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024109682A (ja) * 2017-10-23 2024-08-14 ザ・ジョンズ・ホプキンス・ユニバーシティ 線維芽細胞活性化タンパク質α（ＦＡＰ－α）を標的とする撮像剤および放射線療法用薬剤
JP2021512949A (ja) * 2018-02-06 2021-05-20 ウニベルジテート ハイデルベルク Ｆａｐ阻害物質
JP2023545213A (ja) * 2021-02-10 2023-10-26 烟台藍納成生物技術有限公司 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
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
JP2024527627A (ja) * 2021-07-23 2024-07-25 スリービー・ファーマシューティカルズ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 線維芽細胞活性化タンパク質阻害剤及びその使用
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
JP2025503541A (ja) * 2022-07-20 2025-02-04 嘉興法伯新天医薬科技有限公司 ＦＡＰ－α特異的腫瘍診断イメージング剤
JP7741988B2 (ja) 2022-07-20 2025-09-18 嘉興法伯新天医薬科技有限公司 ＦＡＰ－α特異的腫瘍診断イメージング剤

Also Published As

Publication number Publication date
EP3700580A2 (en) 2020-09-02
WO2019083990A2 (en) 2019-05-02
AU2018355222A1 (en) 2020-04-30
IL274088A (en) 2020-06-30
WO2019083990A3 (en) 2019-06-13
US20250235565A1 (en) 2025-07-24
AU2018355222B2 (en) 2024-10-03
CN111511408A (zh) 2020-08-07
US20200330624A1 (en) 2020-10-22
EA202090776A1 (ru) 2020-07-27
KR20200063230A (ko) 2020-06-04
EP3700580A4 (en) 2021-06-23
US11938201B2 (en) 2024-03-26
US20230364274A1 (en) 2023-11-16
CA3088138A1 (en) 2019-05-02
US20240293584A1 (en) 2024-09-05
BR112020008011A2 (pt) 2020-10-27
MX2023013164A (es) 2023-11-23
KR102764076B1 (ko) 2025-02-05
AU2024203249A1 (en) 2024-06-06
US20250186628A1 (en) 2025-06-12
US12115233B2 (en) 2024-10-15
CN116617420A (zh) 2023-08-22
MX2020004807A (es) 2020-10-05
KR20240162157A (ko) 2024-11-14
JP2024109682A (ja) 2024-08-14

Similar Documents

Publication Publication Date Title
US11938201B2 (en) Imaging and radiotherapeutics agents targeting fibroblast-activation protein-alpha (FAP-alpha)
US20240382629A1 (en) Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen
US11911488B2 (en) Scaffolds and multifunctional intermediates for imaging PSMA and cancer therapy
CN108026144B (zh) 18f-标记的前列腺特异性膜抗原(psma)的抑制剂以及它们作为前列腺癌的成像剂的应用
TW201609153A (zh) 用於正子斷層掃描之化合物
JP7030061B2 (ja) 炭酸脱水酵素ｉｘを標的にする核造影および放射性治療剤ならびにそれらの使用
US20220054659A1 (en) Psma-targeted pamam dendrimers for specific delivery of imaging, contrast and therapeutic agents
US10717750B2 (en) 68Ga-labeled NOTA-chelated PSMA-targeted imaging and therapeutic agents
WO2016149188A1 (en) 68Ga-LABELED NOTA-CHELATED PSMA-TARGETED IMAGING AND THERAPEUTIC AGENTS
HK40094491A (zh) 靶向成纤维细胞活化蛋白α的化合物、药物组合物及用途
CA3024097C (en) Nuclear imaging and radiotherapeutics agents targeting carbonic anhydrase ix and uses thereof
WO2025179155A1 (en) Chemically stable keto-amide-based fibroblast activation protein-targeted conjugates, compositions, and methods of use

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211022

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20211022

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20221108

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230208

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20230516

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20230816

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20231116

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240206

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20240426

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20240702

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240806

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20240917