KR20220066098A - 섬유모세포 활성화 단백질 (fap)-표적화 영상화 및 암 및 다른 섬유화 및 염증성 질환의 요법 - Google Patents

섬유모세포 활성화 단백질 (fap)-표적화 영상화 및 암 및 다른 섬유화 및 염증성 질환의 요법 Download PDF

Info

Publication number
KR20220066098A
KR20220066098A KR1020227012076A KR20227012076A KR20220066098A KR 20220066098 A KR20220066098 A KR 20220066098A KR 1020227012076 A KR1020227012076 A KR 1020227012076A KR 20227012076 A KR20227012076 A KR 20227012076A KR 20220066098 A KR20220066098 A KR 20220066098A
Authority
KR
South Korea
Prior art keywords
compound
alkyl
linker
group
independently
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
KR1020227012076A
Other languages
English (en)
Korean (ko)
Inventor
필립 스튜어트 로우
맛두리 스리니바사라오
라메쉬 무카말라
Original Assignee
퍼듀 리서치 파운데이션
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 퍼듀 리서치 파운데이션 filed Critical 퍼듀 리서치 파운데이션
Publication of KR20220066098A publication Critical patent/KR20220066098A/ko
Pending legal-status Critical Current

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/001Preparation for luminescence or biological staining
    • A61K49/0013Luminescence
    • A61K49/0017Fluorescence in vivo
    • A61K49/0019Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0032Methine dyes, e.g. cyanine dyes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/001Preparation for luminescence or biological staining
    • A61K49/0013Luminescence
    • A61K49/0017Fluorescence in vivo
    • A61K49/0019Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0041Xanthene dyes, used in vivo, e.g. administered to a mice, e.g. rhodamines, rose Bengal
    • A61K49/0043Fluorescein, used in vivo
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/001Preparation for luminescence or biological staining
    • A61K49/0013Luminescence
    • A61K49/0017Fluorescence in vivo
    • A61K49/005Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0052Small organic molecules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/085Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier conjugated systems
    • 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
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0446Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K51/0497Organic compounds conjugates with a carrier being an organic compounds
    • 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
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Radiology & Medical Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020227012076A 2019-09-17 2020-09-17 섬유모세포 활성화 단백질 (fap)-표적화 영상화 및 암 및 다른 섬유화 및 염증성 질환의 요법 Pending KR20220066098A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962901792P 2019-09-17 2019-09-17
US62/901,792 2019-09-17
PCT/US2020/051328 WO2021055641A1 (en) 2019-09-17 2020-09-17 Fibroblast activation protein (fap)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases

Publications (1)

Publication Number Publication Date
KR20220066098A true KR20220066098A (ko) 2022-05-23

Family

ID=74883518

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020227012076A Pending KR20220066098A (ko) 2019-09-17 2020-09-17 섬유모세포 활성화 단백질 (fap)-표적화 영상화 및 암 및 다른 섬유화 및 염증성 질환의 요법

Country Status (11)

Country Link
US (1) US20220409747A1 (https=)
EP (1) EP4031184A4 (https=)
JP (2) JP2022548155A (https=)
KR (1) KR20220066098A (https=)
CN (1) CN114901315B (https=)
AU (2) AU2020348781B2 (https=)
BR (1) BR112022005013A2 (https=)
CA (1) CA3150890A1 (https=)
IL (1) IL291386A (https=)
MX (1) MX2022003215A (https=)
WO (1) WO2021055641A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2934532B1 (en) 2012-12-20 2019-10-23 Purdue Research Foundation Chimeric antigen receptor-expressing t cells as anti-cancer therapeutics
JP7282521B2 (ja) 2016-04-08 2023-05-29 パーデュー・リサーチ・ファウンデイション Car t細胞療法のための方法および組成物
JP7178355B2 (ja) 2017-02-28 2022-11-25 エンドサイト・インコーポレイテッド Car t細胞療法のための組成物および方法
JP7549303B2 (ja) 2018-01-22 2024-09-11 エンドサイト・インコーポレイテッド Car t細胞の使用方法
CN112105382A (zh) 2018-02-23 2020-12-18 恩多塞特公司 用于car t细胞疗法的顺序方法
US20230147962A1 (en) * 2020-02-12 2023-05-11 Philochem Ag Fibroblast activation protein ligands for targeted delivery applications
EP4132921A4 (en) * 2020-04-09 2024-03-27 Purdue Research Foundation Pi3 kinase inhibitors and uses thereof
WO2023244828A1 (en) * 2022-06-17 2023-12-21 Purdue Research Foundation Fibroblast activation protein-targeted nanoparticle magnetic resonance imaging agents
AU2024235779A1 (en) * 2023-03-10 2025-10-23 Purdue Research Foundation Bi-specific adapters and their use with universal car-t cells in the treatment of tumors and the inhibition of cancer-associated fibroblasts
WO2026041108A1 (zh) * 2024-08-23 2026-02-26 苏州博锐创合医药有限公司 基于环肽和共价弹头的化合物及其用途

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8071787B2 (en) * 2009-03-13 2011-12-06 National Health Research Institutes Pyrrolidine compounds
CN103788071A (zh) * 2012-11-01 2014-05-14 中国人民解放军第二军医大学 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
AU2017213404A1 (en) * 2016-01-29 2018-09-20 Kyowa Kirin Co., Ltd. Nucleic acid conjugate
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)
US10966999B2 (en) * 2017-12-20 2021-04-06 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
WO2019154859A1 (en) * 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
SG11202007180QA (en) * 2018-02-06 2020-08-28 Univ Heidelberg Fap inhibitor
DE102018126558A1 (de) * 2018-10-24 2020-04-30 Helmholtz-Zentrum Dresden - Rossendorf E.V. Markierungsvorläufer mit Quadratsäure-Kopplung

Also Published As

Publication number Publication date
CN114901315B (zh) 2025-04-29
MX2022003215A (es) 2022-04-25
AU2020348781A1 (en) 2022-04-14
JP2022548155A (ja) 2022-11-16
BR112022005013A2 (pt) 2022-06-21
WO2021055641A1 (en) 2021-03-25
CN114901315A (zh) 2022-08-12
JP2025131780A (ja) 2025-09-09
EP4031184A4 (en) 2023-12-06
AU2026200943A1 (en) 2026-02-26
CA3150890A1 (en) 2021-03-25
IL291386A (en) 2022-05-01
EP4031184A1 (en) 2022-07-27
AU2020348781B2 (en) 2025-11-27
US20220409747A1 (en) 2022-12-29

Similar Documents

Publication Publication Date Title
KR20220066098A (ko) 섬유모세포 활성화 단백질 (fap)-표적화 영상화 및 암 및 다른 섬유화 및 염증성 질환의 요법
RU2573633C2 (ru) Хинолил-содержащее соединение гидроксамовой кислоты, способ его получения, а также применение при лечении заболеваний, вызванных аномальной активностью протеинкиназы и/или гистондеацетилазы
JP6987641B2 (ja) シリコン系薬物複合体及びその使用方法
US20180298047A1 (en) Trigger-activatable metabolic sugar precursors for cancer-selective labeling and targeting
WO2021068898A1 (zh) 新颖的kras g12c蛋白抑制剂及其制备方法和用途
WO2021016392A1 (en) Multivalent fibroblast-targeted agents and methods of use
JP2024510267A (ja) 線維芽細胞活性化タンパク質を標的とする化合物、およびその使用方法
Xiao et al. Development of bifunctional anti-PD-L1 antibody MMAE conjugate with cytotoxicity and immunostimulation
JP2025534729A (ja) α型葉酸受容体を標的とするペメトレキセド近赤外蛍光分子の蛍光トレーサーとしての用途
CN118252945A (zh) 肿瘤微环境激活的药物偶联物及抗体药物偶联物
US20250195532A1 (en) Novel phosphoinositide 3-kinase (pi3k) inhibitor, compositions comprising the same, methods of making, and methods of treating a disease
EP4062935A1 (en) Theranostic system for directed diffusion of therapeutic and imaging agents to cancer cells
CN106317018B (zh) 一种肿瘤靶向性亲脂性阳离子-苯丁酸氮芥化合物及制备方法和在白蛋白纳米药物中的应用
CN111093717B (zh) 靶向性纳米颗粒
CN113512022A (zh) 一种基于pH响应的多功能荧光链接体及制备方法和应用
KR102068860B1 (ko) Vegfr-3 저해제의 간세포암 치료를 위한 용도
WO2024260425A1 (zh) 靶向fap的化合物、基于其的放射性核素标记配合物以及其制备方法和应用
CN116747317B (zh) 靶向b7-h3抗体-mmae偶联物及其应用
EA051572B1 (ru) Фибробласт-активирующий белок (far)-таргетированная визуализация и терапия злокачественных опухолей и других фиброзирующих и воспалительных заболеваний
KR20240040099A (ko) Sn38을 포함하는 항체-약물 접합체 중간체 및 그의 제조 방법
CN108314741B (zh) 一种肿瘤血管靶向抗癌肽nkl-dota及其制备方法
CN118878585B (zh) 一种靶向her2铂基抗体偶联物及其合成与肿瘤治疗的应用
CN117460507A (zh) 靶向成纤维细胞激活蛋白的化合物及其使用方法
CN121108109A (zh) 一种靶向alk蛋白的protac化合物及其抗肿瘤应用
CN119971065A (zh) 含毛兰素的抗体药物偶联物及其制备方法和应用

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

D21 Rejection of application intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000