JP2022548155A - 線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法 - Google Patents

線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法 Download PDF

Info

Publication number
JP2022548155A
JP2022548155A JP2022517166A JP2022517166A JP2022548155A JP 2022548155 A JP2022548155 A JP 2022548155A JP 2022517166 A JP2022517166 A JP 2022517166A JP 2022517166 A JP2022517166 A JP 2022517166A JP 2022548155 A JP2022548155 A JP 2022548155A
Authority
JP
Japan
Prior art keywords
compound
alkyl
linker
independently
group
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
JP2022517166A
Other languages
English (en)
Japanese (ja)
Other versions
JPWO2021055641A5 (https=
JP2022548155A5 (https=
Inventor
フィリップ スチュアート ロウ
マドゥリ シュリニヴァーサラオ
ラメシュ ムッカマーラ
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.)
Purdue Research Foundation
Original Assignee
Purdue Research Foundation
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 Purdue Research Foundation filed Critical Purdue Research Foundation
Publication of JP2022548155A publication Critical patent/JP2022548155A/ja
Publication of JPWO2021055641A5 publication Critical patent/JPWO2021055641A5/ja
Publication of JP2022548155A5 publication Critical patent/JP2022548155A5/ja
Priority to JP2025095652A priority Critical patent/JP2025131780A/ja
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)
JP2022517166A 2019-09-17 2020-09-17 線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法 Pending JP2022548155A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025095652A JP2025131780A (ja) 2019-09-17 2025-06-09 線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025095652A Division JP2025131780A (ja) 2019-09-17 2025-06-09 線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法

Publications (3)

Publication Number Publication Date
JP2022548155A true JP2022548155A (ja) 2022-11-16
JPWO2021055641A5 JPWO2021055641A5 (https=) 2023-09-25
JP2022548155A5 JP2022548155A5 (https=) 2023-09-25

Family

ID=74883518

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2022517166A Pending JP2022548155A (ja) 2019-09-17 2020-09-17 線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法
JP2025095652A Pending JP2025131780A (ja) 2019-09-17 2025-06-09 線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2025095652A Pending JP2025131780A (ja) 2019-09-17 2025-06-09 線維芽細胞活性化タンパク質(fap)を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法

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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100234431A1 (en) * 2009-03-13 2010-09-16 National Health Research Institutes Pyrrolidine compounds
WO2018111989A1 (en) * 2016-12-14 2018-06-21 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
WO2019083990A2 (en) * 2017-10-23 2019-05-02 The Johns Hopkins University IMAGING AND RADIATION THERAPY AGENTS TARGETING α-FIBROBLAST ACTIVATION PROTEIN α (FAP-α)
WO2019154886A1 (en) * 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
WO2019154859A1 (en) * 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
DE102018126558A1 (de) * 2018-10-24 2020-04-30 Helmholtz-Zentrum Dresden - Rossendorf E.V. Markierungsvorläufer mit Quadratsäure-Kopplung

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100234431A1 (en) * 2009-03-13 2010-09-16 National Health Research Institutes Pyrrolidine compounds
WO2018111989A1 (en) * 2016-12-14 2018-06-21 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
WO2019083990A2 (en) * 2017-10-23 2019-05-02 The Johns Hopkins University IMAGING AND RADIATION THERAPY AGENTS TARGETING α-FIBROBLAST ACTIVATION PROTEIN α (FAP-α)
WO2019154886A1 (en) * 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
WO2019154859A1 (en) * 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JUN XU ET AL.: ""The SAR studies on FAP inhibitors as tumor-targeted agents"", MEDICINAL CHEMISTRY RESEARCH, vol. 24, no. 4, JPN7024003280, 2014, pages 1744 - 1752, ISSN: 0005690739 *
TING-YUEH TSAI ET AL.: ""Substituted 4-Carboxymethylpyroglutamic Acid Diamides as Potent and Selective Inhibitors of Fibrob", JOURNAL OF MEDICINAL CHEMISTRY, vol. 53, no. 18, JPN6024030827, 2010, pages 6572 - 6583, ISSN: 0005690740 *

Also Published As

Publication number Publication date
CN114901315B (zh) 2025-04-29
MX2022003215A (es) 2022-04-25
AU2020348781A1 (en) 2022-04-14
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
KR20220066098A (ko) 2022-05-23
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
CN114901315B (zh) 癌症和其他纤维化和炎性疾病的成纤维细胞活化蛋白(fap)靶向的成像和治疗
JP6987641B2 (ja) シリコン系薬物複合体及びその使用方法
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
KR20090108086A (ko) 췌장암 치료용 조성물
JP2020507584A (ja) 癌選択的標識および標的化のためのトリガー活性化可能な糖コンジュゲート
US20240238458A1 (en) Compounds targeting fibroblast-activation protein and methods of use thereof
JP2007536276A (ja) 3−アリール−5,6−ジ置換ピリダジン類
JP2012180365A (ja) 1−アリール−4−置換イソキノリン類
TW202346293A (zh) 含氮雜環衍生物及其组合物和藥學上的應用
CN108404138A (zh) 一种靶向cd24单克隆抗体与二乙胺偶氮鎓二醇盐的偶联物及其应用
WO2024140798A1 (zh) Menin抑制剂及其用途
CN106317018A (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
KR20260025869A (ko) Fap 표적화 화합물, 이에 기반한 방사성 핵종 표지 착물 및 그 제조 방법과 응용
WO2023232142A1 (zh) 一种药物化合物及其用途
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
CN117460507A (zh) 靶向成纤维细胞激活蛋白的化合物及其使用方法
JP2022521715A (ja) がん治療のためのfgfr阻害剤
HK40072758A (en) Multivalent fibroblast-targeted agents and methods of use
CN119971065A (zh) 含毛兰素的抗体药物偶联物及其制备方法和应用
WO2024179381A1 (zh) 一类化学偶联连接子及其用途
CN118878585A (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
HK40031591B (zh) 用於低氧成像、映射和治疗的标记物、缀合物、组合物和方法

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220603

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230914

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20230914

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20231128

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20240731

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240805

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20241105

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20250210

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250609