IL289673B2 - Compounds comprising a protein ligand for fibroblast activation and their use - Google Patents

Compounds comprising a protein ligand for fibroblast activation and their use

Info

Publication number
IL289673B2
IL289673B2 IL289673A IL28967322A IL289673B2 IL 289673 B2 IL289673 B2 IL 289673B2 IL 289673 A IL289673 A IL 289673A IL 28967322 A IL28967322 A IL 28967322A IL 289673 B2 IL289673 B2 IL 289673B2
Authority
IL
Israel
Prior art keywords
compounds
activation protein
protein ligand
fibroblast activation
fibroblast
Prior art date
Application number
IL289673A
Other languages
English (en)
Hebrew (he)
Other versions
IL289673A (en
IL289673B1 (en
Inventor
Frank Osterkamp
Dirk Zboralski
Eberhard Schneider
Christian Haase
Matthias Paschke
Aileen Hohne
Jan Ungewiss
Christiane Smerling
Ulrich Reineke
Anne Bredenbeck
Original Assignee
3B Pharmaceuticals Gmbh
Frank Osterkamp
Dirk Zboralski
Eberhard Schneider
Christian Haase
Matthias Paschke
Aileen Hohne
Jan Ungewiss
Christiane Smerling
Ulrich Reineke
Anne Bredenbeck
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
Priority claimed from EP19000325.1A external-priority patent/EP3763726A1/en
Application filed by 3B Pharmaceuticals Gmbh, Frank Osterkamp, Dirk Zboralski, Eberhard Schneider, Christian Haase, Matthias Paschke, Aileen Hohne, Jan Ungewiss, Christiane Smerling, Ulrich Reineke, Anne Bredenbeck filed Critical 3B Pharmaceuticals Gmbh
Publication of IL289673A publication Critical patent/IL289673A/en
Publication of IL289673B1 publication Critical patent/IL289673B1/en
Publication of IL289673B2 publication Critical patent/IL289673B2/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/14—Dipeptidyl-peptidases and tripeptidyl-peptidases (3.4.14)
    • C12Y304/14005—Dipeptidyl-peptidase IV (3.4.14.5)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Immunology (AREA)
  • General Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
IL289673A 2019-07-08 2020-07-08 Compounds comprising a protein ligand for fibroblast activation and their use IL289673B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19000325.1A EP3763726A1 (en) 2019-07-08 2019-07-08 Compounds comprising a fibroblast activation protein ligand and use thereof
EP19198810 2019-09-20
PCT/EP2020/069308 WO2021005131A1 (en) 2019-07-08 2020-07-08 Compounds comprising a fibroblast activation protein ligand and use thereof

Publications (3)

Publication Number Publication Date
IL289673A IL289673A (en) 2022-03-01
IL289673B1 IL289673B1 (en) 2025-12-01
IL289673B2 true IL289673B2 (en) 2026-04-01

Family

ID=71409440

Family Applications (2)

Application Number Title Priority Date Filing Date
IL289673A IL289673B2 (en) 2019-07-08 2020-07-08 Compounds comprising a protein ligand for fibroblast activation and their use
IL324399A IL324399A (en) 2019-07-08 2020-07-08 Compounds comprising a fibroblast activation protein ligand and use thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL324399A IL324399A (en) 2019-07-08 2020-07-08 Compounds comprising a fibroblast activation protein ligand and use thereof

Country Status (12)

Country Link
US (1) US20220315554A1 (https=)
EP (1) EP3997104A1 (https=)
JP (2) JP7801207B2 (https=)
KR (1) KR20220032078A (https=)
CN (3) CN114341158B (https=)
AU (1) AU2020309161A1 (https=)
BR (1) BR112022000144A2 (https=)
CA (1) CA3145872A1 (https=)
CL (1) CL2022000016A1 (https=)
IL (2) IL289673B2 (https=)
MX (1) MX2022000251A (https=)
WO (1) WO2021005131A1 (https=)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI3997103T3 (fi) 2019-07-08 2025-02-03 3B Pharmaceuticals Gmbh Fibroblastien aktivaatioproteiinin ligandia käsittäviä yhdisteitä ja niiden käyttö
CN115943312A (zh) 2020-05-07 2023-04-07 法国居里学院 免疫抑制性成纤维细胞群体的生物标志物antxr1及其在预测对免疫疗法的反应中的用途
WO2022115778A1 (en) * 2020-11-30 2022-06-02 Rayzebio, Inc. Radiopharmaceutical conjugate compositions and uses thereof
EP4050018A1 (en) * 2021-01-07 2022-08-31 3B Pharmaceuticals GmbH Compounds comprising a fibroblast activation protein ligand and use thereof
GB202109922D0 (en) 2021-07-09 2021-08-25 Blue Earth Diagnostics Ltd Radiotracers and therapeutics binding to fibroblast activation protein (fap)
TW202340226A (zh) * 2021-12-17 2023-10-16 德商３Ｂ製藥有限公司 碳酸酐酶ix配位體
EP4475900A1 (en) 2022-02-09 2024-12-18 Novartis AG Pharmaceutical compositions comprising a 225-actinium-labelled complex and a bismuth sequestering agent
IL322552A (en) * 2023-02-10 2025-10-01 Chengdu New Radiomedicine Tech Co Ltd Polypeptide compound and its use
AU2024221970A1 (en) 2023-02-14 2025-09-11 Radiovaxx Gmbh Drug and treatment method
WO2024198838A1 (zh) * 2023-03-27 2024-10-03 晶核生物医药科技(南京)有限公司 环状多肽类化合物及其应用
EP4692105A1 (en) * 2023-03-27 2026-02-11 Bivision Pharmaceuticals, Inc Cyclic polypeptide compound and use thereof
WO2024198836A1 (zh) * 2023-03-27 2024-10-03 晶核生物医药科技(南京)有限公司 环状多肽类化合物及其应用
CN118930606A (zh) * 2023-05-11 2024-11-12 成都纽瑞特医疗科技股份有限公司 靶向成纤维细胞活化蛋白的多肽放射性核素配合物及其应用
WO2025011611A1 (zh) * 2023-07-11 2025-01-16 江苏恒瑞医药股份有限公司 一种成纤维细胞活化蛋白配体及其用途
WO2025046043A1 (en) 2023-08-31 2025-03-06 Stichting Radboud Universitair Medisch Centrum Endometriosis tracer
WO2025082283A1 (zh) * 2023-10-16 2025-04-24 四川科伦博泰生物医药股份有限公司 环肽结构的配体化合物及其核素标记物、药物组合物及应用
US20250186630A1 (en) 2023-12-12 2025-06-12 Viewpoint Molecular Targeting, Inc. Fibroblast activation protein targeting peptides
WO2025163556A1 (en) 2024-02-01 2025-08-07 Novartis Ag Methods for treating cancer
WO2026008525A1 (en) * 2024-07-01 2026-01-08 Bayer Aktiengesellschaft Stable radionuclide-containing formulations
WO2026017046A1 (zh) * 2024-07-19 2026-01-22 晶核生物医药科技(南京)有限公司 一种环多肽、其制备方法和应用
WO2026021314A1 (zh) * 2024-07-22 2026-01-29 山东威智知科药业有限公司 Fap化合物及其用途
WO2026041109A1 (zh) * 2024-08-23 2026-02-26 苏州博锐创合医药有限公司 成纤维细胞活化蛋白抑制剂及其用途
CN120590466A (zh) * 2025-08-06 2025-09-05 首都医科大学脑重大疾病研究中心(北京脑重大疾病研究院) 一种靶向成纤维细胞活化蛋白的化合物及其应用

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4885363A (en) 1987-04-24 1989-12-05 E. R. Squibb & Sons, Inc. 1-substituted-1,4,7-triscarboxymethyl-1,4,7,10-tetraazacyclododecane and analogs
US5021556A (en) 1987-07-22 1991-06-04 Neorx Corporation Method of radiolabeling chelating compounds comprising sulfur atoms with metal radionuclides
US5075099A (en) 1988-05-31 1991-12-24 Neorx Corporation Metal radionuclide chelating compounds for improved chelation kinetics
US5364613A (en) 1989-04-07 1994-11-15 Sieving Paul F Polychelants containing macrocyclic chelant moieties
US5367080A (en) 1990-11-08 1994-11-22 Sterling Winthrop Inc. Complexing agents and targeting radioactive immunoreagents useful in therapeutic and diagnostic imaging compositions and methods
US5965107A (en) 1992-03-13 1999-10-12 Diatide, Inc. Technetium-99m labeled peptides for imaging
US5886142A (en) 1997-05-20 1999-03-23 Thomas Jefferson University Radiolabeled thrombus imaging agents
ATE357509T1 (de) 1997-09-29 2007-04-15 Point Therapeutics Inc Stimulierung von hämatopoietischen zellen im vitro
EP0953639A1 (en) 1998-04-30 1999-11-03 Boehringer Ingelheim International GmbH FAPalpha-specific antibody with improved producibility
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
EP1268550A2 (en) 2000-03-17 2003-01-02 Boehringer Ingelheim Pharma KG Human fap-alpha-specific antibodies
EP1452868A2 (en) * 2003-02-27 2004-09-01 Pepscan Systems B.V. Method for selecting a candidate drug compound
US7374898B2 (en) * 2004-10-12 2008-05-20 The Research Foundation Of State University Of New York Peptide inhibitors against seprase
US7399869B2 (en) 2005-05-19 2008-07-15 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
US8933201B2 (en) 2006-06-07 2015-01-13 The Board Of Regents Of The University Of Oklahoma Substrates and inhibitors of antiplasmin cleaving enzyme and fibroblast activation protein and methods of use
WO2008116054A1 (en) 2007-03-20 2008-09-25 Trustees Of Tufts College Inhibitors of fibroblast activation protein, and methods of use thereof
EP2100900A1 (en) 2008-03-07 2009-09-16 Universitätsspital Basel Bombesin analog peptide antagonist conjugates
WO2010036814A1 (en) 2008-09-25 2010-04-01 Molecular Insight Pharmaceuticals, Inc. Selective seprase inhibitors
CA2776037A1 (en) 2009-10-02 2011-04-07 Ludwig Institute For Cancer Research Ltd Anti-fibroblast activation protein antibodies and methods and uses thereof
CA2806021C (en) 2010-08-13 2019-05-21 Roche Glycart Ag Anti-fap antibodies and methods of use
WO2013107820A1 (en) 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
BR112014022435B1 (pt) * 2012-03-21 2023-02-14 Takeda Pharmaceutical Company Limited Inibidores de tfpi e métodos de uso
UA118028C2 (uk) 2013-04-03 2018-11-12 Рош Глікарт Аг Біспецифічне антитіло, специфічне щодо fap і dr5, антитіло, специфічне щодо dr5, і спосіб їх застосування
GB201402006D0 (en) 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
RU2743781C2 (ru) * 2014-06-10 2021-02-25 3Б Фармасьютикалз Гмбх Конъюгат, содержащий лиганд рецепторов нейротензина, и его применение
WO2016146174A1 (en) * 2015-03-17 2016-09-22 Biontech Ag Compositions and methods for diagnosis and treatment of cancer
WO2017127007A1 (en) * 2016-01-20 2017-07-27 Poypeptide Laboratories Holding (Ppl) Ab METHOD FOR PREPARATION OF PEPTIDES WITH psWANG LINKER
CN109689115A (zh) 2016-06-10 2019-04-26 拜耳制药股份公司 放射性药物配合物
CN105949282B (zh) * 2016-06-20 2020-06-16 郑州大学 一种靶向fap的抗血管生成肽z-gp-v2及其应用
CN106046121B (zh) * 2016-06-20 2020-06-16 郑州大学 一种靶向fap的抗血管生成肽z-gp-v1及其应用
JP2018035137A (ja) 2016-07-13 2018-03-08 マブイミューン ダイアグノスティックス エイジーＭａｂｉｍｍｕｎｅ Ｄｉａｇｎｏｓｔｉｃｓ Ａｇ 新規な抗線維芽細胞活性化タンパク質（ｆａｐ）結合薬剤およびその使用
EA202090776A1 (ru) 2017-10-23 2020-07-27 Дзе Джонс Хопкинс Юниверсити Визуализирующие и радиотерапевтические агенты, нацеленные на фибробласт-активирующий белок-альфа (fapalpha)
FI3997103T3 (fi) * 2019-07-08 2025-02-03 3B Pharmaceuticals Gmbh Fibroblastien aktivaatioproteiinin ligandia käsittäviä yhdisteitä ja niiden käyttö

Also Published As

Publication number Publication date
CN118955620A (zh) 2024-11-15
EP3997104A1 (en) 2022-05-18
IL289673A (en) 2022-03-01
MX2022000251A (es) 2022-02-21
IL324399A (en) 2026-01-01
CA3145872A1 (en) 2021-01-14
KR20220032078A (ko) 2022-03-15
CL2022000016A1 (es) 2022-08-19
CN114341158A (zh) 2022-04-12
IL289673B1 (en) 2025-12-01
US20220315554A1 (en) 2022-10-06
AU2020309161A1 (en) 2022-01-27
JP2026062901A (ja) 2026-04-10
JP7801207B2 (ja) 2026-01-16
BR112022000144A2 (pt) 2022-02-22
CN114341158B (zh) 2024-08-06
WO2021005131A1 (en) 2021-01-14
CN118930608A (zh) 2024-11-12
JP2022541752A (ja) 2022-09-27

Similar Documents

Publication Publication Date Title
IL289673B2 (en) Compounds comprising a protein ligand for fibroblast activation and their use
SI3997103T1 (sl) Spojine, ki obsegajo ligand proteina za aktiviranje fibroblastov in uporaba le teh
IL320762A (en) Fibrous binders and their use
SG11202100931QA (en) Muscle-targeting complexes and uses thereof
IL290089A (en) Heterotandem bicyclic peptide complexes
SI4464721T1 (sl) Heterotandemski biciklični peptidni kompleksi
GB2603645B (en) Polypeptides having anti-senescent effects and uses thereof
IL287782A (en) 33cd-binding polypeptides and their uses
EP3988090A4 (en) LIGAND COMPOUND OF P62 AND ITS RE-PHAGIC PROMOTING USE
GB2600564B (en) A fusion protein comprising IL13
GB2600592B (en) Polypeptide and use thereof
IL289390A (en) peptide-mhc complexes
EP3882263A4 (en) GLUCAGON DERIVED PEPTIDE AND USE THEREOF
PL3847011T3 (pl) Laminowana tuba i jej wdrożenia
GB201900253D0 (en) Catalysts and uses thereof
PT3997103T (pt) Compostos que compreendem um ligando da proteína de ativação de fibroblastos e sua utilização
EP3947418C0 (en) PEPTIDES AND THEIR USE
HK40067286A (en) Compounds comprising a fibroblast activation protein ligand and use thereof
GB2588174B (en) A jig and use thereof
EP3696187A4 (en) SYNTHETIC PEPTIDE SP4 AND ITS USE
HK40094265A (en) Compounds comprising a fibroblast activation protein ligand and use thereof
HK40068857A (en) Fibroblast activation protein binding agents and use thereof
HK40043584A (en) Fibroblast binding agents and use thereof
GB201819307D0 (en) Prophyrin complexes and use thereof
IL290844A (en) Antifibrotic compounds and their uses