BR112022019121A2 - Agentes de imageamento e produtos radiofarmacêuticos direcionados a fap e usos dos mesmos - Google Patents
Agentes de imageamento e produtos radiofarmacêuticos direcionados a fap e usos dos mesmosInfo
- Publication number
- BR112022019121A2 BR112022019121A2 BR112022019121A BR112022019121A BR112022019121A2 BR 112022019121 A2 BR112022019121 A2 BR 112022019121A2 BR 112022019121 A BR112022019121 A BR 112022019121A BR 112022019121 A BR112022019121 A BR 112022019121A BR 112022019121 A2 BR112022019121 A2 BR 112022019121A2
- Authority
- BR
- Brazil
- Prior art keywords
- fap
- imaging agents
- cancer
- products directed
- radiopharmaceutical products
- Prior art date
Links
- 239000012216 imaging agent Substances 0.000 title abstract 3
- 239000012217 radiopharmaceutical Substances 0.000 title abstract 3
- 229940121896 radiopharmaceutical Drugs 0.000 title abstract 3
- 230000002799 radiopharmaceutical effect Effects 0.000 title abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 5
- 201000011510 cancer Diseases 0.000 abstract 3
- 210000002950 fibroblast Anatomy 0.000 abstract 2
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 208000029742 colonic neoplasm Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037828 epithelial carcinoma Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000010837 poor prognosis Methods 0.000 abstract 1
- 150000003384 small molecules Chemical class 0.000 abstract 1
- 210000002536 stromal cell Anatomy 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/0002—General or multifunctional contrast agents, e.g. chelated agents
-
- 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
- A61K49/00—Preparations for testing in vivo
- A61K49/001—Preparation for luminescence or biological staining
- A61K49/006—Biological staining of tissues in vivo, e.g. methylene blue or toluidine blue O administered in the buccal area to detect epithelial cancer cells, dyes used for delineating tissues during surgery
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biodiversity & Conservation Biology (AREA)
- Oncology (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Enzymes And Modification Thereof (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
AGENTES DE IMAGEAMENTO E PRODUTOS RADIOFARMACÊUTICOS DIRECIONADOS A FAP E USOS DOS MESMOS. O estroma tumoral, responsável por grande parte da massa tumoral, representa um alvo atraente para a liberação de compostos diagnósticos e terapêuticos. Nesse documento, o foco está notavelmente em uma subpopulação de células estromais, conhecidas como fibroblastos associados ao câncer, que estão presentes em mais de 90% dos carcinomas epiteliais, incluindo câncer de pâncreas, cólon e mama. Os fibroblastos associados ao câncer apresentam alta expressão de FAP, que não é detectável em tecido normal adulto, mas está associado a um prognóstico ruim em pacientes com câncer. A presente invenção fornece agentes radiofarmacêuticos e de imageamento de moléculas pequenas com base em um inibidor específico de FAP.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062993874P | 2020-03-24 | 2020-03-24 | |
| PCT/US2021/023862 WO2021195198A1 (en) | 2020-03-24 | 2021-03-24 | Fap-targeted radiopharmaceuticals and imaging agents, and uses related thereto |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112022019121A2 true BR112022019121A2 (pt) | 2023-02-14 |
Family
ID=77890585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022019121A BR112022019121A2 (pt) | 2020-03-24 | 2021-03-24 | Agentes de imageamento e produtos radiofarmacêuticos direcionados a fap e usos dos mesmos |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11707539B2 (pt) |
| EP (1) | EP4126053A1 (pt) |
| JP (1) | JP2023519247A (pt) |
| KR (1) | KR20220158038A (pt) |
| CN (1) | CN115697413A (pt) |
| AU (1) | AU2021244541A1 (pt) |
| BR (1) | BR112022019121A2 (pt) |
| CA (1) | CA3171183A1 (pt) |
| CL (1) | CL2022002603A1 (pt) |
| CO (1) | CO2022014985A2 (pt) |
| IL (1) | IL296658A (pt) |
| MX (1) | MX2022011842A (pt) |
| PE (1) | PE20230490A1 (pt) |
| TW (1) | TW202202150A (pt) |
| WO (1) | WO2021195198A1 (pt) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023519247A (ja) | 2020-03-24 | 2023-05-10 | トラスティーズ オブ タフツ カレッジ | Ｆａｐ標的化放射性医薬品およびイメージング剤、ならびにそれらに関連する使用 |
| MX2021005089A (es) * | 2021-04-30 | 2022-11-01 | Instituto Nac De Investigaciones Nucleares | Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos. |
| WO2023069711A1 (en) * | 2021-10-22 | 2023-04-27 | Trustees Of Tufts College | Fap-targeted neutron capture agents, and uses and formulations related thereto |
| CN114149489B (zh) * | 2021-11-18 | 2023-12-15 | 厦门大学 | 一种靶向tigit的放射性标记化合物及其制备方法和应用 |
| CN115838393B (zh) * | 2023-02-16 | 2023-05-05 | 烟台蓝纳成生物技术有限公司 | 用于fapi合成的中间体及其制备方法和应用 |
| CN116120290A (zh) * | 2023-03-01 | 2023-05-16 | 广东药科大学附属第一医院 | 一种靶向成纤维细胞激活蛋白的mr探针的制备方法 |
| CN118619941A (zh) * | 2023-03-03 | 2024-09-10 | 晶核生物医药科技(南京)有限公司 | 一种含氮杂环类化合物及其制备方法与用途 |
| CN116650679A (zh) * | 2023-04-14 | 2023-08-29 | 河北医科大学第四医院 | 一种靶向fgfr1的影像探针及其应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7399869B2 (en) * | 2005-05-19 | 2008-07-15 | Genentech, Inc. | Fibroblast activation protein inhibitor compounds and methods |
| AU2006264305B2 (en) | 2005-07-05 | 2012-07-05 | Trustees Of Tufts College | Inhibitors of fibroblast activation protein alpha |
| RU2011116223A (ru) * | 2008-09-25 | 2012-10-27 | Моликьюлар Инсайт Фармасьютикалз, Инк. (Us) | Селективные ингибиторы сепразы |
| EP3102242A2 (en) | 2014-02-03 | 2016-12-14 | Philochem AG | Targeted drug conjugates |
| EP3555627B1 (en) * | 2016-12-14 | 2023-11-22 | Purdue Research Foundation | Fibroblast activation protein (fap)-targeted imaging and therapy |
| AU2019360944B2 (en) | 2018-10-17 | 2022-09-29 | Purdue Research Foundation | Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis |
| JP2023519247A (ja) | 2020-03-24 | 2023-05-10 | トラスティーズ オブ タフツ カレッジ | Ｆａｐ標的化放射性医薬品およびイメージング剤、ならびにそれらに関連する使用 |
-
2021
- 2021-03-24 JP JP2022557768A patent/JP2023519247A/ja active Pending
- 2021-03-24 CN CN202180037504.9A patent/CN115697413A/zh active Pending
- 2021-03-24 KR KR1020227036805A patent/KR20220158038A/ko unknown
- 2021-03-24 AU AU2021244541A patent/AU2021244541A1/en active Pending
- 2021-03-24 MX MX2022011842A patent/MX2022011842A/es unknown
- 2021-03-24 TW TW110110644A patent/TW202202150A/zh unknown
- 2021-03-24 EP EP21775253.4A patent/EP4126053A1/en active Pending
- 2021-03-24 IL IL296658A patent/IL296658A/en unknown
- 2021-03-24 WO PCT/US2021/023862 patent/WO2021195198A1/en active Application Filing
- 2021-03-24 PE PE2022002065A patent/PE20230490A1/es unknown
- 2021-03-24 US US17/211,481 patent/US11707539B2/en active Active
- 2021-03-24 BR BR112022019121A patent/BR112022019121A2/pt unknown
- 2021-03-24 CA CA3171183A patent/CA3171183A1/en active Pending
-
2022
- 2022-09-23 CL CL2022002603A patent/CL2022002603A1/es unknown
- 2022-10-21 CO CONC2022/0014985A patent/CO2022014985A2/es unknown
- 2022-11-18 US US17/990,347 patent/US20230330275A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CN115697413A (zh) | 2023-02-03 |
| PE20230490A1 (es) | 2023-03-23 |
| CA3171183A1 (en) | 2021-09-30 |
| IL296658A (en) | 2022-11-01 |
| JP2023519247A (ja) | 2023-05-10 |
| KR20220158038A (ko) | 2022-11-29 |
| US11707539B2 (en) | 2023-07-25 |
| CL2022002603A1 (es) | 2023-05-26 |
| AU2021244541A1 (en) | 2022-10-13 |
| US20220370647A1 (en) | 2022-11-24 |
| TW202202150A (zh) | 2022-01-16 |
| CO2022014985A2 (es) | 2022-12-30 |
| US20230330275A1 (en) | 2023-10-19 |
| EP4126053A1 (en) | 2023-02-08 |
| MX2022011842A (es) | 2022-10-20 |
| WO2021195198A1 (en) | 2021-09-30 |
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