JPWO2021005125A5 - - Google Patents
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- JPWO2021005125A5 JPWO2021005125A5 JP2022501192A JP2022501192A JPWO2021005125A5 JP WO2021005125 A5 JPWO2021005125 A5 JP WO2021005125A5 JP 2022501192 A JP2022501192 A JP 2022501192A JP 2022501192 A JP2022501192 A JP 2022501192A JP WO2021005125 A5 JPWO2021005125 A5 JP WO2021005125A5
- Authority
- JP
- Japan
- Prior art keywords
- solvate
- acceptable salt
- cancer
- compound
- pharmaceutically acceptable
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 53
- 201000010099 disease Diseases 0.000 claims description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 21
- 239000000203 mixture Substances 0.000 claims description 15
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 238000000746 purification Methods 0.000 claims description 2
- 230000005855 radiation Effects 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims 26
- 239000012453 solvate Substances 0.000 claims 26
- 206010028980 Neoplasm Diseases 0.000 claims 15
- 150000004697 chelate complex Chemical class 0.000 claims 6
- 210000002950 fibroblast Anatomy 0.000 claims 6
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 claims 4
- 230000004913 activation Effects 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- 102000004169 proteins and genes Human genes 0.000 claims 4
- 108090000623 proteins and genes Proteins 0.000 claims 4
- 208000035269 cancer or benign tumor Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010027406 Mesothelioma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 239000002738 chelating agent Substances 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 2
- 201000011519 neuroendocrine tumor Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 210000001519 tissue Anatomy 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims 1
- 206010061934 Salivary gland cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 1
- 238000002372 labelling Methods 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002025 prostate sarcoma Diseases 0.000 claims 1
- 201000001513 prostate squamous cell carcinoma Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 11
- 238000003745 diagnosis Methods 0.000 description 4
- 239000000463 material Substances 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024221293A JP7783396B2 (ja) | 2019-07-08 | 2024-12-18 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
| JP2025203677A JP2026035703A (ja) | 2019-07-08 | 2025-11-26 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
Applications Claiming Priority (5)
| 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 |
| EP19000325.1 | 2019-07-08 | ||
| EP19198813.8 | 2019-09-20 | ||
| EP19198813 | 2019-09-20 | ||
| PCT/EP2020/069298 WO2021005125A1 (en) | 2019-07-08 | 2020-07-08 | Compounds comprising a fibroblast activation protein ligand and use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024221293A Division JP7783396B2 (ja) | 2019-07-08 | 2024-12-18 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022541753A JP2022541753A (ja) | 2022-09-27 |
| JP2022541753A5 JP2022541753A5 (https=) | 2024-04-02 |
| JPWO2021005125A5 true JPWO2021005125A5 (https=) | 2024-04-02 |
| JP7608425B2 JP7608425B2 (ja) | 2025-01-06 |
Family
ID=71409439
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022501192A Active JP7608425B2 (ja) | 2019-07-08 | 2020-07-08 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
| JP2024221293A Active JP7783396B2 (ja) | 2019-07-08 | 2024-12-18 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
| JP2025203677A Pending JP2026035703A (ja) | 2019-07-08 | 2025-11-26 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024221293A Active JP7783396B2 (ja) | 2019-07-08 | 2024-12-18 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
| JP2025203677A Pending JP2026035703A (ja) | 2019-07-08 | 2025-11-26 | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US12427210B2 (https=) |
| EP (2) | EP3997103B9 (https=) |
| JP (3) | JP7608425B2 (https=) |
| KR (1) | KR20220032079A (https=) |
| CN (3) | CN118406106A (https=) |
| AU (1) | AU2020310538B2 (https=) |
| BR (1) | BR112022000122A2 (https=) |
| CA (1) | CA3145340A1 (https=) |
| CL (1) | CL2021003580A1 (https=) |
| DK (1) | DK3997103T3 (https=) |
| ES (1) | ES3012534T3 (https=) |
| FI (1) | FI3997103T3 (https=) |
| HU (1) | HUE070009T2 (https=) |
| IL (2) | IL320543A (https=) |
| LT (1) | LT3997103T (https=) |
| MX (1) | MX2022000252A (https=) |
| PL (1) | PL3997103T3 (https=) |
| RS (1) | RS66480B9 (https=) |
| SI (1) | SI3997103T1 (https=) |
| WO (1) | WO2021005125A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL289673B2 (en) * | 2019-07-08 | 2026-04-01 | 3B Pharmaceuticals Gmbh | Compounds comprising a protein ligand for fibroblast activation and their use |
| 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 |
| EP4251639A1 (en) * | 2020-11-30 | 2023-10-04 | Rayzebio, Inc. | Radiopharmaceutical conjugate compositions and uses thereof |
| US20240139350A1 (en) * | 2021-02-01 | 2024-05-02 | Five Eleven Pharma, Inc | Radioactively labeled ligand for fibroblast activation protein-alpha imaging agent and preparation method therefor |
| 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 |
| NZ803235A (en) | 2021-02-10 | 2026-01-30 | Yantai Lannacheng Biotechnology Co Ltd | Truncated evans blue modified fibroblast activation protein inhibitor, preparation method therefor, and application thereof |
| GB202109922D0 (en) | 2021-07-09 | 2021-08-25 | Blue Earth Diagnostics Ltd | Radiotracers and therapeutics binding to fibroblast activation protein (fap) |
| EP4475900A1 (en) | 2022-02-09 | 2024-12-18 | Novartis AG | Pharmaceutical compositions comprising a 225-actinium-labelled complex and a bismuth sequestering agent |
| EP4282439A1 (en) | 2022-05-23 | 2023-11-29 | Erasmus University Rotterdam Medical Center | Radioisotope labeled sstr2-agonists with linkers |
| CN115304582B (zh) * | 2022-07-20 | 2023-05-12 | 北京法伯新天医药科技有限公司 | FAP-α特异性肿瘤诊断显像剂 |
| EP4311557A1 (en) * | 2022-07-26 | 2024-01-31 | Oncomatryx Biopharma, S.L. | Fap-targeted antibody-drug conjugates |
| JP2025530229A (ja) * | 2022-09-07 | 2025-09-11 | ３ベー ファーマシューティカルズ ゲーエムベーハー | 前立腺特異的膜抗原（ｐｓｍａ）リガンドおよびその使用 |
| EP4342890A1 (en) | 2022-09-21 | 2024-03-27 | Erasmus University Rotterdam Medical Center | Platform and scaffold for fap targeting agents |
| 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 |
| KR20260009883A (ko) | 2023-05-24 | 2026-01-20 | 베이징 창핑 래보러토리 | 신규 삼관능 화합물 및 이의 용도 |
| TW202502800A (zh) * | 2023-07-11 | 2025-01-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種成纖維細胞活化蛋白配體及其用途 |
| 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 |
| 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 |
| TW202532108A (zh) | 2024-02-01 | 2025-08-16 | 瑞士商諾華公司 | 治療癌症的方法 |
| CN121045338A (zh) * | 2025-11-05 | 2025-12-02 | 原子高科股份有限公司 | 一种靶向caix的环肽及其制备方法与应用 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2304206A1 (en) | 1997-09-29 | 1999-04-08 | Point Therapeutics, Inc. | Stimulation of hematopoietic cells in 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 |
| JP2003530092A (ja) | 2000-03-17 | 2003-10-14 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | ヒトＦＡＰ−α−特異抗体 |
| 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 |
| EP1943257A2 (en) | 2005-05-19 | 2008-07-16 | 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 |
| WO2010036814A1 (en) | 2008-09-25 | 2010-04-01 | Molecular Insight Pharmaceuticals, Inc. | Selective seprase inhibitors |
| WO2010071894A2 (en) | 2008-12-19 | 2010-06-24 | Baxter International Inc. | Tfpi inhibitors and methods of use |
| EP2483316A1 (en) | 2009-10-02 | 2012-08-08 | Ludwig Institute for Cancer Research Ltd. | Anti-fibroblast activation protein antibodies and methods and uses thereof |
| AU2011227714B2 (en) | 2010-03-19 | 2014-09-04 | Takeda Pharmaceutical Company Limited | TFPI inhibitors and methods of use |
| HUE036077T2 (hu) | 2010-08-13 | 2018-06-28 | Roche Glycart Ag | Anti-FAP ellenanyagok és alkalmazásukra szolgáló eljárások |
| WO2013107820A1 (en) | 2012-01-17 | 2013-07-25 | Universiteit Antwerpen | Novel fap inhibitors |
| WO2013141965A1 (en) | 2012-03-21 | 2013-09-26 | Baxter International Inc. | Tfpi inhibitors and methods of use |
| EP2740726A1 (en) | 2012-12-07 | 2014-06-11 | 3B Pharmaceuticals GmbH | Neurotensin receptor ligands |
| 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 |
| CN106794264B (zh) | 2014-06-10 | 2021-03-23 | 3B制药有限公司 | 包含神经降压肽受体配体的缀合物及其用途 |
| EP2954933A1 (en) | 2014-06-10 | 2015-12-16 | 3B Pharmaceuticals GmbH | Conjugate comprising a neurotensin receptor ligand |
| WO2016146174A1 (en) | 2015-03-17 | 2016-09-22 | Biontech Ag | Compositions and methods for diagnosis and treatment of cancer |
| EP3405476B1 (en) | 2016-01-20 | 2022-05-18 | Polypeptide Laboratories Holding (PPL) AB | METHOD FOR PREPARATION OF PEPTIDES WITH psWANG LINKER |
| WO2017211809A1 (en) | 2016-06-10 | 2017-12-14 | Bayer Pharma Aktiengesellschaft | Radio-pharmaceutical complexes |
| 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 |
| 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 |
| 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 |
| 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) |
| IL289673B2 (en) | 2019-07-08 | 2026-04-01 | 3B Pharmaceuticals Gmbh | Compounds comprising a protein ligand for fibroblast activation and their use |
| 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 |
-
2020
- 2020-07-08 CN CN202410413792.9A patent/CN118406106A/zh active Pending
- 2020-07-08 FI FIEP20735646.0T patent/FI3997103T3/fi active
- 2020-07-08 WO PCT/EP2020/069298 patent/WO2021005125A1/en not_active Ceased
- 2020-07-08 EP EP20735646.0A patent/EP3997103B9/en active Active
- 2020-07-08 RS RS20250117A patent/RS66480B9/sr unknown
- 2020-07-08 IL IL320543A patent/IL320543A/en unknown
- 2020-07-08 PL PL20735646.0T patent/PL3997103T3/pl unknown
- 2020-07-08 LT LTEPPCT/EP2020/069298T patent/LT3997103T/lt unknown
- 2020-07-08 IL IL289675A patent/IL289675B2/en unknown
- 2020-07-08 HU HUE20735646A patent/HUE070009T2/hu unknown
- 2020-07-08 DK DK20735646.0T patent/DK3997103T3/da active
- 2020-07-08 SI SI202030573T patent/SI3997103T1/sl unknown
- 2020-07-08 US US17/625,139 patent/US12427210B2/en active Active
- 2020-07-08 BR BR112022000122A patent/BR112022000122A2/pt unknown
- 2020-07-08 CN CN202080062650.2A patent/CN114341159B/zh active Active
- 2020-07-08 ES ES20735646T patent/ES3012534T3/es active Active
- 2020-07-08 JP JP2022501192A patent/JP7608425B2/ja active Active
- 2020-07-08 MX MX2022000252A patent/MX2022000252A/es unknown
- 2020-07-08 EP EP24213879.0A patent/EP4517326A3/en active Pending
- 2020-07-08 AU AU2020310538A patent/AU2020310538B2/en active Active
- 2020-07-08 KR KR1020227004043A patent/KR20220032079A/ko active Pending
- 2020-07-08 CA CA3145340A patent/CA3145340A1/en active Pending
- 2020-07-08 CN CN202410413789.7A patent/CN118388588A/zh active Pending
-
2021
- 2021-12-30 CL CL2021003580A patent/CL2021003580A1/es unknown
-
2024
- 2024-12-18 JP JP2024221293A patent/JP7783396B2/ja active Active
-
2025
- 2025-11-18 US US19/392,245 patent/US20260061086A1/en active Pending
- 2025-11-26 JP JP2025203677A patent/JP2026035703A/ja active Pending
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