JP6744826B2 - Fap活性化治療剤及びそれに関連する使用 - Google Patents
Fap活性化治療剤及びそれに関連する使用 Download PDFInfo
- Publication number
- JP6744826B2 JP6744826B2 JP2016572687A JP2016572687A JP6744826B2 JP 6744826 B2 JP6744826 B2 JP 6744826B2 JP 2016572687 A JP2016572687 A JP 2016572687A JP 2016572687 A JP2016572687 A JP 2016572687A JP 6744826 B2 JP6744826 B2 JP 6744826B2
- Authority
- JP
- Japan
- Prior art keywords
- prodrug
- fap
- pharmaceutically acceptable
- alkyl
- certain embodiments
- 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.)
- Expired - Fee Related
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/69—Boron compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/54—Medicinal 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/62—Medicinal 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 a protein, peptide or polyamino acid
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462011989P | 2014-06-13 | 2014-06-13 | |
| US62/011,989 | 2014-06-13 | ||
| US201462051033P | 2014-09-16 | 2014-09-16 | |
| US62/051,033 | 2014-09-16 | ||
| PCT/US2015/035798 WO2015192123A1 (en) | 2014-06-13 | 2015-06-15 | Fap-activated therapeutic agents, and uses related thereto |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020130483A Division JP7093912B2 (ja) | 2014-06-13 | 2020-07-31 | Fap活性化治療剤及びそれに関連する使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017519753A JP2017519753A (ja) | 2017-07-20 |
| JP2017519753A5 JP2017519753A5 (enExample) | 2018-02-01 |
| JP6744826B2 true JP6744826B2 (ja) | 2020-08-19 |
Family
ID=54834485
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016572687A Expired - Fee Related JP6744826B2 (ja) | 2014-06-13 | 2015-06-15 | Fap活性化治療剤及びそれに関連する使用 |
| JP2020130483A Active JP7093912B2 (ja) | 2014-06-13 | 2020-07-31 | Fap活性化治療剤及びそれに関連する使用 |
| JP2022086532A Active JP7530111B2 (ja) | 2014-06-13 | 2022-05-27 | Fap活性化治療剤及びそれに関連する使用 |
| JP2024115840A Pending JP2024150608A (ja) | 2014-06-13 | 2024-07-19 | Fap活性化治療剤及びそれに関連する使用 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020130483A Active JP7093912B2 (ja) | 2014-06-13 | 2020-07-31 | Fap活性化治療剤及びそれに関連する使用 |
| JP2022086532A Active JP7530111B2 (ja) | 2014-06-13 | 2022-05-27 | Fap活性化治療剤及びそれに関連する使用 |
| JP2024115840A Pending JP2024150608A (ja) | 2014-06-13 | 2024-07-19 | Fap活性化治療剤及びそれに関連する使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (6) | US10245248B2 (enExample) |
| EP (2) | EP3154594B1 (enExample) |
| JP (4) | JP6744826B2 (enExample) |
| CN (4) | CN113786495A (enExample) |
| CA (1) | CA2952051C (enExample) |
| DK (1) | DK3154594T3 (enExample) |
| ES (1) | ES2951596T3 (enExample) |
| FI (1) | FI3154594T3 (enExample) |
| HR (1) | HRP20230854T1 (enExample) |
| HU (1) | HUE063194T2 (enExample) |
| IL (2) | IL249370B (enExample) |
| PL (1) | PL3154594T3 (enExample) |
| PT (1) | PT3154594T (enExample) |
| SI (1) | SI3154594T1 (enExample) |
| WO (1) | WO2015192123A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020183448A (ja) * | 2014-06-13 | 2020-11-12 | バック バイオサイエンシーズ, エルエルシーBach BioSciences, LLC | Fap活性化治療剤及びそれに関連する使用 |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| WO2017189569A1 (en) * | 2016-04-25 | 2017-11-02 | Trustees Of Tufts College | Multimediator dpp4 and fap inhibitors, and uses related thereto |
| MX2019004950A (es) | 2016-10-28 | 2019-09-26 | Icahn School Med Mount Sinai | Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2. |
| CA3045037A1 (en) | 2016-12-08 | 2018-06-14 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating cdk4/6-mediated cancer |
| CN110291401B (zh) | 2016-12-14 | 2023-04-11 | 普渡研究基金会 | 成纤维细胞活化蛋白(fap)-靶向成像和治疗 |
| ES2894106T3 (es) * | 2017-04-21 | 2022-02-11 | Safe Implant Tech Aps | Partículas de oro para su uso en la terapia para prevenir o reducir la contractura capsular |
| GB201710973D0 (en) | 2017-07-07 | 2017-08-23 | Avacta Life Sciences Ltd | Scaffold proteins |
| WO2019154859A1 (en) * | 2018-02-06 | 2019-08-15 | Universität Heidelberg | Fap inhibitor |
| JP2021515013A (ja) * | 2018-03-06 | 2021-06-17 | アイカーン スクール オブ メディスン アット マウント シナイ | セリンスレオニンキナーゼ(akt)分解/破壊化合物および使用方法 |
| CN108864250A (zh) * | 2018-05-29 | 2018-11-23 | 北京大学 | 一种FAPα酶敏感的吉西他滨前体药物及其制备方法和应用 |
| WO2019236567A2 (en) * | 2018-06-04 | 2019-12-12 | Trustees Of Tufts College | Tumor microenvironment-activated drug-binder conjugated, and uses related thereto |
| WO2019246570A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| AU2019360944B2 (en) * | 2018-10-17 | 2022-09-29 | Purdue Research Foundation | Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis |
| WO2020210337A1 (en) * | 2019-04-09 | 2020-10-15 | Dana-Farber Cancer Institute, Inc. | Degradation of akt by conjugation of atp-competitive akt inhibitor gdc-0068 with e3 ligase ligands and methods of use |
| CN118908962A (zh) | 2019-05-06 | 2024-11-08 | 西奈山伊坎医学院 | 作为hpk1的降解剂的异双功能化合物 |
| WO2021016392A1 (en) * | 2019-07-22 | 2021-01-28 | Purdue Research Foundation | Multivalent fibroblast-targeted agents and methods of use |
| JP7638664B2 (ja) | 2020-01-31 | 2025-03-04 | キヤノン株式会社 | 光電変換装置、光電変換システム、および移動体 |
| CN111233955B (zh) * | 2020-02-28 | 2022-06-10 | 南京缘聚医药科技有限公司 | 一类噻唑酮甲酰胞嘧啶衍生物及其药物用途 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| WO2022026729A1 (en) * | 2020-07-31 | 2022-02-03 | The Johns Hopkins University | Fap-activated compounds for treatment of cancer |
| KR20230141755A (ko) * | 2020-10-30 | 2023-10-10 | 아박타 라이프 사이언시스 리미티드 | 효소 활성화 혈청 반감기 연장된 치료 접합체 |
| WO2022094262A1 (en) * | 2020-10-30 | 2022-05-05 | Avacta Life Sciences Limited | Fap-activated serum extended half-life therapeutic conjugates |
| CN116981479A (zh) * | 2020-12-17 | 2023-10-31 | 塔夫茨大学信托人 | Fap激活的放射治疗诊断法以及与之相关的用途 |
| US20240238458A1 (en) * | 2021-03-16 | 2024-07-18 | Purdue Research Foundation | Compounds targeting fibroblast-activation protein and methods of use thereof |
| CN113018450B (zh) * | 2021-05-24 | 2021-08-06 | 潍坊中医药产业技术研究院 | 一种具有肿瘤细胞和肿瘤相关成纤维细胞双靶向功能的药物载体、制备方法及应用 |
| CN113845563B (zh) * | 2021-09-28 | 2024-02-20 | 遵义医药高等专科学校 | 一种FAPα酶激活式鬼臼毒素衍生物及其制备方法与应用 |
| CN120077031A (zh) | 2022-07-05 | 2025-05-30 | 亚历克斯·祖内克 | 用于多管齐下化疗的前药试剂盒 |
| EP4615521A1 (en) * | 2022-11-09 | 2025-09-17 | Purdue Research Foundation | Keto-amide-based fibroblast activation protein-targeted ligand linked to an imaging or therapeutic agent, compositions and methods of use |
| WO2025159301A1 (ko) * | 2024-01-24 | 2025-07-31 | 서울대학교산학협력단 | 섬유아세포 활성화 단백질에 의해 활성화되는 프로드러그 화합물 |
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| WO2008116053A2 (en) | 2007-03-20 | 2008-09-25 | Trustees Of Tufts College | Fap-activated chemotherapeutic compounds, and methods of use thereof |
| CN108383893A (zh) | 2011-08-30 | 2018-08-10 | 塔夫茨大学信托人 | 用于治疗实体瘤的fap-活化的蛋白酶体抑制剂 |
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| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| CN113786495A (zh) | 2014-06-13 | 2021-12-14 | 塔夫茨大学信托人 | Fap激活的治疗剂以及其相关用途 |
| JP2017529853A (ja) | 2014-09-25 | 2017-10-12 | アムジエン・インコーポレーテツド | プロテアーゼにより活性化可能な二重特異性タンパク質 |
| WO2017173347A1 (en) | 2016-04-01 | 2017-10-05 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Par2 mimetic peptides and uses thereof |
| WO2017189569A1 (en) | 2016-04-25 | 2017-11-02 | Trustees Of Tufts College | Multimediator dpp4 and fap inhibitors, and uses related thereto |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020183448A (ja) * | 2014-06-13 | 2020-11-12 | バック バイオサイエンシーズ, エルエルシーBach BioSciences, LLC | Fap活性化治療剤及びそれに関連する使用 |
| JP7093912B2 (ja) | 2014-06-13 | 2022-07-01 | バック バイオサイエンシーズ,エルエルシー | Fap活性化治療剤及びそれに関連する使用 |
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