JP2022514352A - 線維芽細胞活性化タンパク質の阻害剤 - Google Patents

線維芽細胞活性化タンパク質の阻害剤 Download PDF

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JP2022514352A
JP2022514352A JP2021535552A JP2021535552A JP2022514352A JP 2022514352 A JP2022514352 A JP 2022514352A JP 2021535552 A JP2021535552 A JP 2021535552A JP 2021535552 A JP2021535552 A JP 2021535552A JP 2022514352 A JP2022514352 A JP 2022514352A
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cyano
mmol
quinoline
oxoethyl
difluoropyrrolidin
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JP2022514352A5 (https=
Inventor
プジャラ，ブラーマム
パンパティル，ダヤナンド
ベルナレス，セバスチャン
ベルマール，セバスチャン
ディアズ，ゴンザロ アンドレ ウレタ
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プラクシス バイオテック エルエルシー
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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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2021535552A 2018-12-21 2019-12-21 線維芽細胞活性化タンパク質の阻害剤 Pending JP2022514352A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862784291P 2018-12-21 2018-12-21
US62/784,291 2018-12-21
US201962863853P 2019-06-19 2019-06-19
US62/863,853 2019-06-19
PCT/US2019/068189 WO2020132661A2 (en) 2018-12-21 2019-12-21 Inhibitors of fibroblast activation protein

Publications (2)

Publication Number Publication Date
JP2022514352A true JP2022514352A (ja) 2022-02-10
JP2022514352A5 JP2022514352A5 (https=) 2022-12-28

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US (2) US11504364B2 (https=)
EP (1) EP3898654A4 (https=)
JP (1) JP2022514352A (https=)
CN (1) CN113811529A (https=)
WO (1) WO2020132661A2 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022516555A (ja) * 2019-01-04 2022-02-28 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤

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US11780821B2 (en) 2017-12-15 2023-10-10 Praxis Biotech LLC Inhibitors of fibroblast activation protein
EP4096677A4 (en) * 2020-01-31 2024-02-28 Purdue Research Foundation Fibroblast activation protein (fap) - targeted antifibrotic therapy
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
CN114380795A (zh) * 2020-10-22 2022-04-22 四川大学华西医院 氘代fap抑制剂及其应用
CN114621155A (zh) * 2020-12-14 2022-06-14 四川科伦药物研究院有限公司 一种制备卡马替尼的方法
EP4263535A1 (en) * 2020-12-17 2023-10-25 Astrazeneca AB N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)- quinoline-4-carboxamides
EP4122499A1 (en) * 2021-07-23 2023-01-25 3B Pharmaceuticals GmbH Fibroblast activation protein inhibitors and use thereof
WO2023233023A1 (en) 2022-06-03 2023-12-07 Universiteit Antwerpen Inhibitors of fibroblast activation protein
IL317722A (en) * 2022-06-21 2025-02-01 Astrazeneca Ab Solid state forms of N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)-6-morpholinoquinoline-4-carboxamide
JP2025525344A (ja) * 2022-06-21 2025-08-05 アストラゼネカ・アクチエボラーグ Ｎ－（２－（４－シアノチアゾリジン－３－イル）－２－オキソエチル）－キノリン－４－カルボキサミド
EP4543869A1 (en) * 2022-06-21 2025-04-30 Astrazeneca AB N-(2-(3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)- quinoline-4-carboxamides
WO2025037000A1 (en) 2023-08-17 2025-02-20 Universiteit Antwerpen Novel fibroblast activation protein inhibitors and medical uses thereof
WO2025046043A1 (en) 2023-08-31 2025-03-06 Stichting Radboud Universitair Medisch Centrum Endometriosis tracer
WO2025106939A1 (en) * 2023-11-16 2025-05-22 Praxis Biotech LLC Conjugates targeting fibroblast activation protein and uses thereof
WO2025106926A1 (en) * 2023-11-16 2025-05-22 Praxis Biotech LLC Conjugates targeting fibroblast activation protein and uses thereof
CN120400145A (zh) * 2025-04-03 2025-08-01 江南大学 基因fap在制备非酒精性脂肪型肝炎的药物中的应用

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JP2021506972A (ja) * 2017-12-15 2021-02-22 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤

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WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
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US8338450B2 (en) 2007-09-21 2012-12-25 Lupin Limited Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors
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WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
JP2021506972A (ja) * 2017-12-15 2021-02-22 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤

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Publication number Priority date Publication date Assignee Title
JP2022516555A (ja) * 2019-01-04 2022-02-28 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤

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US20200206216A1 (en) 2020-07-02
EP3898654A4 (en) 2022-10-26
WO2020132661A2 (en) 2020-06-25
CN113811529A (zh) 2021-12-17
US20230144841A1 (en) 2023-05-11
EP3898654A2 (en) 2021-10-27
US11504364B2 (en) 2022-11-22
WO2020132661A3 (en) 2020-07-30

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