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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JPWO2020132661A5 (https=
JP2022514352A5 (https=
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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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (3)

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JP2022514352A true JP2022514352A (ja) 2022-02-10
JPWO2020132661A5 JPWO2020132661A5 (https=) 2022-12-28
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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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
WO2021155292A1 (en) * 2020-01-31 2021-08-05 Philip Stewart Low Fibroblast activation protein (fap) - targeted antifibrotic therapy
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
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
CN116745291A (zh) * 2020-12-17 2023-09-12 阿斯利康(瑞典)有限公司 N-(2-(4-氰基噻唑烷-3-基)-2-氧代乙基)-喹啉-4-甲酰胺
EP4122499A1 (en) * 2021-07-23 2023-01-25 3B Pharmaceuticals GmbH Fibroblast activation protein inhibitors and use thereof
EP4531932A1 (en) 2022-06-03 2025-04-09 Universiteit Antwerpen Inhibitors of fibroblast activation protein
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
WO2023247488A1 (en) * 2022-06-21 2023-12-28 Astrazeneca Ab N-(2-(3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)- quinoline-4-carboxamides
CA3260370A1 (en) * 2022-06-21 2023-12-28 Astrazeneca Ab SOLID FORMS OF N-(2-(4-CYANOTHIAZOLIDIN-3-YL)-2-OXOEETHYL)-6-MORPHOLINOQUINOLEIN-4-CARBOXAMIDE
WO2025037000A1 (en) 2023-08-17 2025-02-20 Universiteit Antwerpen Novel fibroblast activation protein inhibitors and medical uses thereof
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
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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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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WO2004071454A2 (en) * 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
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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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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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EP3898654A2 (en) 2021-10-27
US20200206216A1 (en) 2020-07-02
EP3898654A4 (en) 2022-10-26
US20230144841A1 (en) 2023-05-11
WO2020132661A3 (en) 2020-07-30
CN113811529A (zh) 2021-12-17
WO2020132661A2 (en) 2020-06-25
US11504364B2 (en) 2022-11-22

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