CN113811529A - 成纤维细胞激活蛋白抑制剂 - Google Patents

成纤维细胞激活蛋白抑制剂 Download PDF

Info

Publication number
CN113811529A
CN113811529A CN201980092135.6A CN201980092135A CN113811529A CN 113811529 A CN113811529 A CN 113811529A CN 201980092135 A CN201980092135 A CN 201980092135A CN 113811529 A CN113811529 A CN 113811529A
Authority
CN
China
Prior art keywords
cyano
compound
quinoline
oxoethyl
difluoropyrrolidin
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.)
Pending
Application number
CN201980092135.6A
Other languages
English (en)
Chinese (zh)
Inventor
B·普加拉
D·潘帕蒂尔
S·伯纳勒斯
S·贝尔马尔
G·A·乌拉塔·迪亚兹
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Praxis Biotechnology Co ltd
Praxis Biotech LLC
Original Assignee
Praxis Biotechnology Co ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Praxis Biotechnology Co ltd filed Critical Praxis Biotechnology Co ltd
Publication of CN113811529A publication Critical patent/CN113811529A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • 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)
CN201980092135.6A 2018-12-21 2019-12-21 成纤维细胞激活蛋白抑制剂 Pending CN113811529A (zh)

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 (1)

Publication Number Publication Date
CN113811529A true CN113811529A (zh) 2021-12-17

Family

ID=71101996

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980092135.6A Pending CN113811529A (zh) 2018-12-21 2019-12-21 成纤维细胞激活蛋白抑制剂

Country Status (5)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114126597A (zh) * 2019-01-04 2022-03-01 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂
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

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004071454A2 (en) * 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
WO2007085895A2 (en) * 2005-09-02 2007-08-02 Ferring B.V. Fap inhibitors
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
WO2018111989A1 (en) * 2016-12-14 2018-06-21 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
CN112105354A (zh) * 2017-12-15 2020-12-18 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4357293B2 (ja) 2001-06-27 2009-11-04 スミスクライン ビーチャム コーポレーション ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類
US7399869B2 (en) 2005-05-19 2008-07-15 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
CA2617715A1 (en) 2005-08-11 2007-02-15 F. Hoffmann-La Roche Ag Pharmaceutical composition comprising a dpp-iv inhibitor
CN101230058A (zh) 2007-01-23 2008-07-30 上海恒瑞医药有限公司 双环氮杂烷类衍生物、其制备方法及其在医药上的用途
US8338450B2 (en) 2007-09-21 2012-12-25 Lupin Limited Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors
WO2009116067A2 (en) 2008-01-10 2009-09-24 Sun Pharma Advanced Research Company Limited Novel derivatives of acyl cyanopyrrolidines
WO2010083570A1 (en) 2009-01-23 2010-07-29 The University Of Sydney Novel metabolic disease therapy
EP2730571A1 (en) 2012-11-12 2014-05-14 Universitat De Barcelona 1-[1-(benzoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonitrile derivatives
CA2991628C (en) 2015-07-16 2020-04-07 Bioxcel Therapeutics, Inc. A novel approach for treatment of cancer using immunomodulation
WO2017189569A1 (en) 2016-04-25 2017-11-02 Trustees Of Tufts College Multimediator dpp4 and fap inhibitors, and uses related thereto
JP7071366B2 (ja) 2016-12-14 2022-05-18 メディミューン，エルエルシー 注射情報を取得して送信するための、プランジャロッド内に埋設された多部品センサ
EA202090776A1 (ru) 2017-10-23 2020-07-27 Дзе Джонс Хопкинс Юниверсити Визуализирующие и радиотерапевтические агенты, нацеленные на фибробласт-активирующий белок-альфа (fapalpha)
EP3749663A1 (en) 2018-02-06 2020-12-16 Universität Heidelberg Fap inhibitor
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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004071454A2 (en) * 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
WO2007085895A2 (en) * 2005-09-02 2007-08-02 Ferring B.V. Fap inhibitors
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
WO2018111989A1 (en) * 2016-12-14 2018-06-21 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
CN112105354A (zh) * 2017-12-15 2020-12-18 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KOEN JANSEN等: "Extended Structure−Activity Relationship and Pharmacokinetic Investigation of (4-Quinolinoyl)glycyl-2-cyanopyrrolidine Inhibitors of Fibroblast Activation Protein (FAP)" *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114126597A (zh) * 2019-01-04 2022-03-01 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂
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

Also Published As

Publication number Publication date
US20200206216A1 (en) 2020-07-02
EP3898654A4 (en) 2022-10-26
WO2020132661A2 (en) 2020-06-25
US20230144841A1 (en) 2023-05-11
EP3898654A2 (en) 2021-10-27
US11504364B2 (en) 2022-11-22
WO2020132661A3 (en) 2020-07-30
JP2022514352A (ja) 2022-02-10

Similar Documents

Publication Publication Date Title
CN113811529A (zh) 成纤维细胞激活蛋白抑制剂
US10766881B2 (en) 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
US11780821B2 (en) Inhibitors of fibroblast activation protein
JP3544675B2 (ja) 血管形成阻害活性を有するフタラジン
TWI779022B (zh) Ask1抑制劑化合物及其用途
EP2978752B1 (en) 6-(5-hydroxy-1h-pyrazol-1-yl)nicotinamide derivatives and their use as phd inhibitors
CN114126597A (zh) 成纤维细胞激活蛋白抑制剂
WO2014040549A1 (zh) 炔杂芳环化合物及其应用
WO2024083255A1 (zh) 苄基或噻吩亚甲基取代的氨基喹唑啉衍生物及其作为sos1降解剂的用途
WO2015158310A1 (zh) 一种酪氨酸激酶抑制剂及其用途
CN113454081A (zh) 咪唑并吡啶基化合物及其用于治疗增生性疾病的用途
CN112292374B (zh) 一种新型磷酸肌醇3-激酶抑制剂及其制备方法和用途
WO2019047161A1 (en) IMIDAZOLIDINE COMPOUNDS
CN108191837A (zh) PI3Kα/mTOR双激酶抑制剂及其药物组合物和应用
CN103214481B (zh) 新型咪唑并[1,2-a]吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途
CN114181160A (zh) 含2,4-二苯胺嘧啶酰肼衍生物及其制备方法与应用
CN109666022B (zh) 三氮唑衍生物及其制备方法和用途
CN105541792B (zh) 多环类pi3k抑制剂
CN121824433A (zh) 一种解旋酶抑制剂、其制备方法及其用途
WO2014139391A1 (en) Substituted pyridine compounds as kinases inhibitors
CN115894376A (zh) 一种芳香族酰胺类化合物、药物组合物及其用途
EA045526B1 (ru) Производные бензиламида в качестве ингибиторов рецептора i/alk5 трансформирующего фактора роста-бета
HK40058867A (en) Imidazopyridinyl compounds and use thereof for treatment of proliferative disorders
WO2021017068A1 (zh) 吡咯并吡唑类衍生物、其制备方法及其在医药上的应用

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20211217