CN114126597A - 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

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Publication number
CN114126597A
CN114126597A CN202080007971.2A CN202080007971A CN114126597A CN 114126597 A CN114126597 A CN 114126597A CN 202080007971 A CN202080007971 A CN 202080007971A CN 114126597 A CN114126597 A CN 114126597A
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compound
pharmaceutically acceptable
aryl
acceptable salt
cyano
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Chinese (zh)
Inventor
S·伯纳勒斯
B·普加拉
D·潘帕蒂尔
G·A·乌拉塔·迪亚兹
S·贝尔马尔
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Praxis Biotechnology Co ltd
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Praxis Biotechnology Co ltd
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Publication of CN114126597A publication Critical patent/CN114126597A/zh
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    • 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202080007971.2A 2019-01-04 2020-01-03 成纤维细胞激活蛋白抑制剂 Pending CN114126597A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962788722P 2019-01-04 2019-01-04
US62/788,722 2019-01-04
US201962863853P 2019-06-19 2019-06-19
US62/863,853 2019-06-19
PCT/US2020/012260 WO2020142742A1 (en) 2019-01-04 2020-01-03 Inhibitors of fibroblast activation protein

Publications (1)

Publication Number Publication Date
CN114126597A true CN114126597A (zh) 2022-03-01

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CN202080007971.2A Pending CN114126597A (zh) 2019-01-04 2020-01-03 成纤维细胞激活蛋白抑制剂

Country Status (13)

Country Link
US (1) US20200216417A1 (https=)
EP (1) EP3906024A4 (https=)
JP (1) JP2022516555A (https=)
KR (1) KR20210113634A (https=)
CN (1) CN114126597A (https=)
AU (1) AU2020204714A1 (https=)
BR (1) BR112021011861A2 (https=)
CA (1) CA3124525A1 (https=)
CL (1) CL2021001739A1 (https=)
IL (1) IL284434A (https=)
MX (1) MX2021007948A (https=)
SG (1) SG11202106399XA (https=)
WO (1) WO2020142742A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115819443A (zh) * 2022-08-02 2023-03-21 中国科学院上海应用物理研究所 一种含烯基化合物及其应用
WO2026025908A1 (zh) * 2024-08-02 2026-02-05 江苏华益科技有限公司 一种靶向fap化合物及其制备方法

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
EP3728228A1 (en) 2017-12-22 2020-10-28 Ravenna Pharmaceuticals, Inc. Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
CN113811529A (zh) 2018-12-21 2021-12-17 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
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
WO2020254559A1 (en) 2019-06-19 2020-12-24 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
WO2021155292A1 (en) * 2020-01-31 2021-08-05 Philip Stewart Low Fibroblast activation protein (fap) - targeted antifibrotic therapy
WO2025159534A1 (ko) * 2024-01-24 2025-07-31 서울대학교산학협력단 3-스티릴피리딘 구조 기반의 섬유아세포 활성화 단백질 표적 물질

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060276435A1 (en) * 2005-05-19 2006-12-07 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
US20070098781A1 (en) * 2005-08-11 2007-05-03 Loeffler Bernd M Modified release compositions for DPP-IV inhibitors
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
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
CN113811529A (zh) * 2018-12-21 2021-12-17 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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060276435A1 (en) * 2005-05-19 2006-12-07 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
US20070098781A1 (en) * 2005-08-11 2007-05-03 Loeffler Bernd M Modified release compositions for DPP-IV inhibitors
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
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
CN113811529A (zh) * 2018-12-21 2021-12-17 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 ET AL.: "Extended Structure-Activity Relationship and Pharmacokinetic Investigation of (4-Quinolinoyl)glycyl-2-cyanopyrrolidine Inhibitors of Fibroblast Activation Protein (FAP)", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, pages 3053 - 3074, XP055727968, DOI: 10.1021/jm500031w *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115819443A (zh) * 2022-08-02 2023-03-21 中国科学院上海应用物理研究所 一种含烯基化合物及其应用
CN119798158A (zh) * 2022-08-02 2025-04-11 中国科学院上海应用物理研究所 一种含苯并吡啶环类化合物及其制备方法
CN119874743A (zh) * 2022-08-02 2025-04-25 中国科学院上海应用物理研究所 一种含硼化合物及其制备方法
WO2026025908A1 (zh) * 2024-08-02 2026-02-05 江苏华益科技有限公司 一种靶向fap化合物及其制备方法

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Publication number Publication date
AU2020204714A1 (en) 2021-07-08
CA3124525A1 (en) 2020-07-09
EP3906024A1 (en) 2021-11-10
CL2021001739A1 (es) 2022-01-21
IL284434A (en) 2021-08-31
EP3906024A4 (en) 2022-10-26
KR20210113634A (ko) 2021-09-16
JP2022516555A (ja) 2022-02-28
BR112021011861A2 (pt) 2021-09-08
US20200216417A1 (en) 2020-07-09
WO2020142742A1 (en) 2020-07-09
SG11202106399XA (en) 2021-07-29
MX2021007948A (es) 2021-08-11

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Application publication date: 20220301