JP2022516555A - 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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JP2022516555A
JP2022516555A JP2021538976A JP2021538976A JP2022516555A JP 2022516555 A JP2022516555 A JP 2022516555A JP 2021538976 A JP2021538976 A JP 2021538976A JP 2021538976 A JP2021538976 A JP 2021538976A JP 2022516555 A JP2022516555 A JP 2022516555A
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pharmaceutically acceptable
aryl
acceptable salt
cyano
alkyl
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JP2022516555A5 (https=
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ベルナレス，セバスチャン
プジャラ，ブラーマム
パンパティル，ダヤナンド
ディアズ，ゴンザロ アンドレ ウレタ
ベルマール，セバスチャン
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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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    • 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)
JP2021538976A 2019-01-04 2020-01-03 線維芽細胞活性化タンパク質の阻害剤 Pending JP2022516555A (ja)

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 (2)

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JP2022516555A true JP2022516555A (ja) 2022-02-28
JP2022516555A5 JP2022516555A5 (https=) 2023-01-11

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JP2021538976A Pending JP2022516555A (ja) 2019-01-04 2020-01-03 線維芽細胞活性化タンパク質の阻害剤

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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=)

Families Citing this family (10)

* 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
US11780821B2 (en) 2017-12-15 2023-10-10 Praxis Biotech LLC Inhibitors of fibroblast activation protein
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
US11504364B2 (en) 2018-12-21 2022-11-22 Praxis Biotech LLC Inhibitors of fibroblast activation protein
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
BR112021025637A2 (pt) 2019-06-19 2022-02-01 Nmd Pharma As Compostos para o tratamento de doenças neuromusculares
EP4096677A4 (en) * 2020-01-31 2024-02-28 Purdue Research Foundation Fibroblast activation protein (fap) - targeted antifibrotic therapy
CN115819443B (zh) * 2022-08-02 2025-03-21 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
WO2025159534A1 (ko) * 2024-01-24 2025-07-31 서울대학교산학협력단 3-스티릴피리딘 구조 기반의 섬유아세포 활성화 단백질 표적 물질
CN118978511A (zh) * 2024-08-02 2024-11-19 江苏华益科技有限公司 一种靶向fap化合物及其制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2022514352A (ja) * 2018-12-21 2022-02-10 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

Family Cites Families (2)

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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2022514352A (ja) * 2018-12-21 2022-02-10 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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J. MED. CHEM., vol. 57, JPN6023050432, 2014, pages 3053 - 3074, ISSN: 0005216965 *

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Publication number Publication date
CN114126597A (zh) 2022-03-01
WO2020142742A1 (en) 2020-07-09
CL2021001739A1 (es) 2022-01-21
IL284434A (en) 2021-08-31
CA3124525A1 (en) 2020-07-09
MX2021007948A (es) 2021-08-11
EP3906024A1 (en) 2021-11-10
BR112021011861A2 (pt) 2021-09-08
EP3906024A4 (en) 2022-10-26
SG11202106399XA (en) 2021-07-29
US20200216417A1 (en) 2020-07-09
KR20210113634A (ko) 2021-09-16
AU2020204714A1 (en) 2021-07-08

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