JP7515049B2 - がんの処置のためのtgf-ベータr1(alk5)阻害剤としての(ピリジン-2-イル)アミン誘導体 - Google Patents

がんの処置のためのtgf-ベータr1(alk5)阻害剤としての(ピリジン-2-イル)アミン誘導体 Download PDF

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JP7515049B2
JP7515049B2 JP2021536757A JP2021536757A JP7515049B2 JP 7515049 B2 JP7515049 B2 JP 7515049B2 JP 2021536757 A JP2021536757 A JP 2021536757A JP 2021536757 A JP2021536757 A JP 2021536757A JP 7515049 B2 JP7515049 B2 JP 7515049B2
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JP2022517730A (ja
JP2022517730A5 (cg-RX-API-DMAC7.html
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トム ヤオ-シャン ウー,
チフイ ジン,
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ネクサス セラピューティクス, インコーポレイテッド
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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
    • A61K31/33—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021536757A 2018-12-27 2019-12-17 がんの処置のためのtgf-ベータr1(alk5)阻害剤としての(ピリジン-2-イル)アミン誘導体 Active JP7515049B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023005014A JP2023052437A (ja) 2018-12-27 2023-01-17 がんの処置のためのtgf-ベータr1(alk5)阻害剤としての(ピリジン-2-イル)アミン誘導体

Applications Claiming Priority (3)

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US201862785616P 2018-12-27 2018-12-27
US62/785,616 2018-12-27
PCT/US2019/066993 WO2020139636A1 (en) 2018-12-27 2019-12-17 (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer

Related Child Applications (1)

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JP2023005014A Division JP2023052437A (ja) 2018-12-27 2023-01-17 がんの処置のためのtgf-ベータr1(alk5)阻害剤としての(ピリジン-2-イル)アミン誘導体

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JP2022517730A JP2022517730A (ja) 2022-03-10
JP2022517730A5 JP2022517730A5 (cg-RX-API-DMAC7.html) 2022-12-16
JP7515049B2 true JP7515049B2 (ja) 2024-07-12

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JP2023005014A Pending JP2023052437A (ja) 2018-12-27 2023-01-17 がんの処置のためのtgf-ベータr1(alk5)阻害剤としての(ピリジン-2-イル)アミン誘導体

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US (2) US12102626B2 (cg-RX-API-DMAC7.html)
EP (1) EP3902796B1 (cg-RX-API-DMAC7.html)
JP (2) JP7515049B2 (cg-RX-API-DMAC7.html)
KR (1) KR102832376B1 (cg-RX-API-DMAC7.html)
CN (1) CN113348167B (cg-RX-API-DMAC7.html)
AR (1) AR117539A1 (cg-RX-API-DMAC7.html)
AU (1) AU2019417418B2 (cg-RX-API-DMAC7.html)
BR (1) BR112021007006A2 (cg-RX-API-DMAC7.html)
CA (1) CA3117838A1 (cg-RX-API-DMAC7.html)
EA (1) EA202191619A1 (cg-RX-API-DMAC7.html)
ES (1) ES2972516T3 (cg-RX-API-DMAC7.html)
IL (1) IL284266B2 (cg-RX-API-DMAC7.html)
MX (1) MX2021007738A (cg-RX-API-DMAC7.html)
SG (1) SG11202103457PA (cg-RX-API-DMAC7.html)
TW (1) TWI884934B (cg-RX-API-DMAC7.html)
WO (1) WO2020139636A1 (cg-RX-API-DMAC7.html)

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
WO2021216454A1 (en) 2020-04-21 2021-10-28 Lexicon Pharmaceuticals, Inc. 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections
JP2023522688A (ja) 2020-04-21 2023-05-31 レクシコン ファーマシューティカルズ インコーポレイテッド ウイルス感染症の治療に使用されるaak1阻害剤
CN113214111A (zh) * 2021-04-30 2021-08-06 上海立科化学科技有限公司 3-(2-氰基苯基)丙酸及4-氰基-1-茚满酮的制备方法
US12263576B2 (en) 2021-08-19 2025-04-01 Hyundai Mobis Co., Ltd. Robot system for automated assembly of modular component
EP4464694A4 (en) * 2022-01-14 2026-04-01 Shanghai Hansoh Biomedical Co Ltd POLYCYCLIC DERIVATIVE CONTAINING PYRIDINE, ITS PREPARATION PROCESS AND ITS USE
CN121554469B (zh) * 2026-01-23 2026-04-17 四川大学华西医院 一种alk5 protac化合物及其应用

Citations (3)

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WO2009022171A1 (en) 2007-08-13 2009-02-19 Astrazeneca Ab Pyridinyiioxy pyridines as alk5 inhibitors
JP2016535745A (ja) 2014-10-07 2016-11-17 イーライ リリー アンド カンパニー アミノピリジルオキシピラゾール化合物
JP2017501200A (ja) 2014-01-01 2017-01-12 メディベイション テクノロジーズ, インコーポレイテッド 化合物及び使用方法

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UA80571C2 (en) 2002-11-22 2007-10-10 Lilly Co Eli Quinolinyl-pyrrolopyrazoles
TW200538120A (en) 2004-02-20 2005-12-01 Kirin Brewery Compound having TGF-beta inhibitory activity and pharmaceutical composition containing same
US8080568B1 (en) 2010-06-29 2011-12-20 Ewha University - Industry Collaboration Foundation 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors
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WO2012151137A1 (en) * 2011-05-04 2012-11-08 Merck Sharp & Dohme Corp. Amino-pyridine-containing spleen tyrosine kinase (syk) inhibitors
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JP2016535745A (ja) 2014-10-07 2016-11-17 イーライ リリー アンド カンパニー アミノピリジルオキシピラゾール化合物

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Publication number Publication date
CN113348167A (zh) 2021-09-03
TW202039436A (zh) 2020-11-01
IL284266B1 (en) 2024-02-01
AR117539A1 (es) 2021-08-11
BR112021007006A2 (pt) 2021-08-10
IL284266B2 (en) 2024-06-01
KR20210110316A (ko) 2021-09-07
WO2020139636A1 (en) 2020-07-02
TWI884934B (zh) 2025-06-01
AU2019417418A1 (en) 2021-04-15
EP3902796A1 (en) 2021-11-03
CN113348167B (zh) 2026-01-09
KR102832376B1 (ko) 2025-07-09
NZ775362A (en) 2025-02-28
US20240398776A1 (en) 2024-12-05
EA202191619A1 (ru) 2021-09-28
IL284266A (en) 2021-08-31
CA3117838A1 (en) 2020-07-02
EP3902796C0 (en) 2024-02-07
ES2972516T3 (es) 2024-06-13
US12102626B2 (en) 2024-10-01
JP2022517730A (ja) 2022-03-10
EP3902796B1 (en) 2024-02-07
SG11202103457PA (en) 2021-05-28
JP2023052437A (ja) 2023-04-11
AU2019417418B2 (en) 2025-02-27
MX2021007738A (es) 2021-08-05
US20220054465A1 (en) 2022-02-24

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