JP7808032B2 - トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体 - Google Patents

トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体

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Publication number
JP7808032B2
JP7808032B2 JP2022531434A JP2022531434A JP7808032B2 JP 7808032 B2 JP7808032 B2 JP 7808032B2 JP 2022531434 A JP2022531434 A JP 2022531434A JP 2022531434 A JP2022531434 A JP 2022531434A JP 7808032 B2 JP7808032 B2 JP 7808032B2
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disease
acetamide
pyrazol
pharmaceutically acceptable
group
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JP2023504795A5 (cg-RX-API-DMAC7.html
JP2023504795A (ja
Inventor
ボセール アータル レイモン
パンピン カサル ベゴーニャ
カストロ パロミノ ラリア ジュリオ
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アゴマブ スペイン， エス．エル．ユー．
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Priority to JP2025116497A priority Critical patent/JP2025163046A/ja
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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
    • A61K31/47—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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
JP2022531434A 2019-11-28 2020-11-27 トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体 Active JP7808032B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025116497A JP2025163046A (ja) 2019-11-28 2025-07-10 トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19383057.7 2019-11-28
EP19383057 2019-11-28
PCT/EP2020/083566 WO2021105317A1 (en) 2019-11-28 2020-11-27 Benzylamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5

Related Child Applications (1)

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JP2025116497A Division JP2025163046A (ja) 2019-11-28 2025-07-10 トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体

Publications (3)

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JP2023504795A JP2023504795A (ja) 2023-02-07
JP2023504795A5 JP2023504795A5 (cg-RX-API-DMAC7.html) 2023-12-06
JP7808032B2 true JP7808032B2 (ja) 2026-01-28

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Family Applications (2)

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JP2022531434A Active JP7808032B2 (ja) 2019-11-28 2020-11-27 トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体
JP2025116497A Pending JP2025163046A (ja) 2019-11-28 2025-07-10 トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体

Family Applications After (1)

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JP2025116497A Pending JP2025163046A (ja) 2019-11-28 2025-07-10 トランスフォーミング増殖因子－β受容体Ｉ／ＡＬＫ５の阻害剤としてのベンジルアミド誘導体

Country Status (15)

Country Link
US (2) US12297186B2 (cg-RX-API-DMAC7.html)
EP (1) EP4065572A1 (cg-RX-API-DMAC7.html)
JP (2) JP7808032B2 (cg-RX-API-DMAC7.html)
CN (1) CN114787145B (cg-RX-API-DMAC7.html)
AR (1) AR120578A1 (cg-RX-API-DMAC7.html)
AU (1) AU2020394531B2 (cg-RX-API-DMAC7.html)
BR (1) BR112022010251A2 (cg-RX-API-DMAC7.html)
CA (1) CA3160963A1 (cg-RX-API-DMAC7.html)
ES (1) ES3029608T1 (cg-RX-API-DMAC7.html)
IL (1) IL293388B2 (cg-RX-API-DMAC7.html)
MX (1) MX2022005843A (cg-RX-API-DMAC7.html)
PH (1) PH12022551177A1 (cg-RX-API-DMAC7.html)
SA (1) SA522432749B1 (cg-RX-API-DMAC7.html)
WO (1) WO2021105317A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA202205149B (cg-RX-API-DMAC7.html)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3978487A1 (en) 2020-09-30 2022-04-06 Origo Biopharma, S.L. 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5
AU2025225502A1 (en) 2024-02-22 2026-07-30 Agomab Spain S.L.U. Crystalline phase forms of a benzylamide derivative
WO2026082960A1 (en) 2024-10-18 2026-04-23 Agomab Therapeutics Nv 1,5-naphtyridine and quinoline based inhibitors of alk5
WO2026082968A1 (en) 2024-10-18 2026-04-23 Agomab Therapeutics Nv Novel compounds
CN122036718A (zh) * 2026-01-30 2026-05-15 安炎达医药技术(广州)有限公司 一种alk5抑制剂及其制备方法和应用

Citations (2)

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JP2004521915A (ja) 2001-02-02 2004-07-22 グラクソ　グループ　リミテッド Ｔｇｆ過剰発現に対するピラゾール誘導体
JP2006517592A (ja) 2003-02-12 2006-07-27 バイオジェン・アイデック・エムエイ・インコーポレイテッド ピラゾールおよびそれらを製造し使用する方法

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DE3621540A1 (de) 1986-06-27 1988-01-07 Basf Ag Chinolinderivate, verfahren zu ihrer herstellung, diese enthaltende mikrobizide und ihre verwendung zur bekaempfung von bakterien und pilzen
WO2004026306A2 (en) 2002-09-18 2004-04-01 Pfizer Products Inc. Pyrazole derivatives as transforming growth factor (tgf) inhibitors
WO2004026302A1 (en) * 2002-09-19 2004-04-01 Eli Lilly And Company Methods of inhibiting tgf beta with substituted pyrazoles
CN102056907B (zh) 2008-04-04 2014-12-31 武田药品工业株式会社 杂环衍生物及其用途
US8937150B2 (en) 2009-06-11 2015-01-20 Abbvie Inc. Anti-viral compounds
WO2011076725A1 (en) 2009-12-21 2011-06-30 Bayer Cropscience Ag Thienylpyri (mi) dinylazole and their use for controlling phytopathogenic fungi
RU2612958C2 (ru) * 2011-07-13 2017-03-14 Ск Кемикалз Ко., Лтд. 2-пиридилзамещенные имидазолы в качестве ингибиторов alk5 и/или alk4
US11021468B2 (en) * 2015-04-01 2021-06-01 Rigel Pharmaceuticals, Inc. TGF-ß inhibitors
WO2016172631A2 (en) 2015-04-24 2016-10-27 President And Fellows Of Harvard College Substrate selective inhibitors of insulin-degrading enzyme (ide) and uses thereof
KR102434226B1 (ko) * 2016-06-30 2022-08-19 한미약품 주식회사 Alk5 억제제로서의 신규 피라졸 유도체 및 이의 용도
JP2021518855A (ja) 2018-03-02 2021-08-05 ユニヴェルシテ ド ローザンヌ Ｗｎｔシグナル伝達経路阻害剤としてのピラゾール誘導体
US11945803B2 (en) 2018-08-07 2024-04-02 Tosk, Inc. Modulators of RAS GTPase
CN110433164A (zh) * 2019-08-15 2019-11-12 南开大学 TGF-beta受体分子抑制剂在治疗小鼠动物模型中急性髓系白血病的应用
EP3978487A1 (en) 2020-09-30 2022-04-06 Origo Biopharma, S.L. 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5

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Publication number Priority date Publication date Assignee Title
JP2004521915A (ja) 2001-02-02 2004-07-22 グラクソ　グループ　リミテッド Ｔｇｆ過剰発現に対するピラゾール誘導体
JP2006517592A (ja) 2003-02-12 2006-07-27 バイオジェン・アイデック・エムエイ・インコーポレイテッド ピラゾールおよびそれらを製造し使用する方法

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Cancer Science，2005年10月17日，Vol.96, No.11，p791-800，doi:10.1111/j.1349-7006.2005.00103.x
Journal of Medicinal Chemistry，2003年09月11日，Vol.46, No.19，p3953-3956，doi:10.1021/jm0205705

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SA522432749B1 (ar) 2025-05-12
AU2020394531B2 (en) 2026-06-25
US12297186B2 (en) 2025-05-13
CN114787145B (zh) 2024-03-26
KR20220107180A (ko) 2022-08-02
WO2021105317A1 (en) 2021-06-03
IL293388B1 (en) 2025-12-01
EP4065572A1 (en) 2022-10-05
ES3029608T1 (en) 2025-06-24
IL293388B2 (en) 2026-04-01
BR112022010251A2 (pt) 2022-09-06
US20250333395A1 (en) 2025-10-30
JP2025163046A (ja) 2025-10-28
AU2020394531A1 (en) 2022-06-09
AR120578A1 (es) 2022-02-23
US20230025933A1 (en) 2023-01-26
JP2023504795A (ja) 2023-02-07
PH12022551177A1 (en) 2024-02-05
ZA202205149B (en) 2025-06-25
MX2022005843A (es) 2022-07-19
IL293388A (en) 2022-07-01
CA3160963A1 (en) 2021-06-03
CN114787145A (zh) 2022-07-22

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