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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JP2023504795A (ja
JP2023504795A5 (https=
JPWO2021105317A5 (https=
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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Publication of JP2023504795A5 publication Critical patent/JP2023504795A5/ja
Publication of JPWO2021105317A5 publication Critical patent/JPWO2021105317A5/ja
Priority to JP2025116497A priority Critical patent/JP2025163046A/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs 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)

Application Number Title Priority Date Filing Date
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 (4)

Publication Number Publication Date
JP2023504795A JP2023504795A (ja) 2023-02-07
JP2023504795A5 JP2023504795A5 (https=) 2023-12-06
JPWO2021105317A5 JPWO2021105317A5 (https=) 2023-12-06
JP7808032B2 true JP7808032B2 (ja) 2026-01-28

Family

ID=68808255

Family Applications (2)

Application Number Title Priority Date Filing Date
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)

Application Number Title Priority Date Filing Date
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 (16)

Country Link
US (2) US12297186B2 (https=)
EP (1) EP4065572A1 (https=)
JP (2) JP7808032B2 (https=)
KR (1) KR20220107180A (https=)
CN (1) CN114787145B (https=)
AR (1) AR120578A1 (https=)
AU (1) AU2020394531A1 (https=)
BR (1) BR112022010251A2 (https=)
CA (1) CA3160963A1 (https=)
ES (1) ES3029608T1 (https=)
IL (1) IL293388B2 (https=)
MX (1) MX2022005843A (https=)
PH (1) PH12022551177A1 (https=)
SA (1) SA522432749B1 (https=)
WO (1) WO2021105317A1 (https=)
ZA (1) ZA202205149B (https=)

Families Citing this family (2)

* 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
TW202543626A (zh) 2024-02-22 2025-11-16 西班牙商亞哥邁伯西班牙有限公司 新穎結晶相形式

Citations (2)

* Cited by examiner, † Cited by third party
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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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
HRP20050247A2 (en) 2002-09-18 2005-10-31 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
AR079545A1 (es) 2009-12-21 2012-02-01 Bayer Cropscience Ag Tienilpiri(mi)dinilazol
DK2731949T3 (en) * 2011-07-13 2018-06-14 Tiumbio Co Ltd 2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND / OR ALK4 INHIBITORS
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
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

Non-Patent Citations (2)

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

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