AU2021353965A1 - 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 - Google Patents

2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 Download PDF

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Publication number
AU2021353965A1
AU2021353965A1 AU2021353965A AU2021353965A AU2021353965A1 AU 2021353965 A1 AU2021353965 A1 AU 2021353965A1 AU 2021353965 A AU2021353965 A AU 2021353965A AU 2021353965 A AU2021353965 A AU 2021353965A AU 2021353965 A1 AU2021353965 A1 AU 2021353965A1
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AU
Australia
Prior art keywords
pyrazol
quinolin
methylpyridin
acetamido
benzoate
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
AU2021353965A
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English (en)
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AU2021353965A9 (en
Inventor
Ramón BOSSER ARTAL
Julio Castro Palomino Laria
Begoña PAMPÍN CASAL
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Agomab Spain SLU
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Agomab Spain S L U
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Agomab Spain S L U filed Critical Agomab Spain S L U
Publication of AU2021353965A1 publication Critical patent/AU2021353965A1/en
Publication of AU2021353965A9 publication Critical patent/AU2021353965A9/en
Pending legal-status Critical Current

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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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2021353965A 2020-09-30 2021-09-29 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 Pending AU2021353965A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20382861.1 2020-09-30
EP20382861.1A EP3978487A1 (en) 2020-09-30 2020-09-30 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5
PCT/EP2021/076730 WO2022069509A1 (en) 2020-09-30 2021-09-29 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5

Publications (2)

Publication Number Publication Date
AU2021353965A1 true AU2021353965A1 (en) 2023-04-27
AU2021353965A9 AU2021353965A9 (en) 2024-08-01

Family

ID=72744716

Family Applications (1)

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AU2021353965A Pending AU2021353965A1 (en) 2020-09-30 2021-09-29 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5

Country Status (14)

Country Link
US (1) US12577230B2 (https=)
EP (2) EP3978487A1 (https=)
JP (1) JP7752684B2 (https=)
KR (1) KR20230079027A (https=)
CN (1) CN116323601A (https=)
AR (1) AR123543A1 (https=)
AU (1) AU2021353965A1 (https=)
BR (1) BR112023004612A2 (https=)
CA (1) CA3196108A1 (https=)
ES (1) ES3029607T1 (https=)
IL (1) IL301663B1 (https=)
MX (1) MX2023002900A (https=)
PH (1) PH12023550777A1 (https=)
WO (1) WO2022069509A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4065572A1 (en) 2019-11-28 2022-10-05 Origo Biopharma, S.L. Benzylamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5
WO2026017797A1 (en) 2024-07-17 2026-01-22 Agomab Spain S.L.U. Crystalline forms
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

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6514977B1 (en) * 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
PL337020A1 (en) * 1997-05-22 2000-07-31 Searle & Co Substituted pyrazoles as kinase p38 inhibitors
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
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
CL2004000234A1 (es) 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
WO2007005951A2 (en) * 2005-07-05 2007-01-11 Aryx Therapeutics, Inc. Stereoisomeric pyridyl and pyridonyl compounds and methods for the treatment of gastrointestinal and central nervous system disorders
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
ES2579832T3 (es) 2011-10-14 2016-08-17 Bristol-Myers Squibb Company Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa
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
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
EP4065572A1 (en) 2019-11-28 2022-10-05 Origo Biopharma, S.L. Benzylamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5

Also Published As

Publication number Publication date
AR123543A1 (es) 2022-12-14
PH12023550777A1 (en) 2023-11-20
IL301663B1 (en) 2026-01-01
ES3029607T1 (en) 2025-06-24
CN116323601A (zh) 2023-06-23
BR112023004612A2 (pt) 2023-04-11
MX2023002900A (es) 2023-05-25
EP3978487A1 (en) 2022-04-06
US12577230B2 (en) 2026-03-17
JP2023544716A (ja) 2023-10-25
IL301663A (en) 2023-05-01
JP7752684B2 (ja) 2025-10-10
AU2021353965A9 (en) 2024-08-01
US20230373966A1 (en) 2023-11-23
CA3196108A1 (en) 2022-04-07
WO2022069509A1 (en) 2022-04-07
EP4222149A1 (en) 2023-08-09
KR20230079027A (ko) 2023-06-05

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