JP7752684B2 - 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２－（３－ピリジン－２－イル－４－キノリン－４－イル－ピラゾール－１－イル）－アセタミド誘導体 - 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２－（３－ピリジン－２－イル－４－キノリン－４－イル－ピラゾール－１－イル）－アセタミド誘導体

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Publication number
JP7752684B2
JP7752684B2 JP2023519608A JP2023519608A JP7752684B2 JP 7752684 B2 JP7752684 B2 JP 7752684B2 JP 2023519608 A JP2023519608 A JP 2023519608A JP 2023519608 A JP2023519608 A JP 2023519608A JP 7752684 B2 JP7752684 B2 JP 7752684B2
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Prior art keywords
pyrazol
quinolin
methylpyridin
acetamido
benzoate
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JP2023519608A
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English (en)
Japanese (ja)
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JP2023544716A (ja
JP2023544716A5 (https=
JPWO2022069509A5 (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
Original Assignee
アゴマブ スペイン， エス．エル．ユー．
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Publication of JP2023544716A publication Critical patent/JP2023544716A/ja
Publication of JP2023544716A5 publication Critical patent/JP2023544716A5/ja
Publication of JPWO2022069509A5 publication Critical patent/JPWO2022069509A5/ja
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Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

Landscapes

  • 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)
JP2023519608A 2020-09-30 2021-09-29 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２－（３－ピリジン－２－イル－４－キノリン－４－イル－ピラゾール－１－イル）－アセタミド誘導体 Active JP7752684B2 (ja)

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 (4)

Publication Number Publication Date
JP2023544716A JP2023544716A (ja) 2023-10-25
JP2023544716A5 JP2023544716A5 (https=) 2024-10-08
JPWO2022069509A5 JPWO2022069509A5 (https=) 2024-10-08
JP7752684B2 true JP7752684B2 (ja) 2025-10-10

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Family Applications (1)

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JP2023519608A Active JP7752684B2 (ja) 2020-09-30 2021-09-29 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２－（３－ピリジン－２－イル－４－キノリン－４－イル－ピラゾール－１－イル）－アセタミド誘導体

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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002508754A (ja) 1997-05-22 2002-03-19 ジー ディ サール アンド カンパニ ｐ３８キナーゼ阻害剤としての置換基を有するピラゾール類
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
JP2009500419A (ja) 2005-07-05 2009-01-08 アリックス セラピューティクス、インコーポレイテッド 立体異性体のピリジル及びピリドニル化合物並びに消化管障害及び中枢神経系障害の治療方法

Family Cites Families (14)

* 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
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
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002508754A (ja) 1997-05-22 2002-03-19 ジー ディ サール アンド カンパニ ｐ３８キナーゼ阻害剤としての置換基を有するピラゾール類
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
JP2009500419A (ja) 2005-07-05 2009-01-08 アリックス セラピューティクス、インコーポレイテッド 立体異性体のピリジル及びピリドニル化合物並びに消化管障害及び中枢神経系障害の治療方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Bioorganic & Medicinal Chemistry Letters，2020年，30，126822
Bioorganic & Medicinal Chemistry，2011年，19，2633-2640

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
AU2021353965A1 (en) 2023-04-27
US12577230B2 (en) 2026-03-17
JP2023544716A (ja) 2023-10-25
IL301663A (en) 2023-05-01
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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