CN116323601A - 作为转化生长因子-β 受体I/ALK5抑制剂的2-(3-吡啶-2-基-4-喹啉-4-基-吡唑-1-基)-乙酰胺衍生物 - Google Patents

作为转化生长因子-β 受体I/ALK5抑制剂的2-(3-吡啶-2-基-4-喹啉-4-基-吡唑-1-基)-乙酰胺衍生物 Download PDF

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Publication number
CN116323601A
CN116323601A CN202180066883.4A CN202180066883A CN116323601A CN 116323601 A CN116323601 A CN 116323601A CN 202180066883 A CN202180066883 A CN 202180066883A CN 116323601 A CN116323601 A CN 116323601A
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CN
China
Prior art keywords
pyrazol
quinolin
methylpyridin
acetamido
fluoro
Prior art date
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
CN202180066883.4A
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English (en)
Chinese (zh)
Inventor
R·鲍瑟尔阿尔塔
B·潘平卡萨尔
J·卡斯特罗帕洛米诺拉里亚
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Agomeb Spain SA
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Agomeb Spain SA
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Filing date
Publication date
Application filed by Agomeb Spain SA filed Critical Agomeb Spain SA
Publication of CN116323601A publication Critical patent/CN116323601A/zh
Pending legal-status Critical Current

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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
    • 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

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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)
CN202180066883.4A 2020-09-30 2021-09-29 作为转化生长因子-β 受体I/ALK5抑制剂的2-(3-吡啶-2-基-4-喹啉-4-基-吡唑-1-基)-乙酰胺衍生物 Pending CN116323601A (zh)

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 (1)

Publication Number Publication Date
CN116323601A true CN116323601A (zh) 2023-06-23

Family

ID=72744716

Family Applications (1)

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CN202180066883.4A Pending CN116323601A (zh) 2020-09-30 2021-09-29 作为转化生长因子-β 受体I/ALK5抑制剂的2-(3-吡啶-2-基-4-喹啉-4-基-吡唑-1-基)-乙酰胺衍生物

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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002066462A1 (en) * 2001-02-02 2002-08-29 Glaxo Group Limited Pyrazole derivatives against tgf overexpression
WO2004026302A1 (en) * 2002-09-19 2004-04-01 Eli Lilly And Company Methods of inhibiting tgf beta with substituted pyrazoles
CN102056907A (zh) * 2008-04-04 2011-05-11 武田药品工业株式会社 杂环衍生物及其用途
CN103764655A (zh) * 2011-07-13 2014-04-30 Sk化学公司 作为alk5和/或alk4抑制剂的经2-吡啶基取代的咪唑

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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
HRP20050247A2 (en) 2002-09-18 2005-10-31 Pfizer Products Inc. Pyrazole derivatives as transforming growth factor (tgf) inhibitors
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
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
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002066462A1 (en) * 2001-02-02 2002-08-29 Glaxo Group Limited Pyrazole derivatives against tgf overexpression
WO2004026302A1 (en) * 2002-09-19 2004-04-01 Eli Lilly And Company Methods of inhibiting tgf beta with substituted pyrazoles
CN102056907A (zh) * 2008-04-04 2011-05-11 武田药品工业株式会社 杂环衍生物及其用途
CN103764655A (zh) * 2011-07-13 2014-04-30 Sk化学公司 作为alk5和/或alk4抑制剂的经2-吡啶基取代的咪唑

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
CHENG HUAJIN等: "Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors", 《BIOORGANIC & MEDICINAL CHEMISTRY》, vol. 19, 10 February 2011 (2011-02-10), pages 2633 - 2640, XP002794438 *
WEN-JING ZHU等: "Design, synthesis , and antifi brosis evaluation of 4-(benzo-[c ][1, 2, 5] thiadiazo l-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno -[3, 2, -c ]pyridin-2-yl)pyrazole derivatives", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》, vol. 180, 5 July 2019 (2019-07-05), pages 15 - 27 *
YAN-WEI LI等: "Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, vol. 30, 17 November 2019 (2019-11-17), pages 1 - 12, XP086033969, DOI: 10.1016/j.bmcl.2019.126822 *

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
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
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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