CN114787145B - 作为转化生长因子-β受体I/ALK5抑制剂的苯甲酰胺衍生物 - Google Patents

作为转化生长因子-β受体I/ALK5抑制剂的苯甲酰胺衍生物 Download PDF

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Publication number
CN114787145B
CN114787145B CN202080080848.3A CN202080080848A CN114787145B CN 114787145 B CN114787145 B CN 114787145B CN 202080080848 A CN202080080848 A CN 202080080848A CN 114787145 B CN114787145 B CN 114787145B
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Prior art keywords
pyrazol
acetamide
quinolin
pharmaceutically acceptable
pyridin
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Chinese (zh)
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CN114787145A (zh
Inventor
R·鲍瑟尔阿尔塔
B·潘平卡萨尔
J·C·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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    • 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)
CN202080080848.3A 2019-11-28 2020-11-27 作为转化生长因子-β受体I/ALK5抑制剂的苯甲酰胺衍生物 Active CN114787145B (zh)

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

Publications (2)

Publication Number Publication Date
CN114787145A CN114787145A (zh) 2022-07-22
CN114787145B true CN114787145B (zh) 2024-03-26

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CN202080080848.3A Active CN114787145B (zh) 2019-11-28 2020-11-27 作为转化生长因子-β受体I/ALK5抑制剂的苯甲酰胺衍生物

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 (5)

* 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
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
WO2016160833A1 (en) * 2015-04-01 2016-10-06 Rigel Pharmaceuticals, Inc. TGF-β INHIBITORS
CN109415346A (zh) * 2016-06-30 2019-03-01 韩美药品株式会社 作为alk5抑制剂的新型吡唑衍生物及其用途
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

Family Cites Families (11)

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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
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
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
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 (5)

* 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
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
WO2016160833A1 (en) * 2015-04-01 2016-10-06 Rigel Pharmaceuticals, Inc. TGF-β INHIBITORS
CN109415346A (zh) * 2016-06-30 2019-03-01 韩美药品株式会社 作为alk5抑制剂的新型吡唑衍生物及其用途
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

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
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;Cheng Hua Jin et al.;《Bioorganic & Medicinal Chemistry》;第19卷;第2633-2640页 *
Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)- 4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors;Cheng Hua Jin et al.;《European Journal of Medicinal Chemistry》;第46卷;第3917-3925页 *
转化生长因子-β 抑制剂研究进展;盖小雄等;《药学学报》;第50卷(第4期);第413-418页 *

Also Published As

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
JP7808032B2 (ja) 2026-01-28
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

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