KR20230051500A - Alk5 억제제로서 피리다진일 아미노 유도체 - Google Patents

Alk5 억제제로서 피리다진일 아미노 유도체 Download PDF

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KR20230051500A
KR20230051500A KR1020237005127A KR20237005127A KR20230051500A KR 20230051500 A KR20230051500 A KR 20230051500A KR 1020237005127 A KR1020237005127 A KR 1020237005127A KR 20237005127 A KR20237005127 A KR 20237005127A KR 20230051500 A KR20230051500 A KR 20230051500A
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South Korea
Prior art keywords
chloro
fluorophenyl
amino
ethyl
pyridazin
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Korean (ko)
Inventor
다니엘라 피찌라니
마테오 비아제티
파올로 론키
파올로 브루노
사라 과리엔토
바바라 베르타니
다니엘레 파라
알레시오 바릴리
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키에시 파르마슈티시 엣스. 피. 에이.
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Publication of KR20230051500A publication Critical patent/KR20230051500A/ko
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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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)
KR1020237005127A 2020-07-15 2021-07-14 Alk5 억제제로서 피리다진일 아미노 유도체 Withdrawn KR20230051500A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20185890.9 2020-07-15
EP20185890 2020-07-15
PCT/EP2021/069649 WO2022013307A1 (en) 2020-07-15 2021-07-14 Pyridazinyl amino derivatives as alk5 inhibitors

Publications (1)

Publication Number Publication Date
KR20230051500A true KR20230051500A (ko) 2023-04-18

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KR1020237005127A Withdrawn KR20230051500A (ko) 2020-07-15 2021-07-14 Alk5 억제제로서 피리다진일 아미노 유도체

Country Status (19)

Country Link
US (1) US12479826B2 (https=)
EP (1) EP4182308B1 (https=)
JP (1) JP7686741B2 (https=)
KR (1) KR20230051500A (https=)
CN (1) CN116096719B (https=)
AR (1) AR122986A1 (https=)
AU (1) AU2021307559A1 (https=)
BR (1) BR112023000588A8 (https=)
CA (1) CA3184990A1 (https=)
DK (1) DK4182308T3 (https=)
ES (1) ES2997111T3 (https=)
FI (1) FI4182308T3 (https=)
HR (1) HRP20241617T1 (https=)
HU (1) HUE069150T2 (https=)
MX (1) MX2023000521A (https=)
PL (1) PL4182308T3 (https=)
PT (1) PT4182308T (https=)
SI (1) SI4182308T1 (https=)
WO (1) WO2022013307A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024225819A1 (ko) * 2023-04-28 2024-10-31 한국원자력의학원 N-메틸피페라진 에탄올 카바메이트 구조를 포함하는 신규 화합물 및 이의 용도

Families Citing this family (6)

* Cited by examiner, † Cited by third party
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JP7702205B2 (ja) * 2021-09-15 2025-07-03 株式会社東芝 新規アミン化合物、酸性ガス吸収剤、酸性ガスの除去方法及び酸性ガス除去
CN114957331A (zh) * 2022-04-22 2022-08-30 北京康辰药业股份有限公司 磷酸酯取代的环丙酰胺衍生喹唑啉类化合物的制备方法
WO2024180206A1 (en) 2023-03-02 2024-09-06 Chiesi Farmaceutici S.P.A. Pyridazinyl amino derivatives as alk5 inhibitors
WO2024180207A1 (en) 2023-03-02 2024-09-06 Chiesi Farmaceutici S.P.A. Pyridazinyl amino derivatives as alk5 inhibitors
WO2025132458A1 (en) 2023-12-18 2025-06-26 Chiesi Farmaceutici S.P.A. Pyridazinyl amino derivatives as alk5 inhibitors
WO2025132460A1 (en) 2023-12-18 2025-06-26 Chiesi Farmaceutici S.P.A. Pyridazinyl amino derivatives as alk5 inhibitors

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DE60001229T2 (de) 1999-04-09 2003-10-30 Smithkline Beecham Corp., Philadelphia Triarylimidazole
AR029803A1 (es) 2000-02-21 2003-07-16 Smithkline Beecham Plc Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
EP1317450B1 (en) * 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2423050A1 (en) 2000-09-20 2002-03-28 Ortho-Mcneil Pharmaceutical, Inc. Pyrazine derivatives as modulators of tyrosine kinases
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
JP2006503043A (ja) * 2002-09-10 2006-01-26 サイオス インク. TGFβ阻害剤
AU2004278382B2 (en) * 2003-09-30 2008-09-18 Amgen Inc. Vanilloid receptor ligands and their use in treatments
BRPI0714409A2 (pt) 2006-07-14 2013-03-12 Novartis Ag derivados de pirimidina como inibidores de alk-5
ES2375425T3 (es) 2007-07-26 2012-02-29 Novartis Ag Compuestos org�?nicos.
BRPI0817434A2 (pt) 2007-10-17 2015-06-16 Novartis Ag Composto orgânicos
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
MX2010007604A (es) 2008-01-11 2010-08-02 Novartis Ag Pirimidinas como inhibidores de cinasa.
US8343966B2 (en) 2008-01-11 2013-01-01 Novartis Ag Organic compounds
EA201001687A1 (ru) 2008-04-29 2011-06-30 Новартис Аг Производные имидазопиридина в качестве ингибиторов активиноподобной рецепторной киназы ( alk-4 или alk-5 )
CN102596200A (zh) * 2009-11-07 2012-07-18 默克专利有限公司 作为TGF-β受体激酶抑制剂的杂芳基氨基喹啉类
DK2731949T3 (en) 2011-07-13 2018-06-14 Tiumbio Co Ltd 2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND / OR ALK4 INHIBITORS
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US20200247812A1 (en) * 2018-07-10 2020-08-06 Integral Biosciences Private Limited Heterocyclic compounds and methods of use

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WO2024225819A1 (ko) * 2023-04-28 2024-10-31 한국원자력의학원 N-메틸피페라진 에탄올 카바메이트 구조를 포함하는 신규 화합물 및 이의 용도

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Publication number Publication date
DK4182308T3 (da) 2024-10-21
BR112023000588A2 (pt) 2023-01-31
ES2997111T3 (en) 2025-03-19
AR122986A1 (es) 2022-10-19
TW202216677A (zh) 2022-05-01
HRP20241617T1 (hr) 2025-01-31
CA3184990A1 (en) 2022-01-20
WO2022013307A1 (en) 2022-01-20
PT4182308T (pt) 2024-12-04
AU2021307559A1 (en) 2023-02-16
JP2023533849A (ja) 2023-08-04
US12479826B2 (en) 2025-11-25
BR112023000588A8 (pt) 2023-05-09
JP7686741B2 (ja) 2025-06-02
EP4182308A1 (en) 2023-05-24
US20240018122A1 (en) 2024-01-18
CN116096719A (zh) 2023-05-09
SI4182308T1 (sl) 2025-04-30
FI4182308T3 (fi) 2024-12-07
HUE069150T2 (hu) 2025-02-28
PL4182308T3 (pl) 2025-01-07
EP4182308B1 (en) 2024-09-04
CN116096719B (zh) 2025-09-30
MX2023000521A (es) 2023-02-13

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