JP7686741B2 - Alk5阻害剤としてのピリダジニルアミノ誘導体 - Google Patents

Alk5阻害剤としてのピリダジニルアミノ誘導体 Download PDF

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JP7686741B2
JP7686741B2 JP2023502861A JP2023502861A JP7686741B2 JP 7686741 B2 JP7686741 B2 JP 7686741B2 JP 2023502861 A JP2023502861 A JP 2023502861A JP 2023502861 A JP2023502861 A JP 2023502861A JP 7686741 B2 JP7686741 B2 JP 7686741B2
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chloro
fluorophenyl
amino
ethyl
pyridazin
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JP2023533849A5 (https=
JP2023533849A (ja
JPWO2022013307A5 (https=
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ピッツィラーニ,ダニエラ
ビアジェッティ,マッテオ
ロンキ,パウロ
ブルーノ,パオロ
グアリエント,サーラ
ベルターニ,バルバラ
パーラ,ダニエーレ
バリッリ,アレッシオ
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キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ
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    • 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
    • C07D401/02Heterocyclic 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
    • 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
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    • 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)
JP2023502861A 2020-07-15 2021-07-14 Alk5阻害剤としてのピリダジニルアミノ誘導体 Active JP7686741B2 (ja)

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 (4)

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JP2023533849A JP2023533849A (ja) 2023-08-04
JP2023533849A5 JP2023533849A5 (https=) 2024-07-22
JPWO2022013307A5 JPWO2022013307A5 (https=) 2024-07-22
JP7686741B2 true JP7686741B2 (ja) 2025-06-02

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JP2023502861A Active JP7686741B2 (ja) 2020-07-15 2021-07-14 Alk5阻害剤としてのピリダジニルアミノ誘導体

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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=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
KR20240159754A (ko) * 2023-04-28 2024-11-06 한국원자력의학원 N-메틸피페라진 에탄올 카바메이트(N-methylpiperazine ethanol carbamate) 구조를 포함하는 신규 화합물 및 이의 용도
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

Citations (6)

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WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2006503043A (ja) 2002-09-10 2006-01-26 サイオス インク. TGFβ阻害剤
JP2007533635A (ja) 2003-09-30 2007-11-22 アムジエン・インコーポレーテツド バニロイド受容体リガンドおよび治療おけるこれらの使用
JP2013510103A (ja) 2009-11-07 2013-03-21 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング TGF−β受容体キナーゼ阻害剤としてのヘテロアリールアミノキノリン
JP2017501200A (ja) 2014-01-01 2017-01-12 メディベイション テクノロジーズ, インコーポレイテッド 化合物及び使用方法
WO2020012357A1 (en) 2018-07-10 2020-01-16 Integral Biosciences Pvt. Ltd. Heterocyclic compounds and methods of use

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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
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
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 )
DK2731949T3 (en) 2011-07-13 2018-06-14 Tiumbio Co Ltd 2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND / OR ALK4 INHIBITORS

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2006503043A (ja) 2002-09-10 2006-01-26 サイオス インク. TGFβ阻害剤
JP2007533635A (ja) 2003-09-30 2007-11-22 アムジエン・インコーポレーテツド バニロイド受容体リガンドおよび治療おけるこれらの使用
JP2013510103A (ja) 2009-11-07 2013-03-21 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング TGF−β受容体キナーゼ阻害剤としてのヘテロアリールアミノキノリン
JP2017501200A (ja) 2014-01-01 2017-01-12 メディベイション テクノロジーズ, インコーポレイテッド 化合物及び使用方法
WO2020012357A1 (en) 2018-07-10 2020-01-16 Integral Biosciences Pvt. Ltd. Heterocyclic compounds and methods of use

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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
KR20230051500A (ko) 2023-04-18
US12479826B2 (en) 2025-11-25
BR112023000588A8 (pt) 2023-05-09
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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