JP7649560B2 - 新規fyn及びvegfr2キナーゼ阻害剤 - Google Patents

新規fyn及びvegfr2キナーゼ阻害剤 Download PDF

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JP7649560B2
JP7649560B2 JP2022534848A JP2022534848A JP7649560B2 JP 7649560 B2 JP7649560 B2 JP 7649560B2 JP 2022534848 A JP2022534848 A JP 2022534848A JP 2022534848 A JP2022534848 A JP 2022534848A JP 7649560 B2 JP7649560 B2 JP 7649560B2
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ethyl
pyrazol
phenyl
benzamide
compound
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JP2023505684A (ja
JPWO2021116005A5 (enExample
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クラウディオ ロヴァティ、ルチオ
カゼッリ、ジャンフランコ
アルトゥシ、ロベルト
メンヌーニ、ラウラ
コラーチェ、ファブリツィオ
マンデッリ、ステファノ
ボヴィーノ、クララ
マガラチー、フィリッポ
ブッツィ、ベネデッタ
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ロッタファーム・バイオテック・エッセ・エッレ・エッレ
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2022534848A 2019-12-09 2020-12-07 新規fyn及びvegfr2キナーゼ阻害剤 Active JP7649560B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EPPCT/EP2019/084287 2019-12-09
PCT/EP2019/084287 WO2021115560A1 (en) 2019-12-09 2019-12-09 New fyn and vegfr2 kinase inhibitors
PCT/EP2020/084847 WO2021116005A1 (en) 2019-12-09 2020-12-07 New fyn and vegfr2 kinase inhibitors

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JP2023505684A JP2023505684A (ja) 2023-02-10
JPWO2021116005A5 JPWO2021116005A5 (enExample) 2023-12-07
JP7649560B2 true JP7649560B2 (ja) 2025-03-21

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EP (1) EP4073057B1 (enExample)
JP (1) JP7649560B2 (enExample)
CN (1) CN115279747B (enExample)
ES (1) ES2972638T3 (enExample)
WO (2) WO2021115560A1 (enExample)

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003517447A (ja) 1998-11-06 2003-05-27 ビーエーエスエフ アクチェンゲゼルシャフト 三環式ピラゾール誘導体
JP2009541480A (ja) 2006-06-30 2009-11-26 アストラゼネカ アクチボラグ 癌の治療において有用なピリミジン誘導体
JP2010529990A (ja) 2007-06-15 2010-09-02 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤およびそれを使用するための方法
JP2011506454A (ja) 2007-12-13 2011-03-03 グラクソスミスクライン エルエルシー チアゾールおよびオキサゾールキナーゼ阻害薬
US20130172353A1 (en) 2011-12-28 2013-07-04 Allergan, Inc. 3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivatives as kinase inhibitors
JP2018507857A (ja) 2015-03-18 2018-03-22 ロッタファーム・バイオテック・エッセ・エッレ・エッレ 新規fynキナーゼ阻害剤
JP2018531916A (ja) 2015-09-09 2018-11-01 ウォーレン シー. ラウ, 新規のfynキナーゼ阻害剤の方法、組成物、及び使用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1848694T3 (da) 2005-02-07 2010-01-25 Hoffmann La Roche Heterocykliske substituerede phenylmethanoner som inhibitorer af glycintransporter
JP5301469B2 (ja) 2007-02-26 2013-09-25 メルク カナダ インコーポレイテッド Ep4受容体アンタゴニストとしてのインドール及びインドリンシクロプロピルアミド誘導体

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003517447A (ja) 1998-11-06 2003-05-27 ビーエーエスエフ アクチェンゲゼルシャフト 三環式ピラゾール誘導体
JP2009541480A (ja) 2006-06-30 2009-11-26 アストラゼネカ アクチボラグ 癌の治療において有用なピリミジン誘導体
JP2010529990A (ja) 2007-06-15 2010-09-02 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤およびそれを使用するための方法
JP2011506454A (ja) 2007-12-13 2011-03-03 グラクソスミスクライン エルエルシー チアゾールおよびオキサゾールキナーゼ阻害薬
US20130172353A1 (en) 2011-12-28 2013-07-04 Allergan, Inc. 3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivatives as kinase inhibitors
JP2018507857A (ja) 2015-03-18 2018-03-22 ロッタファーム・バイオテック・エッセ・エッレ・エッレ 新規fynキナーゼ阻害剤
JP2018531916A (ja) 2015-09-09 2018-11-01 ウォーレン シー. ラウ, 新規のfynキナーゼ阻害剤の方法、組成物、及び使用

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WO2021115560A1 (en) 2021-06-17
CN115279747A (zh) 2022-11-01
ES2972638T3 (es) 2024-06-13
CN115279747B (zh) 2024-11-05
EP4073057B1 (en) 2023-11-29
WO2021116005A8 (en) 2022-07-14
WO2021116005A1 (en) 2021-06-17
JP2023505684A (ja) 2023-02-10
US20230061118A1 (en) 2023-03-02
EP4073057A1 (en) 2022-10-19

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