JP7433463B2 - ピリミジン含有含窒素二環化合物 - Google Patents

ピリミジン含有含窒素二環化合物 Download PDF

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JP7433463B2
JP7433463B2 JP2022553287A JP2022553287A JP7433463B2 JP 7433463 B2 JP7433463 B2 JP 7433463B2 JP 2022553287 A JP2022553287 A JP 2022553287A JP 2022553287 A JP2022553287 A JP 2022553287A JP 7433463 B2 JP7433463 B2 JP 7433463B2
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salt
mmol
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JPWO2022070289A1 (https=
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浩一郎 新井
健一郎 鷹羽
公和 跡部
好聖 高島
直美 青野
アンドリュー ジョン ポッター
ダニエル ポール マドックス
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Vernalis R&D Ltd
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    • 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
    • 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • C07D417/08Heterocyclic 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 carbon chain containing alicyclic 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
    • C07D417/14Heterocyclic 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
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07D498/08Bridged 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
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/18Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2022553287A 2020-09-30 2020-09-30 ピリミジン含有含窒素二環化合物 Active JP7433463B2 (ja)

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PCT/JP2020/037048 WO2022070289A1 (ja) 2020-09-30 2020-09-30 ピリミジン含有含窒素二環化合物

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JPWO2022070289A1 JPWO2022070289A1 (https=) 2022-04-07
JP7433463B2 true JP7433463B2 (ja) 2024-02-19

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US (1) US12590090B2 (https=)
EP (1) EP4223750B1 (https=)
JP (1) JP7433463B2 (https=)
KR (1) KR20230084145A (https=)
CN (1) CN116194454B (https=)
AU (1) AU2020471055B8 (https=)
CA (1) CA3194164A1 (https=)
ES (1) ES3036969T3 (https=)
MX (1) MX2023003698A (https=)
PL (1) PL4223750T3 (https=)
WO (1) WO2022070289A1 (https=)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012068546A1 (en) 2010-11-19 2012-05-24 Ligand Pharmaceuticals Incorporated Heterocycle amines and uses thereof
WO2013106614A1 (en) 2012-01-13 2013-07-18 Bristol-Myers Squibb Company Triazolyl-substituted pyridyl compounds useful as kinase inhibitors
WO2019070093A1 (en) 2017-10-02 2019-04-11 1ST Biotherapeutics, Inc. BENZOTHIAZOL COMPOUNDS AND METHODS OF USING THE SAME FOR TREATING NEURODEGENERATIVE DISORDERS

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110003219A (zh) 2010-07-13 2019-07-12 弗·哈夫曼-拉罗切有限公司 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物
US9169260B2 (en) * 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
EP2691399B1 (en) 2011-03-28 2016-07-13 F.Hoffmann-La Roche Ag Thiazolopyrimidine compounds
WO2013042137A1 (en) 2011-09-19 2013-03-28 Aurigene Discovery Technologies Limited Bicyclic heterocycles as irak4 inhibitors
EP2802590B1 (en) 2012-01-10 2017-03-01 F. Hoffmann-La Roche AG Thienopyrimidine compounds
RU2548363C2 (ru) 2012-01-25 2015-04-20 Общество с ограниченной ответственностью "Асинэкс Медхим." СЕЛЕКТИВНЫЕ ИНГИБИТОРЫ Haspin киназы
CN106232122A (zh) 2013-09-27 2016-12-14 林伯士艾瑞斯公司 Irak抑制剂和其用途
DK3126330T3 (en) 2014-04-04 2019-04-23 Pfizer BICYCLE-FUSED HETEROARYL OR ARYL COMPOUNDS AND USE THEREOF AS IRAC4 INHIBITORS
US9969749B2 (en) 2014-09-30 2018-05-15 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
US10329294B2 (en) 2015-03-12 2019-06-25 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of IRAK4 activity
CN108473498B (zh) * 2015-12-22 2021-11-02 豪夫迈·罗氏有限公司 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物
CN106946890A (zh) * 2017-04-26 2017-07-14 中国药科大学 吡啶类irak4抑制剂、其制备方法及应用
WO2022070288A1 (ja) * 2020-09-30 2022-04-07 旭化成ファーマ株式会社 含窒素二環化合物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012068546A1 (en) 2010-11-19 2012-05-24 Ligand Pharmaceuticals Incorporated Heterocycle amines and uses thereof
WO2013106614A1 (en) 2012-01-13 2013-07-18 Bristol-Myers Squibb Company Triazolyl-substituted pyridyl compounds useful as kinase inhibitors
WO2019070093A1 (en) 2017-10-02 2019-04-11 1ST Biotherapeutics, Inc. BENZOTHIAZOL COMPOUNDS AND METHODS OF USING THE SAME FOR TREATING NEURODEGENERATIVE DISORDERS

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HEIFETZ,A. et al.,Fragment Molecular Orbital Method Applied to Lead Optimization of Novel Interleukin-2 Inducible T-Ce,Journal of Medicinal Chemistry,2016年,Vol.59, No.9,pp.4352-4363,DOI 10.1021/acs.jmedchem.6b00045
NAIR,S. et al.,Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Mod,ACS Medicinal Chemistry Letters,2020年06月10日,Vol.11, No.7,pp.1402-1409,DOI 10.1021/acsmedchemlett.0c00082

Also Published As

Publication number Publication date
WO2022070289A1 (ja) 2022-04-07
ES3036969T3 (en) 2025-09-25
US12590090B2 (en) 2026-03-31
AU2020471055B8 (en) 2023-12-21
CN116194454B (zh) 2025-02-18
PL4223750T3 (pl) 2025-09-15
EP4223750A4 (en) 2024-06-19
CA3194164A1 (en) 2022-04-07
JPWO2022070289A1 (https=) 2022-04-07
AU2020471055B2 (en) 2023-12-14
KR20230084145A (ko) 2023-06-12
MX2023003698A (es) 2023-06-15
CN116194454A (zh) 2023-05-30
US20240025893A1 (en) 2024-01-25
EP4223750A1 (en) 2023-08-09
EP4223750B1 (en) 2025-06-25
AU2020471055A1 (en) 2023-05-04

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