JP7398391B2 - N-[4-オキソ-2,3-ジヒドロ-1,5-ベンズオキサゼピン-3-イル]-5,6-ジヒドロ-4H-ピロロ[1,2-b]ピラゾール-2-カルボキサミド誘導体及び例えば過敏性腸症候群(IBS)を処置するためのRIP1キナーゼ阻害剤としての関連化合物 - Google Patents

N-[4-オキソ-2,3-ジヒドロ-1,5-ベンズオキサゼピン-3-イル]-5,6-ジヒドロ-4H-ピロロ[1,2-b]ピラゾール-2-カルボキサミド誘導体及び例えば過敏性腸症候群(IBS)を処置するためのRIP1キナーゼ阻害剤としての関連化合物 Download PDF

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JP7398391B2
JP7398391B2 JP2020558018A JP2020558018A JP7398391B2 JP 7398391 B2 JP7398391 B2 JP 7398391B2 JP 2020558018 A JP2020558018 A JP 2020558018A JP 2020558018 A JP2020558018 A JP 2020558018A JP 7398391 B2 JP7398391 B2 JP 7398391B2
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JP2021522206A (ja
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パテル,スナヘル
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F Hoffmann La Roche AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2020558018A 2018-04-20 2019-04-18 N-[4-オキソ-2,3-ジヒドロ-1,5-ベンズオキサゼピン-3-イル]-5,6-ジヒドロ-4H-ピロロ[1,2-b]ピラゾール-2-カルボキサミド誘導体及び例えば過敏性腸症候群(IBS)を処置するためのRIP1キナーゼ阻害剤としての関連化合物 Active JP7398391B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862660397P 2018-04-20 2018-04-20
US62/660,397 2018-04-20
PCT/US2019/028011 WO2019204537A1 (en) 2018-04-20 2019-04-18 N-[4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol e-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs)

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JP2021522206A JP2021522206A (ja) 2021-08-30
JPWO2019204537A5 JPWO2019204537A5 (https=) 2022-04-22
JP2021522206A5 JP2021522206A5 (https=) 2022-04-22
JP7398391B2 true JP7398391B2 (ja) 2023-12-14

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US (1) US11634436B2 (https=)
EP (1) EP3781571B1 (https=)
JP (1) JP7398391B2 (https=)
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WO (1) WO2019204537A1 (https=)

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CN112689636B (zh) 2018-09-10 2024-08-20 科研制药株式会社 新型杂原子芳香族酰胺衍生物以及含有其的药剂
WO2021046515A1 (en) 2019-09-06 2021-03-11 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase i for the treatment of disease
IL291665B2 (en) 2019-09-27 2025-07-01 Univ Texas Inhibitors of receptor interacting protein kinase i for the treatment of disease
JP2023502514A (ja) * 2019-11-26 2023-01-24 ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム 疾患の処置のための受容体相互作用プロテインキナーゼiの阻害剤
JP7701162B2 (ja) * 2020-02-28 2025-07-01 科研製薬株式会社 新規ヘテロ芳香族アミド誘導体又はその塩からなる医薬
AU2021225921A1 (en) * 2020-02-28 2022-09-22 Board Of Regents, The University Of Texas System Inhibitors of Receptor Interacting Protein Kinase I for the treatment of disease
AR121717A1 (es) * 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
CN115038707B (zh) * 2020-05-14 2024-11-22 中国医药研究开发中心有限公司 氮杂卓类稠环化合物及其医药用途
TW202214617A (zh) 2020-06-02 2022-04-16 法商賽諾菲公司 作為ripk1抑制劑之異㗁唑啶及其用途
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AU2021329777A1 (en) * 2020-08-18 2023-03-09 Hutchison Medipharma Limited Pyrimidinone compounds and uses thereof
WO2022171111A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Heteroaryl-fused bicyclic compound as rip1-kinase inhibitors and uses thereof
WO2023020486A1 (zh) * 2021-08-17 2023-02-23 广州市恒诺康医药科技有限公司 Rip1激酶抑制剂类化合物及其组合物和用途
CN115806557B (zh) * 2021-09-14 2025-02-14 中国科学院上海有机化学研究所 抑制细胞程序性死亡的化合物及其制备方法
WO2023083847A1 (en) 2021-11-11 2023-05-19 Sanofi Isoxazolidines as ripk1 inhibitors and use thereof
WO2023109918A1 (zh) * 2021-12-17 2023-06-22 中国科学院上海药物研究所 含氮杂环化合物、其制备方法及其用途
CN116640156B (zh) * 2022-02-22 2025-10-24 上海齐鲁制药研究中心有限公司 Ripk1抑制剂
CN117645579A (zh) * 2022-09-02 2024-03-05 科辉智药生物科技(深圳)有限公司 作为ripk1抑制剂的氮杂䓬类稠环化合物及其应用

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EP3781571C0 (en) 2024-01-17
WO2019204537A1 (en) 2019-10-24
JP2021522206A (ja) 2021-08-30
CN112074519B (zh) 2024-08-02
CN112074519A (zh) 2020-12-11
EP3781571B1 (en) 2024-01-17
US11634436B2 (en) 2023-04-25
EP3781571A1 (en) 2021-02-24
US20210032271A1 (en) 2021-02-04
CN112074519A8 (zh) 2021-05-11

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