CN112074519B - 作为rip1激酶抑制剂用于治疗例如肠易激综合征(ibs)的化合物 - Google Patents

作为rip1激酶抑制剂用于治疗例如肠易激综合征(ibs)的化合物 Download PDF

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CN112074519B
CN112074519B CN201980026880.0A CN201980026880A CN112074519B CN 112074519 B CN112074519 B CN 112074519B CN 201980026880 A CN201980026880 A CN 201980026880A CN 112074519 B CN112074519 B CN 112074519B
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CN112074519A (zh
CN112074519A8 (zh
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S·帕特尔
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically 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)
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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)
CN201980026880.0A 2018-04-20 2019-04-18 作为rip1激酶抑制剂用于治疗例如肠易激综合征(ibs)的化合物 Active CN112074519B (zh)

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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CN112074519A CN112074519A (zh) 2020-12-11
CN112074519A8 CN112074519A8 (zh) 2021-05-11
CN112074519B true CN112074519B (zh) 2024-08-02

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US (1) US11634436B2 (https=)
EP (1) EP3781571B1 (https=)
JP (1) JP7398391B2 (https=)
CN (1) CN112074519B (https=)
WO (1) WO2019204537A1 (https=)

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EP3526219B1 (en) 2016-10-17 2021-12-15 F. Hoffmann-La Roche AG Bicyclic pyridone lactams and methods of use thereof
US11072607B2 (en) 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
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
GB202010409D0 (en) * 2020-07-07 2020-08-19 Reviral Ltd Pharmaceutical compounds
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
JP7398391B2 (ja) 2023-12-14
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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Correction item: Denomination of Invention

Correct: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza * - 3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

False: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza-3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

Number: 50-02

Page: The title page

Volume: 36

Correction item: Denomination of Invention

Correct: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza * - 3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

False: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza-3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

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