CN114466849B - 作为isoqc和/或qc酶的抑制剂的n-取代的-3,4-(稠合5-环)-5-苯基-吡咯烷-2-酮化合物 - Google Patents

作为isoqc和/或qc酶的抑制剂的n-取代的-3,4-(稠合5-环)-5-苯基-吡咯烷-2-酮化合物 Download PDF

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CN114466849B
CN114466849B CN202080056962.2A CN202080056962A CN114466849B CN 114466849 B CN114466849 B CN 114466849B CN 202080056962 A CN202080056962 A CN 202080056962A CN 114466849 B CN114466849 B CN 114466849B
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CN114466849A (zh
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巴斯蒂安·埃弗斯
保罗·E·布伦南
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Hinik Immunization Co ltd
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202080056962.2A 2019-07-12 2020-07-10 作为isoqc和/或qc酶的抑制剂的n-取代的-3,4-(稠合5-环)-5-苯基-吡咯烷-2-酮化合物 Active CN114466849B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19185997 2019-07-12
EP19185997.4 2019-07-12
PCT/EP2020/069630 WO2021009068A1 (en) 2019-07-12 2020-07-10 N-substituted-3,4-(fused 5-ring)-5-phenyl-pyrrolidine-2-one compounds as inhibitors of isoqc and/or qc enzyme

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CN114466849A CN114466849A (zh) 2022-05-10
CN114466849B true CN114466849B (zh) 2024-07-12

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US (1) US20230077723A1 (enExample)
EP (1) EP3997091A1 (enExample)
JP (1) JP2022542540A (enExample)
KR (1) KR20220054293A (enExample)
CN (1) CN114466849B (enExample)
AU (1) AU2020312647A1 (enExample)
BR (1) BR112022000505A8 (enExample)
CA (1) CA3147154A1 (enExample)
IL (1) IL289784A (enExample)
MX (1) MX2022000521A (enExample)
PH (1) PH12022550079A1 (enExample)
WO (1) WO2021009068A1 (enExample)

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CA3226468A1 (en) 2021-08-02 2023-02-09 Andrew Edmunds Microbiocidal pyrazole derivatives
AU2022203580A1 (en) * 2021-09-17 2023-04-06 Academia Sinica Methods of Increasing Cell Phagocytosis
JP2024546927A (ja) 2021-12-17 2024-12-26 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺微生物性ピラゾール誘導体
TW202430514A (zh) 2022-09-30 2024-08-01 瑞士商先正達農作物保護股份公司 殺微生物之吡唑衍生物
PY2403614A (es) 2023-01-27 2025-09-11 Syngenta Crop Protection Ag Derivados de pirazol microbiocidas
AR131665A1 (es) 2023-02-01 2025-04-16 Syngenta Crop Protection Ag Composiciones fungicidas
EP4455142A1 (en) 2023-04-26 2024-10-30 Scenic Immunology B.V. Novel inhibitor of qpctl and/or qc
PY2447478A (es) 2023-06-14 2025-03-18 Syngenta Crop Protection Ag Composiciones fungicidas
WO2025114167A1 (en) 2023-11-28 2025-06-05 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2025163143A1 (en) 2024-02-02 2025-08-07 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2025191053A1 (en) 2024-03-14 2025-09-18 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2025224308A1 (en) * 2024-04-25 2025-10-30 Scenic Immunology B.V. Qpctl inhibitors
WO2026022173A1 (en) 2024-07-26 2026-01-29 Syngenta Crop Protection Ag Microbiocidal pyrazole compounds

Citations (1)

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CN105408335A (zh) * 2013-05-27 2016-03-16 诺华股份有限公司 吡唑并吡咯烷衍生物及其在治疗疾病中的用途

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CN102186475B (zh) * 2008-09-04 2016-08-03 前体生物药物股份公司 新抑制剂
MX2015016421A (es) * 2013-05-28 2016-03-03 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades.
KR102084185B1 (ko) * 2013-08-29 2020-03-04 주식회사 대웅제약 테트라히드로사이클로펜타피롤 유도체 및 이의 제조방법
EP3747438A1 (en) * 2017-07-24 2020-12-09 Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis Treating pathological conditions by direct and indirect targeting of sirpa - cd47 interaction

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CN105408335A (zh) * 2013-05-27 2016-03-16 诺华股份有限公司 吡唑并吡咯烷衍生物及其在治疗疾病中的用途

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US20230077723A1 (en) 2023-03-16
JP2022542540A (ja) 2022-10-05
PH12022550079A1 (en) 2023-04-12
CN114466849A (zh) 2022-05-10
IL289784A (en) 2022-03-01
BR112022000505A2 (pt) 2022-03-22
BR112022000505A8 (pt) 2022-04-12
MX2022000521A (es) 2022-06-14
CA3147154A1 (en) 2021-01-21
WO2021009068A1 (en) 2021-01-21
KR20220054293A (ko) 2022-05-02
EP3997091A1 (en) 2022-05-18
AU2020312647A1 (en) 2022-02-24

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