CN113302184B - 1,3,4-噁二唑啉酮化合物和药物 - Google Patents

1,3,4-噁二唑啉酮化合物和药物 Download PDF

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Publication number
CN113302184B
CN113302184B CN201980089037.7A CN201980089037A CN113302184B CN 113302184 B CN113302184 B CN 113302184B CN 201980089037 A CN201980089037 A CN 201980089037A CN 113302184 B CN113302184 B CN 113302184B
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China
Prior art keywords
oxadiazol
amino
phenyl
ethyl
trifluoromethyl
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Chinese (zh)
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CN113302184A (zh
Inventor
神谷博贵
材木久晃
春田刚位
菊池雄大
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Nippon Shinyaku Co Ltd
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Nippon Shinyaku Co Ltd
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    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
    • A61K31/55—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
    • 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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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
    • C07D471/08—Bridged systems
    • 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
    • C07D471/10—Spiro-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
    • C07D487/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN201980089037.7A 2018-11-15 2019-11-14 1,3,4-噁二唑啉酮化合物和药物 Active CN113302184B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2018214950 2018-11-15
JP2018-214950 2018-11-15
PCT/JP2019/044615 WO2020100959A1 (ja) 2018-11-15 2019-11-14 １，３，４－オキサジアゾロン化合物及び医薬

Publications (2)

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CN113302184A CN113302184A (zh) 2021-08-24
CN113302184B true CN113302184B (zh) 2024-11-22

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US (1) US20220024921A1 (https=)
EP (1) EP3882239A4 (https=)
JP (1) JP7434172B2 (https=)
KR (1) KR20210091767A (https=)
CN (1) CN113302184B (https=)
AU (1) AU2019381493B2 (https=)
BR (1) BR112021009198A2 (https=)
CA (1) CA3117550A1 (https=)
CL (1) CL2021001275A1 (https=)
CO (1) CO2021007442A2 (https=)
EA (1) EA202191349A1 (https=)
EC (1) ECSP21034281A (https=)
IL (1) IL282999A (https=)
MA (1) MA54243A (https=)
MX (1) MX2021005566A (https=)
PE (1) PE20211283A1 (https=)
PH (1) PH12021551103A1 (https=)
SA (1) SA521421997B1 (https=)
SG (1) SG11202104371XA (https=)
TW (1) TWI840448B (https=)
UA (1) UA129949C2 (https=)
WO (1) WO2020100959A1 (https=)

Families Citing this family (3)

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Publication number Priority date Publication date Assignee Title
EP4516778A4 (en) 2022-04-25 2026-04-29 Nippon Shinyaku Co Ltd COMPOUND SERVING AS A DDR1 KINASE INHIBITOR AND MEDICINE
CN117285459B (zh) * 2023-11-24 2024-02-27 上海美迪西生物医药股份有限公司 一种小分子激酶抑制剂化合物的制备方法
CN118515653B (zh) * 2024-07-23 2024-12-10 西湖制药(杭州)有限公司 一种ezh2特异性抑制剂及其制备方法和用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060223801A1 (en) * 2003-09-13 2006-10-05 Astrazeneca Ab Pyrrol derivatives with antibacterial activity
GB201814151D0 (en) * 2018-08-31 2018-10-17 Ucl Business Plc Compounds

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JPH01139581A (ja) * 1987-08-20 1989-06-01 Nissan Chem Ind Ltd テトラヒドロフタルイミド誘導体、その製法および除草剤
EP1797040A1 (en) 2004-09-29 2007-06-20 Ranbaxy Laboratories Limited Muscarinic receptor antagonists
CA2591738A1 (en) 2004-12-22 2006-06-29 Merck & Co., Inc. Process for making substituted piperidines
JP2011515337A (ja) 2008-02-29 2011-05-19 サイレーン ファーマシューティカルズ， インコーポレイテッド プロテインキナーゼモジュレーター
GB0813740D0 (en) 2008-07-28 2008-09-03 Angeletti P Ist Richerche Biologica Therapeutic compounds
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為ｐｉｍ激酶抑制劑之三唑吡啶化合物
CA2819373A1 (en) * 2010-12-09 2012-06-14 Amgen Inc. Bicyclic compounds as pim inhibitors
JP2014510105A (ja) 2011-03-22 2014-04-24 アムジエン・インコーポレーテツド Ｐｉｍ阻害剤としてのアゾール化合物
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
CN104540830A (zh) 2012-06-07 2015-04-22 霍夫曼-拉罗奇有限公司 端锚聚合酶的吡唑并嘧啶酮和吡唑并吡啶酮抑制剂

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060223801A1 (en) * 2003-09-13 2006-10-05 Astrazeneca Ab Pyrrol derivatives with antibacterial activity
GB201814151D0 (en) * 2018-08-31 2018-10-17 Ucl Business Plc Compounds

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Publication number Publication date
AU2019381493B2 (en) 2024-10-31
SA521421997B1 (ar) 2025-04-10
JP7434172B2 (ja) 2024-02-20
PH12021551103A1 (en) 2021-11-22
CL2021001275A1 (es) 2021-11-05
JPWO2020100959A1 (ja) 2021-10-07
ECSP21034281A (es) 2021-06-30
PE20211283A1 (es) 2021-07-19
EP3882239A1 (en) 2021-09-22
US20220024921A1 (en) 2022-01-27
MA54243A (fr) 2021-09-22
AU2019381493A1 (en) 2021-06-03
TWI840448B (zh) 2024-05-01
UA129949C2 (uk) 2025-09-24
TW202031649A (zh) 2020-09-01
KR20210091767A (ko) 2021-07-22
WO2020100959A1 (ja) 2020-05-22
EP3882239A4 (en) 2022-08-10
IL282999A (en) 2021-06-30
CN113302184A (zh) 2021-08-24
SG11202104371XA (en) 2021-05-28
EA202191349A1 (ru) 2021-08-10
CA3117550A1 (en) 2020-05-22
CO2021007442A2 (es) 2021-06-21
MX2021005566A (es) 2021-07-15
BR112021009198A2 (pt) 2021-08-03

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