CN115461338B - 具有kdm5抑制活性的3-氮杂二环(3.1.0)己烷衍生物及其用途 - Google Patents

具有kdm5抑制活性的3-氮杂二环(3.1.0)己烷衍生物及其用途 Download PDF

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Publication number
CN115461338B
CN115461338B CN202180032139.2A CN202180032139A CN115461338B CN 115461338 B CN115461338 B CN 115461338B CN 202180032139 A CN202180032139 A CN 202180032139A CN 115461338 B CN115461338 B CN 115461338B
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azabicyclo
mmol
general formula
substituted
alkyl
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CN115461338A (zh
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角内章人
梅村周平
浅田正树
安纳托利.鲁文斯基
张艳
高桥秀典
哥伦.克里洛夫
猪山大吾
凯尔.康兹
麦兹.史文森
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Ono Pharmaceutical Co Ltd
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Ono Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CN202180032139.2A 2020-05-07 2021-05-06 具有kdm5抑制活性的3-氮杂二环(3.1.0)己烷衍生物及其用途 Active CN115461338B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2020/088925 2020-05-07
CN2020088925 2020-05-07
PCT/CN2021/091843 WO2021223699A1 (en) 2020-05-07 2021-05-06 3-azabicyclo(3.1.0)hexane derivatives having kdm5 inhibitory activity and use thereof

Publications (2)

Publication Number Publication Date
CN115461338A CN115461338A (zh) 2022-12-09
CN115461338B true CN115461338B (zh) 2024-02-20

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CN202180032139.2A Active CN115461338B (zh) 2020-05-07 2021-05-06 具有kdm5抑制活性的3-氮杂二环(3.1.0)己烷衍生物及其用途

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Country Link
US (3) US11691968B2 (https=)
EP (2) EP4471027A1 (https=)
JP (3) JP7643466B2 (https=)
KR (2) KR20260046494A (https=)
CN (1) CN115461338B (https=)
AU (1) AU2021268223B2 (https=)
BR (1) BR112022022005A2 (https=)
CA (1) CA3181604A1 (https=)
ES (1) ES3037418T3 (https=)
IL (1) IL297900B2 (https=)
MX (1) MX2022013692A (https=)
NZ (1) NZ793960A (https=)
TW (1) TWI895412B (https=)
WO (1) WO2021223699A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3999183A4 (en) * 2019-07-17 2023-11-15 Ono Pharmaceutical Co., Ltd. COMPOUNDS HAVING KDM5 INHIBITANT ACTION AND THEIR PHARMACEUTICAL USES
ES3037418T3 (en) 2020-05-07 2025-10-01 Ono Pharmaceutical Co 3-azabicyclo(3.1.0)hexane derivatives having kdm5 inhibitory activity and use thereof
JP7743829B2 (ja) * 2021-11-05 2025-09-25 小野薬品工業株式会社 Kdm5阻害作用を有する化合物を含有する医薬組成物
WO2025239445A1 (ja) * 2024-05-17 2025-11-20 小野薬品工業株式会社 認知症の行動および心理症状の予防、進行抑制および/または治療剤

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1331679A (zh) * 1998-12-23 2002-01-16 辉瑞大药厂 作为阿片受体配体的3-氮杂二环[3.1.0]己烷衍生物
WO2016057924A1 (en) * 2014-10-10 2016-04-14 Genentech, Inc. Pyrrolidine amide compounds as histone demethylase inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0311859D0 (en) 2003-05-22 2003-06-25 Merck Sharp & Dohme Therapeutic agents
JP5017103B2 (ja) 2004-06-17 2012-09-05 トランスフオーム・フアーマシユーチカルズ・インコーポレーテツド 薬剤共結晶組成物および関連した使用方法
JP2008524331A (ja) 2004-12-21 2008-07-10 武田薬品工業株式会社 ジペプチジルペプチダーゼ阻害剤
RU2487127C2 (ru) 2007-10-09 2013-07-10 Ф.Хоффманн-Ля Рош Аг Хиральные цис-имидазолины
CN108341819B (zh) 2017-01-22 2021-06-15 南京药捷安康生物科技有限公司 磷酸二酯酶抑制剂及其用途
EP3999183A4 (en) 2019-07-17 2023-11-15 Ono Pharmaceutical Co., Ltd. COMPOUNDS HAVING KDM5 INHIBITANT ACTION AND THEIR PHARMACEUTICAL USES
ES3037418T3 (en) 2020-05-07 2025-10-01 Ono Pharmaceutical Co 3-azabicyclo(3.1.0)hexane derivatives having kdm5 inhibitory activity and use thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1331679A (zh) * 1998-12-23 2002-01-16 辉瑞大药厂 作为阿片受体配体的3-氮杂二环[3.1.0]己烷衍生物
WO2016057924A1 (en) * 2014-10-10 2016-04-14 Genentech, Inc. Pyrrolidine amide compounds as histone demethylase inhibitors

Also Published As

Publication number Publication date
IL297900B2 (en) 2026-04-01
JP7643466B2 (ja) 2025-03-11
WO2021223699A1 (en) 2021-11-11
JP2023524547A (ja) 2023-06-12
IL297900B1 (en) 2025-12-01
CN115461338A (zh) 2022-12-09
IL297900A (en) 2023-01-01
US12269817B2 (en) 2025-04-08
EP4146645A1 (en) 2023-03-15
US20230271952A1 (en) 2023-08-31
TWI895412B (zh) 2025-09-01
CA3181604A1 (en) 2021-11-11
KR20260046494A (ko) 2026-04-07
TW202200571A (zh) 2022-01-01
JP7643632B2 (ja) 2025-03-11
JP2025081677A (ja) 2025-05-27
KR20230007352A (ko) 2023-01-12
AU2021268223B2 (en) 2025-10-09
AU2021268223A1 (en) 2022-12-08
US20250214984A1 (en) 2025-07-03
EP4471027A1 (en) 2024-12-04
BR112022022005A2 (pt) 2022-12-13
US20230109293A1 (en) 2023-04-06
JP2024177345A (ja) 2024-12-19
KR102937044B1 (ko) 2026-03-09
ES3037418T3 (en) 2025-10-01
EP4146645B1 (en) 2025-06-25
US11691968B2 (en) 2023-07-04
NZ793960A (en) 2025-12-19
MX2022013692A (es) 2022-11-30

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