JP7179049B2 - オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途 - Google Patents

オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途 Download PDF

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JP7179049B2
JP7179049B2 JP2020504160A JP2020504160A JP7179049B2 JP 7179049 B2 JP7179049 B2 JP 7179049B2 JP 2020504160 A JP2020504160 A JP 2020504160A JP 2020504160 A JP2020504160 A JP 2020504160A JP 7179049 B2 JP7179049 B2 JP 7179049B2
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JPWO2019024845A5 (enExample
JP2020528913A (ja
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チェン、ミンホア
チャン、イェンフォン
ホアン、チュンシアン
チャン、シアオユイ
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Bergen Pharmaceutical LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • 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
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020504160A 2017-08-01 2018-07-31 オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途 Active JP7179049B2 (ja)

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JP2022182194A JP2023027066A (ja) 2017-08-01 2022-11-15 オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途

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CN201710648135.2 2017-08-01
CN201710648135 2017-08-01
PCT/CN2018/097797 WO2019024845A1 (zh) 2017-08-01 2018-07-31 一种食欲素受体拮抗剂的晶型及其制备方法和用途

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JP2020528913A JP2020528913A (ja) 2020-10-01
JPWO2019024845A5 JPWO2019024845A5 (enExample) 2022-03-02
JP7179049B2 true JP7179049B2 (ja) 2022-11-28

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JP2022182194A Pending JP2023027066A (ja) 2017-08-01 2022-11-15 オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途

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US (1) US10759779B2 (enExample)
JP (2) JP7179049B2 (enExample)
CN (2) CN115710250A (enExample)
WO (1) WO2019024845A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115710250A (zh) * 2017-08-01 2023-02-24 博健制药有限责任公司 一种食欲素受体拮抗剂的晶型及其制备方法和用途
EP4506325A3 (en) * 2019-05-15 2025-04-30 Eisai R&D Management Co., Ltd. Method and compound useful in preparation of orexin-2 receptor antagonist, and lemborexant having few impurities
WO2020263253A1 (en) * 2019-06-26 2020-12-30 Moline Margaret Lemborexant for treating sleep issues
WO2021050219A1 (en) * 2019-09-13 2021-03-18 Eisai R&D Management Co., Ltd. Pharmaceutical composition for treating insomnia
EP4073058A1 (en) 2019-12-11 2022-10-19 Teva Czech Industries s.r.o. Solid state form of lemborexant
MX2022008260A (es) * 2020-01-16 2022-08-04 Eisai R&D Man Co Ltd Sustancia farmacologica de lemborexant y composicion medicinal que la comprende.
CN119285556B (zh) * 2024-12-13 2025-02-28 四川健林药业有限责任公司 莱博雷生中间体的合成纯化方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008069997A1 (en) 2006-12-01 2008-06-12 Merck & Co., Inc. Substituted diazepan compounds as orexin receptor antagonists
WO2009047723A2 (en) 2007-10-10 2009-04-16 Actelion Pharmaceuticals Ltd Tetrahydroquinoline derivatives for treating post-traumatic stress disorders
WO2012039371A1 (ja) 2010-09-22 2012-03-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 シクロプロパン化合物
JP2015509939A (ja) 2012-02-17 2015-04-02 エーザイ・アール・アンド・ディー・マネジメント株式会社 オレキシン−２受容体アンタゴニストの合成において有用な方法および化合物

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Publication number Priority date Publication date Assignee Title
US6020157A (en) * 1997-04-30 2000-02-01 Smithkline Beecham Corporation Polynucleotides encoding HFGAN72X receptor
US6166193A (en) * 1997-07-25 2000-12-26 Board Of Regents, University Of Texas System Polynucleotides encoding MY1 receptor
RU2703297C2 (ru) * 2014-10-23 2019-10-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Композиции и способы для лечения бессонницы
CN104592184B (zh) 2014-12-15 2017-09-29 云南省药物研究所 灯盏乙素苷元晶型及其制备方法
CN115710250A (zh) * 2017-08-01 2023-02-24 博健制药有限责任公司 一种食欲素受体拮抗剂的晶型及其制备方法和用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008069997A1 (en) 2006-12-01 2008-06-12 Merck & Co., Inc. Substituted diazepan compounds as orexin receptor antagonists
WO2009047723A2 (en) 2007-10-10 2009-04-16 Actelion Pharmaceuticals Ltd Tetrahydroquinoline derivatives for treating post-traumatic stress disorders
WO2012039371A1 (ja) 2010-09-22 2012-03-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 シクロプロパン化合物
JP2015509939A (ja) 2012-02-17 2015-04-02 エーザイ・アール・アンド・ディー・マネジメント株式会社 オレキシン−２受容体アンタゴニストの合成において有用な方法および化合物

Non-Patent Citations (4)

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Title
YOSHIDA, Yu et al.，Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide(E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist，Journal of Medicinal Chemistry，2015年，Vol.58，pp.4648-4664，DOI: 10.1021/acs.jmedchem.5b00217
平山令明，有機化合物結晶作製ハンドブック，2008年，pp. 17-23,37-40,45-51,57-65
松岡 正邦，結晶多形の基礎と応用，普及版 第１刷，株式会社 シーエムシー出版，2010年10月22日，第１０５～１１７頁、第１８１～１９１頁
芦澤 一英、他，医薬品の多形現象と晶析の科学，丸善プラネット株式会社，2002年09月20日，第３０５－３１７頁

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WO2019024845A1 (zh) 2019-02-07
US10759779B2 (en) 2020-09-01
CN110799501A (zh) 2020-02-14
CN110799501B (zh) 2022-11-22
JP2020528913A (ja) 2020-10-01
CN115710250A (zh) 2023-02-24
US20200190060A1 (en) 2020-06-18
JP2023027066A (ja) 2023-03-01

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