JP2024505967A - （４－メチル－２－［１，２，３］トリアゾール－２－イル－フェニル）－［（ｒ）－３－（３－［１，２，３］トリアゾール－２－イル－ベンジル）－モルホリン－４－イル］－メタノンの結晶形 - Google Patents

（４－メチル－２－［１，２，３］トリアゾール－２－イル－フェニル）－［（ｒ）－３－（３－［１，２，３］トリアゾール－２－イル－ベンジル）－モルホリン－４－イル］－メタノンの結晶形 Download PDF

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JP2024505967A
JP2024505967A JP2023546457A JP2023546457A JP2024505967A JP 2024505967 A JP2024505967 A JP 2024505967A JP 2023546457 A JP2023546457 A JP 2023546457A JP 2023546457 A JP2023546457 A JP 2023546457A JP 2024505967 A JP2024505967 A JP 2024505967A
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Prior art keywords
disorders
crystalline form
eating
disorder
triazol
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JP2023546457A
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JP2024505967A5 (https=
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フォン ラウマー マルクス
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Idorsia Pharmaceuticals Ltd
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Idorsia Pharmaceuticals Ltd
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    • 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
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2023546457A 2021-02-02 2022-01-28 （４－メチル－２－［１，２，３］トリアゾール－２－イル－フェニル）－［（ｒ）－３－（３－［１，２，３］トリアゾール－２－イル－ベンジル）－モルホリン－４－イル］－メタノンの結晶形 Pending JP2024505967A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EPPCT/EP2021/052373 2021-02-02
EP2021052373 2021-02-02
PCT/EP2022/051992 WO2022167330A1 (en) 2021-02-02 2022-01-28 A crystalline form of (4-methyl-2-[1,2,3]triazol-2-yl-phenyl)-[(r)-3-(3-[1,2,3]triazol-2-yl-benzyl)-morpholin-4-yl]-methanone

Publications (2)

Publication Number Publication Date
JP2024505967A true JP2024505967A (ja) 2024-02-08
JP2024505967A5 JP2024505967A5 (https=) 2025-02-04

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JP2023546457A Pending JP2024505967A (ja) 2021-02-02 2022-01-28 （４－メチル－２－［１，２，３］トリアゾール－２－イル－フェニル）－［（ｒ）－３－（３－［１，２，３］トリアゾール－２－イル－ベンジル）－モルホリン－４－イル］－メタノンの結晶形

Country Status (8)

Country Link
US (1) US20240116913A1 (https=)
EP (1) EP4288432A1 (https=)
JP (1) JP2024505967A (https=)
KR (1) KR20230142742A (https=)
CN (1) CN116724037A (https=)
CA (1) CA3206675A1 (https=)
TW (1) TW202241447A (https=)
WO (1) WO2022167330A1 (https=)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014532753A (ja) * 2011-11-08 2014-12-08 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ オレキシン受容体アンタゴニストとしての２−（１，２，３−トリアゾール−２−イル）ベンズアミド及び３−（１，２，３−トリアゾール−２−イル）ピコリンアミド誘導体
JP2019108366A (ja) * 2014-02-05 2019-07-04 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｃｇｒｐ活性化合物の錠剤製剤
JP2020511522A (ja) * 2016-12-15 2020-04-16 華領医薬技術（上海）有限公司Ｈｕａ Ｍｅｄｉｃｉｎｅ （Ｓｈａｎｇｈａｉ） Ｌｔｄ． グルコキナーゼ活性化剤の経口製剤およびその製造方法
JP2020529467A (ja) * 2018-02-02 2020-10-08 ノヴォ ノルディスク アー／エス Ｇｌｐ−１アゴニスト、ｎ−（８−（２−ヒドロキシベンゾイル）アミノ）カプリル酸の塩及び滑沢剤を含む固形組成物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014532753A (ja) * 2011-11-08 2014-12-08 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ オレキシン受容体アンタゴニストとしての２−（１，２，３−トリアゾール−２−イル）ベンズアミド及び３−（１，２，３−トリアゾール−２−イル）ピコリンアミド誘導体
JP2019108366A (ja) * 2014-02-05 2019-07-04 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｃｇｒｐ活性化合物の錠剤製剤
JP2020511522A (ja) * 2016-12-15 2020-04-16 華領医薬技術（上海）有限公司Ｈｕａ Ｍｅｄｉｃｉｎｅ （Ｓｈａｎｇｈａｉ） Ｌｔｄ． グルコキナーゼ活性化剤の経口製剤およびその製造方法
JP2020529467A (ja) * 2018-02-02 2020-10-08 ノヴォ ノルディスク アー／エス Ｇｌｐ−１アゴニスト、ｎ−（８−（２−ヒドロキシベンゾイル）アミノ）カプリル酸の塩及び滑沢剤を含む固形組成物

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
BYRN, S. ET AL.: "Pharmaceutical Solids: A Strategic Approach to Regulatory Considerations", PHARMACEUTICAL RESEARCH, vol. 12, no. 7, JPN6014008492, 1995, pages 945 - 954, ISSN: 0005765816 *
厚生省医薬安全局審査管理課長: "医薬品の残留溶媒ガイドラインについて", 医薬審, JPN6014031669, 1998, ISSN: 0005765815 *
平山令明, 有機化合物結晶作製ハンドブック, JPN6014035600, 2008, pages 17 - 23, ISSN: 0005765814 *
芦澤 一英: "塩・結晶形の最適化と結晶化技術", PHARM TECH JAPAN, vol. 18, no. 10, JPN6013060608, 2002, pages 81 - 96, ISSN: 0005769477 *
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005765813 *

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Publication number Publication date
KR20230142742A (ko) 2023-10-11
WO2022167330A1 (en) 2022-08-11
CN116724037A (zh) 2023-09-08
CA3206675A1 (en) 2022-08-11
TW202241447A (zh) 2022-11-01
EP4288432A1 (en) 2023-12-13
US20240116913A1 (en) 2024-04-11

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