JP7454512B2 - 優先的カンナビノイド２アゴニストとしてのピリジン及びピラジン誘導体 - Google Patents

優先的カンナビノイド２アゴニストとしてのピリジン及びピラジン誘導体 Download PDF

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JP7454512B2
JP7454512B2 JP2020572638A JP2020572638A JP7454512B2 JP 7454512 B2 JP7454512 B2 JP 7454512B2 JP 2020572638 A JP2020572638 A JP 2020572638A JP 2020572638 A JP2020572638 A JP 2020572638A JP 7454512 B2 JP7454512 B2 JP 7454512B2
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methoxy
ethyl
pyridine
methoxyazetidin
cyclopropyl
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JP2021528455A5 (OSRAM
JP2021528455A (ja
Inventor
アメタミー，シモン・エム
アッツ，ケネス
ゴッビ，ルカ
グレター，ウーヴェ
グーバ，ヴォルフガング
クレッツ，ユリアン
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F Hoffmann La Roche AG
Eidgenoessische Technische Hochschule Zurich ETHZ
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F Hoffmann La Roche AG
Eidgenoessische Technische Hochschule Zurich ETHZ
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
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    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K9/08—Solutions
    • 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
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • 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
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    • 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
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
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    • A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
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    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
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    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
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    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
JP2020572638A 2018-06-27 2019-06-25 優先的カンナビノイド２アゴニストとしてのピリジン及びピラジン誘導体 Active JP7454512B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18180114 2018-06-27
EP18180114.3 2018-06-27
PCT/EP2019/066733 WO2020002270A1 (en) 2018-06-27 2019-06-25 Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists

Publications (3)

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JP2021528455A JP2021528455A (ja) 2021-10-21
JP2021528455A5 JP2021528455A5 (OSRAM) 2022-06-30
JP7454512B2 true JP7454512B2 (ja) 2024-03-22

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JP2020572638A Active JP7454512B2 (ja) 2018-06-27 2019-06-25 優先的カンナビノイド２アゴニストとしてのピリジン及びピラジン誘導体

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US (1) US11655243B2 (OSRAM)
EP (1) EP3814337B1 (OSRAM)
JP (1) JP7454512B2 (OSRAM)
CN (1) CN112074513B (OSRAM)
WO (1) WO2020002270A1 (OSRAM)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110753690B (zh) 2017-06-20 2023-12-05 豪夫迈·罗氏有限公司 吡啶衍生物
EP3813888B1 (en) * 2018-06-27 2025-11-26 F. Hoffmann-La Roche AG Radiolabeled cannabinoid receptor 2 ligand
MA53002A (fr) 2018-06-27 2021-05-05 Eth Zuerich Nouveaux composés de pyridine et de pyrazine en tant qu'inhibiteurs du récepteur cannabinoïde 2
WO2020002280A1 (en) 2018-06-27 2020-01-02 F. Hoffmann-La Roche Ag Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2

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JP2010505788A (ja) 2006-10-04 2010-02-25 エフ．ホフマン−ラ ロシュ アーゲー Ｃｂ２受容体調節因子としてのピラジン−２−カルボキサミド誘導体
JP2014516071A (ja) 2011-06-10 2014-07-07 エフ．ホフマン−ラ ロシュ アーゲー Ｃｂ２アゴニストとして有用なピリジン−２−アミド
JP2014534210A (ja) 2011-10-28 2014-12-18 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規なピラジン誘導体
JP2016516737A (ja) 2013-03-26 2016-06-09 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規ピリジン誘導体
JP2017509688A (ja) 2014-04-04 2017-04-06 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ カンナビノイド受容体アゴニストとしての５，６−二置換ピリジン−２−カルボキサミド
JP2022501311A (ja) 2018-06-27 2022-01-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 放射性標識カンナビノイド受容体２リガンド

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CA2844834A1 (en) * 2011-09-12 2013-03-21 F.Hoffmann-La Roche Ag 5-cycloalkyl- or 5-heterocyclyl-nicotinamides
TW201326139A (zh) * 2011-10-28 2013-07-01 Hoffmann La Roche 新穎吡□衍生物
PL2928882T3 (pl) 2012-12-07 2017-07-31 F.Hoffmann-La Roche Ag Pochodne pirazyny jako agoniści receptora cb2
JP6426619B2 (ja) 2012-12-07 2018-11-21 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｃｂ２アゴニストとして有用なピリジン−２−アミド
EP3357918A1 (en) * 2012-12-07 2018-08-08 F. Hoffmann-La Roche AG Novel pyridine derivatives
HRP20171459T1 (hr) 2012-12-07 2017-11-03 F. Hoffmann - La Roche Ag Piridin-2-amidi korisni kao agonisti cb2
EP3126359A1 (en) 2014-04-04 2017-02-08 F. Hoffmann-La Roche AG Pyridine-2-amides useful as cb2 agonists
BR112018011562B1 (pt) 2015-12-09 2023-05-02 F. Hoffmann-La Roche Ag Novos derivados de fenil
CN110753690B (zh) 2017-06-20 2023-12-05 豪夫迈·罗氏有限公司 吡啶衍生物
MA53002A (fr) 2018-06-27 2021-05-05 Eth Zuerich Nouveaux composés de pyridine et de pyrazine en tant qu'inhibiteurs du récepteur cannabinoïde 2
WO2020002280A1 (en) 2018-06-27 2020-01-02 F. Hoffmann-La Roche Ag Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
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JP2010505788A (ja) 2006-10-04 2010-02-25 エフ．ホフマン−ラ ロシュ アーゲー Ｃｂ２受容体調節因子としてのピラジン−２−カルボキサミド誘導体
JP2014516071A (ja) 2011-06-10 2014-07-07 エフ．ホフマン−ラ ロシュ アーゲー Ｃｂ２アゴニストとして有用なピリジン−２−アミド
JP2014534210A (ja) 2011-10-28 2014-12-18 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規なピラジン誘導体
JP2016516737A (ja) 2013-03-26 2016-06-09 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規ピリジン誘導体
JP2017509688A (ja) 2014-04-04 2017-04-06 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ カンナビノイド受容体アゴニストとしての５，６−二置換ピリジン−２−カルボキサミド
JP2022501311A (ja) 2018-06-27 2022-01-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 放射性標識カンナビノイド受容体２リガンド

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Publication number Publication date
WO2020002270A1 (en) 2020-01-02
US20210115027A1 (en) 2021-04-22
CN112074513B (zh) 2024-06-14
EP3814337A1 (en) 2021-05-05
US11655243B2 (en) 2023-05-23
CN112074513A (zh) 2020-12-11
JP2021528455A (ja) 2021-10-21
EP3814337B1 (en) 2025-05-14
EP3814337C0 (en) 2025-05-14

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