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 (enExample
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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    • 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
    • A61K47/06—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
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    • 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
    • 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
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    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
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    • A—HUMAN NECESSITIES
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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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    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • C07—ORGANIC CHEMISTRY
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (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)

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

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

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

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201904943A (zh) 2017-06-20 2019-02-01 瑞士商赫孚孟拉羅股份公司 新穎吡啶衍生物
CN112638430B (zh) * 2018-06-27 2023-05-16 豪夫迈·罗氏有限公司 放射性标记的大麻素受体2配体
CA3096777A1 (en) 2018-06-27 2020-02-02 F. Hoffmann-La Roche Ag Novel pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
JP7478672B2 (ja) 2018-06-27 2024-05-07 エフ． ホフマン－ラ ロシュ アーゲー カンナビノイド受容体２の阻害剤としての新規なアゼチジン置換ピリジン及びピラジン化合物

Citations (6)

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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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TW201904943A (zh) 2017-06-20 2019-02-01 瑞士商赫孚孟拉羅股份公司 新穎吡啶衍生物
JP7478672B2 (ja) 2018-06-27 2024-05-07 エフ． ホフマン－ラ ロシュ アーゲー カンナビノイド受容体２の阻害剤としての新規なアゼチジン置換ピリジン及びピラジン化合物
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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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Journal of Medicinal Chemistry ，2015年，Vol. 58, No. 10，p. 4266-4277

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

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