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 PDFInfo
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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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- 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
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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
- C07D401/04—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
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- 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
- A61K47/06—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
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- 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
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- 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
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2813—Inorganic compounds
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- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- 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)
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—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
- A61K9/48—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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (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)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| 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 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021528455A JP2021528455A (ja) | 2021-10-21 |
| JP2021528455A5 JP2021528455A5 (https=) | 2022-06-30 |
| JPWO2020002270A5 JPWO2020002270A5 (https=) | 2022-06-30 |
| JP7454512B2 true JP7454512B2 (ja) | 2024-03-22 |
Family
ID=62814859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US11655243B2 (https=) |
| EP (1) | EP3814337B1 (https=) |
| JP (1) | JP7454512B2 (https=) |
| CN (1) | CN112074513B (https=) |
| WO (1) | WO2020002270A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR112199A1 (es) | 2017-06-20 | 2019-10-02 | Hoffmann La Roche | Derivados de piridina como agonistas inversos del receptor cannabinoide 2 |
| PE20210368A1 (es) | 2018-06-27 | 2021-02-26 | Eth Zuerich | Nuevos compuestos de piridina y pirazina como inhibidores del receptor cannabinoide 2 |
| JP7456948B2 (ja) | 2018-06-27 | 2024-03-27 | エフ. ホフマン-ラ ロシュ アーゲー | 放射性標識カンナビノイド受容体2リガンド |
| CN112119068A (zh) | 2018-06-27 | 2020-12-22 | 豪夫迈·罗氏有限公司 | 作为大麻素受体2的抑制剂的新型氮杂环丁烷-取代的吡啶和吡嗪化合物 |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200808769A (en) * | 2006-04-18 | 2008-02-16 | Astrazeneca Ab | Therapeutic compounds |
| WO2009106561A1 (en) * | 2008-02-27 | 2009-09-03 | Biovitrum Ab (Publ) | Pyrazine compounds for treating gpr119 related disorders |
| MX2014001862A (es) * | 2011-09-12 | 2014-05-30 | Hoffmann La Roche | 5-cicloalquil-o 5-heterociclil-nicotinamidas. |
| TW201326139A (zh) * | 2011-10-28 | 2013-07-01 | Hoffmann La Roche | 新穎吡□衍生物 |
| CN104837818B (zh) | 2012-12-07 | 2017-07-14 | 霍夫曼-拉罗奇有限公司 | 可用作cb2激动剂的吡啶‑2‑酰胺 |
| AU2013354115B2 (en) | 2012-12-07 | 2017-10-05 | F. Hoffmann-La Roche Ag | Novel pyrazine derivatives as CB2 receptor agonists |
| SG10201800170YA (en) | 2012-12-07 | 2018-02-27 | Hoffmann La Roche | Novel pyridine derivatives |
| PL2928868T3 (pl) * | 2012-12-07 | 2017-12-29 | F.Hoffmann-La Roche Ag | Pirydyno-2-amidy użyteczne jako agoniści cb2 |
| WO2015150440A1 (en) * | 2014-04-04 | 2015-10-08 | F. Hoffmann-La Roche Ag | Pyridine-2-amides useful as cb2 agonists |
| EP3386951B1 (en) | 2015-12-09 | 2020-02-26 | H. Hoffnabb-La Roche Ag | Phenyl derivatives as cannabinoid receptor 2 agonists |
| AR112199A1 (es) | 2017-06-20 | 2019-10-02 | Hoffmann La Roche | Derivados de piridina como agonistas inversos del receptor cannabinoide 2 |
| PE20210368A1 (es) | 2018-06-27 | 2021-02-26 | Eth Zuerich | Nuevos compuestos de piridina y pirazina como inhibidores del receptor cannabinoide 2 |
| CN112119068A (zh) | 2018-06-27 | 2020-12-22 | 豪夫迈·罗氏有限公司 | 作为大麻素受体2的抑制剂的新型氮杂环丁烷-取代的吡啶和吡嗪化合物 |
| TWI687701B (zh) | 2018-12-05 | 2020-03-11 | 宏碁股份有限公司 | 判斷電量狀態的方法及其電子裝置 |
-
2019
- 2019-06-25 EP EP19739206.1A patent/EP3814337B1/en active Active
- 2019-06-25 JP JP2020572638A patent/JP7454512B2/ja active Active
- 2019-06-25 CN CN201980029322.XA patent/CN112074513B/zh active Active
- 2019-06-25 WO PCT/EP2019/066733 patent/WO2020002270A1/en not_active Ceased
-
2020
- 2020-12-17 US US17/125,647 patent/US11655243B2/en active Active
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Non-Patent Citations (1)
| Title |
|---|
| Journal of Medicinal Chemistry ,2015年,Vol. 58, No. 10,p. 4266-4277 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3814337C0 (en) | 2025-05-14 |
| CN112074513B (zh) | 2024-06-14 |
| WO2020002270A1 (en) | 2020-01-02 |
| US20210115027A1 (en) | 2021-04-22 |
| CN112074513A (zh) | 2020-12-11 |
| EP3814337A1 (en) | 2021-05-05 |
| EP3814337B1 (en) | 2025-05-14 |
| JP2021528455A (ja) | 2021-10-21 |
| US11655243B2 (en) | 2023-05-23 |
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