CN112074513B - 作为优先大麻素2激动剂的吡啶和吡嗪衍生物 - Google Patents

作为优先大麻素2激动剂的吡啶和吡嗪衍生物 Download PDF

Info

Publication number
CN112074513B
CN112074513B CN201980029322.XA CN201980029322A CN112074513B CN 112074513 B CN112074513 B CN 112074513B CN 201980029322 A CN201980029322 A CN 201980029322A CN 112074513 B CN112074513 B CN 112074513B
Authority
CN
China
Prior art keywords
ethyl
methoxy
methoxyazetidin
cyclopropyl
pyridine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201980029322.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN112074513A (zh
Inventor
西蒙·M·艾梅塔美
肯尼斯·阿特兹
罗卡·戈比
尤伟·格雷瑟
沃尔夫冈·古帕
朱利安·克雷茨
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Eidgenoessische Technische Hochschule Zurich ETHZ
Original Assignee
F Hoffmann La Roche AG
Eidgenoessische Technische Hochschule Zurich ETHZ
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by F Hoffmann La Roche AG, Eidgenoessische Technische Hochschule Zurich ETHZ filed Critical F Hoffmann La Roche AG
Publication of CN112074513A publication Critical patent/CN112074513A/zh
Application granted granted Critical
Publication of CN112074513B publication Critical patent/CN112074513B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (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)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
CN201980029322.XA 2018-06-27 2019-06-25 作为优先大麻素2激动剂的吡啶和吡嗪衍生物 Active CN112074513B (zh)

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 (2)

Publication Number Publication Date
CN112074513A CN112074513A (zh) 2020-12-11
CN112074513B true CN112074513B (zh) 2024-06-14

Family

ID=62814859

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980029322.XA Active CN112074513B (zh) 2018-06-27 2019-06-25 作为优先大麻素2激动剂的吡啶和吡嗪衍生物

Country Status (5)

Country Link
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
CN110753690B (zh) 2017-06-20 2023-12-05 豪夫迈·罗氏有限公司 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
EP3814328A1 (en) 2018-06-27 2021-05-05 F. Hoffmann-La Roche AG Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
CR20200643A (es) 2018-06-27 2021-05-11 Eth Zuerich Nuev0s compuestos de piridina y pirazina com0 inhibidores del receptor connabinoide 2

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101522644A (zh) * 2006-10-04 2009-09-02 霍夫曼-拉罗奇有限公司 作为cb2受体调节剂的吡嗪-2-羧酰胺衍生物
CN103608332A (zh) * 2011-06-10 2014-02-26 霍夫曼-拉罗奇有限公司 可用作cb2激动剂的吡啶-2-酰胺类

Family Cites Families (18)

* Cited by examiner, † Cited by third party
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
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
US9403808B2 (en) * 2011-10-28 2016-08-02 Hoffmann-La Roche Inc. Pyrazine derivatives
MA38217B1 (fr) 2012-12-07 2017-11-30 Hoffmann La Roche Nouveaux dérivés de pyrazine comme agonistes des récepteurs cb2
PT2928868T (pt) 2012-12-07 2017-10-04 Hoffmann La Roche Piridina-2-amidas úteis como agonistas do cb2
KR20150092232A (ko) 2012-12-07 2015-08-12 에프. 호프만-라 로슈 아게 Cb2 작용제로 유용한 피리딘-2-아마이드
SG11201504416XA (en) * 2012-12-07 2015-07-30 Hoffmann La Roche Novel pyridine derivatives
DK2978755T3 (en) * 2013-03-26 2018-03-05 Hoffmann La Roche Hitherto unknown pyridine derivatives
PE20161370A1 (es) * 2014-04-04 2016-12-17 Hoffmann La Roche Nuevos derivados de piridina utiles como antagonistas de cb2
CA2944256A1 (en) * 2014-04-04 2015-10-08 F. Hoffmann-La Roche Ag 5,6-disubstituted pyridine-2-carboxamides as cannabinoid receptor agonists
CR20180298A (es) 2015-12-09 2018-07-18 Hoffmann La Roche Nuevos derivados de fenilo
CN110753690B (zh) 2017-06-20 2023-12-05 豪夫迈·罗氏有限公司 吡啶衍生物
EP3814328A1 (en) 2018-06-27 2021-05-05 F. Hoffmann-La Roche AG Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
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
CR20200643A (es) 2018-06-27 2021-05-11 Eth Zuerich Nuev0s compuestos de piridina y pirazina com0 inhibidores del receptor connabinoide 2
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101522644A (zh) * 2006-10-04 2009-09-02 霍夫曼-拉罗奇有限公司 作为cb2受体调节剂的吡嗪-2-羧酰胺衍生物
CN103608332A (zh) * 2011-06-10 2014-02-26 霍夫曼-拉罗奇有限公司 可用作cb2激动剂的吡啶-2-酰胺类

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Discovery of a High Affinity and Selective Pyridine Analog as a Potential Positron Emission Tomography Imaging Agent for Cannabinoid Type 2 Receptor;Roger Slavik et al.;《J. Med. Chem.》;第58卷;第4266−4277页 *

Also Published As

Publication number Publication date
EP3814337A1 (en) 2021-05-05
EP3814337B1 (en) 2025-05-14
US11655243B2 (en) 2023-05-23
JP2021528455A (ja) 2021-10-21
EP3814337C0 (en) 2025-05-14
WO2020002270A1 (en) 2020-01-02
CN112074513A (zh) 2020-12-11
US20210115027A1 (en) 2021-04-22
JP7454512B2 (ja) 2024-03-22

Similar Documents

Publication Publication Date Title
TWI848092B (zh) 囊腫纖維化跨膜傳導調節蛋白調節劑
CN112074513B (zh) 作为优先大麻素2激动剂的吡啶和吡嗪衍生物
EP2928881B1 (en) Novel pyridine derivatives
CN104837830B (zh) 作为cb2受体激动剂的吡嗪衍生物
JP7445610B2 (ja) 医療に有用な新規化合物
EP3386951B1 (en) Phenyl derivatives as cannabinoid receptor 2 agonists
FR2786185A1 (fr) 3-aminomethylpyrrolidines, compositions pharmaceutiques les contenant et procedes pour les preparer
CN107011272A (zh) 吡嗪衍生物
US12180196B2 (en) Azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
JPWO2020002270A5 (enExample)
HK40035575A (en) Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists
HK40035575B (zh) 作为优先大麻素2激动剂的吡啶和吡嗪衍生物
HK40035571A (en) Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
HK40085255A (en) Phenyl derivatives as cannabinoid receptor 2 agonists
TW201326139A (zh) 新穎吡□衍生物
HK1208030B (zh) 作为cb2受体激动剂的吡嗪衍生物

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40035575

Country of ref document: HK

SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant