CN104837830B - 作为cb2受体激动剂的吡嗪衍生物 - Google Patents

作为cb2受体激动剂的吡嗪衍生物 Download PDF

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Publication number
CN104837830B
CN104837830B CN201380063228.9A CN201380063228A CN104837830B CN 104837830 B CN104837830 B CN 104837830B CN 201380063228 A CN201380063228 A CN 201380063228A CN 104837830 B CN104837830 B CN 104837830B
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cyclopropylmethoxy
difluoro
pyrazine
azetidin
carboxylic acid
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Expired - Fee Related
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CN201380063228.9A
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Chinese (zh)
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CN104837830A (zh
Inventor
巴莱蒂·德瓦苏禄
尤伟·格雷瑟
马蒂亚斯·内特科文
斯蒂芬·勒韦尔
马克·罗杰斯-埃文斯
坦贾·舒尔兹-加施
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • 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
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
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  • Transplantation (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201380063228.9A 2012-12-07 2013-12-04 作为cb2受体激动剂的吡嗪衍生物 Expired - Fee Related CN104837830B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12196024.9 2012-12-07
EP12196024 2012-12-07
PCT/EP2013/075444 WO2014086807A1 (en) 2012-12-07 2013-12-04 Novel pyrazine derivatives as cb2 receptor agonists

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CN104837830A CN104837830A (zh) 2015-08-12
CN104837830B true CN104837830B (zh) 2018-07-20

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CN201380063228.9A Expired - Fee Related CN104837830B (zh) 2012-12-07 2013-12-04 作为cb2受体激动剂的吡嗪衍生物

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US (1) US9512141B2 (enExample)
EP (1) EP2928882B1 (enExample)
JP (1) JP6322646B2 (enExample)
KR (1) KR20150092156A (enExample)
CN (1) CN104837830B (enExample)
AR (1) AR093804A1 (enExample)
AU (1) AU2013354115B2 (enExample)
BR (1) BR112015009603A2 (enExample)
CA (1) CA2885418A1 (enExample)
CL (1) CL2015001318A1 (enExample)
CR (1) CR20150210A (enExample)
CY (1) CY1118808T1 (enExample)
DK (1) DK2928882T3 (enExample)
EA (1) EA025840B1 (enExample)
ES (1) ES2621958T3 (enExample)
HR (1) HRP20170572T1 (enExample)
HU (1) HUE030836T2 (enExample)
IL (1) IL237982A (enExample)
IN (1) IN2015DN03145A (enExample)
LT (1) LT2928882T (enExample)
MA (1) MA38217B1 (enExample)
MX (1) MX2015006036A (enExample)
PE (1) PE20151060A1 (enExample)
PH (1) PH12015501072A1 (enExample)
PL (1) PL2928882T3 (enExample)
PT (1) PT2928882T (enExample)
RS (1) RS55951B1 (enExample)
SG (1) SG11201504011UA (enExample)
SI (1) SI2928882T1 (enExample)
TW (1) TW201427960A (enExample)
UA (1) UA116894C2 (enExample)
WO (1) WO2014086807A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105143220B (zh) 2013-03-07 2018-06-22 豪夫迈·罗氏有限公司 吡唑衍生物
PE20151559A1 (es) 2013-03-26 2015-11-05 Hoffmann La Roche Nuevos derivados de piridina
HRP20181141T1 (hr) 2013-05-02 2018-09-21 F. Hoffmann - La Roche Ag Derivati purina kao agonisti cb2 receptora
BR112015027394A8 (pt) 2013-05-02 2018-01-30 Hoffmann La Roche derivados de pirrolo[2,3-d]pirimidina como agonistas de receptor cb2
AU2014317229B2 (en) 2013-09-06 2018-11-08 F. Hoffmann-La Roche Ag Novel triazolo(4,5-d)pyrimidine derivatives
AR099933A1 (es) * 2014-04-04 2016-08-31 Hoffmann La Roche Derivados heterocíclicos de piridina agonistas de cb2
WO2017097732A1 (en) * 2015-12-09 2017-06-15 F. Hoffmann-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
EP3814328B1 (en) 2018-06-27 2026-03-11 F. Hoffmann-La Roche AG Novel azetidine-substituted pyridine compounds as inhibitors of cannabinoid receptor 2
EP3814337B1 (en) 2018-06-27 2025-05-14 F. Hoffmann-La Roche AG Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists
MX2020012760A (es) 2018-06-27 2021-03-25 Hoffmann La Roche Nuevos compuestos de piridina y pirazina como inhibidores del receptor cannabinoide 2.
EP3995155A1 (en) 2018-06-27 2022-05-11 F. Hoffmann-La Roche AG Radiolabeled cannabinoid receptor 2 ligand
WO2022128050A1 (en) 2020-12-14 2022-06-23 Symrise Ag Medicament for fighting inflammation and pain

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007147746A1 (en) * 2006-06-19 2007-12-27 F. Hoffmann-La Roche Ag 2-pyrazinecarboxamide derivatives
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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012031817A1 (en) 2010-09-09 2012-03-15 F. Hoffmann-La Roche Ag Determination of abca1 protein levels in cells
US9321727B2 (en) 2011-06-10 2016-04-26 Hoffmann-La Roche Inc. Pyridine derivatives as agonists of the CB2 receptor
US9403808B2 (en) * 2011-10-28 2016-08-02 Hoffmann-La Roche Inc. Pyrazine derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007147746A1 (en) * 2006-06-19 2007-12-27 F. Hoffmann-La Roche Ag 2-pyrazinecarboxamide derivatives
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

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CR20150210A (es) 2015-05-29
DK2928882T3 (en) 2017-02-20
CN104837830A (zh) 2015-08-12
PE20151060A1 (es) 2015-07-25
MA38217B1 (fr) 2017-11-30
HUE030836T2 (en) 2017-06-28
SG11201504011UA (en) 2015-07-30
KR20150092156A (ko) 2015-08-12
MA38217A1 (fr) 2017-02-28
IN2015DN03145A (enExample) 2015-10-02
CY1118808T1 (el) 2018-01-10
EA025840B1 (ru) 2017-02-28
RS55951B1 (sr) 2017-09-29
WO2014086807A1 (en) 2014-06-12
HK1208030A1 (en) 2016-02-19
US20150299220A1 (en) 2015-10-22
CL2015001318A1 (es) 2015-10-02
PL2928882T3 (pl) 2017-07-31
CA2885418A1 (en) 2014-06-12
IL237982A (en) 2017-06-29
JP6322646B2 (ja) 2018-05-09
US9512141B2 (en) 2016-12-06
PT2928882T (pt) 2017-03-16
LT2928882T (lt) 2017-03-27
PH12015501072B1 (en) 2015-08-03
ES2621958T3 (es) 2017-07-05
EP2928882A1 (en) 2015-10-14
EP2928882B1 (en) 2017-01-18
AU2013354115B2 (en) 2017-10-05
MX2015006036A (es) 2015-08-07
PH12015501072A1 (en) 2015-08-03
JP2016505557A (ja) 2016-02-25
AR093804A1 (es) 2015-06-24
AU2013354115A1 (en) 2015-04-09
UA116894C2 (uk) 2018-05-25
HRP20170572T1 (hr) 2017-06-16
EA201590827A1 (ru) 2015-09-30
SI2928882T1 (sl) 2017-05-31
BR112015009603A2 (pt) 2017-07-04
TW201427960A (zh) 2014-07-16

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