HRP20170572T1 - Derivati pirazina kao agonisti receptora cb2 - Google Patents

Derivati pirazina kao agonisti receptora cb2 Download PDF

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Publication number
HRP20170572T1
HRP20170572T1 HRP20170572TT HRP20170572T HRP20170572T1 HR P20170572 T1 HRP20170572 T1 HR P20170572T1 HR P20170572T T HRP20170572T T HR P20170572TT HR P20170572 T HRP20170572 T HR P20170572T HR P20170572 T1 HRP20170572 T1 HR P20170572T1
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HR
Croatia
Prior art keywords
cyclopropylmethoxy
difluoro
azetidin
pyrazine
carbonyl
Prior art date
Application number
HRP20170572TT
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English (en)
Croatian (hr)
Inventor
Baledi DHURWASULU
Uwe Grether
Matthias Nettekoven
Stephan Roever
Mark Rogers-Evans
Tanja Schulz-Gasch
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F. Hoffmann - La Roche Ag
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Application filed by F. Hoffmann - La Roche Ag filed Critical F. Hoffmann - La Roche Ag
Publication of HRP20170572T1 publication Critical patent/HRP20170572T1/hr

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
HRP20170572TT 2012-12-07 2013-12-04 Derivati pirazina kao agonisti receptora cb2 HRP20170572T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12196024 2012-12-07
PCT/EP2013/075444 WO2014086807A1 (en) 2012-12-07 2013-12-04 Novel pyrazine derivatives as cb2 receptor agonists
EP13799545.2A EP2928882B1 (en) 2012-12-07 2013-12-04 Pyrazine derivatives as cb2 receptor agonists

Publications (1)

Publication Number Publication Date
HRP20170572T1 true HRP20170572T1 (hr) 2017-06-16

Family

ID=47290805

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20170572TT HRP20170572T1 (hr) 2012-12-07 2013-12-04 Derivati pirazina kao agonisti receptora cb2

Country Status (32)

Country Link
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
JP6514119B2 (ja) 2013-03-07 2019-05-15 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 新規ピラゾール誘導体
NO2978755T3 (enExample) 2013-03-26 2018-06-02
PE20151977A1 (es) 2013-05-02 2016-01-07 Hoffmann La Roche Nuevos derivados de purina
KR20160002857A (ko) 2013-05-02 2016-01-08 에프. 호프만-라 로슈 아게 CB2 수용체 작용제로서의 피롤로[2,3-d]피리미딘 유도체
KR20220140651A (ko) 2013-09-06 2022-10-18 에프. 호프만-라 로슈 아게 신규의 트라이아졸로[4,5-d]피리미딘 유도체
CA2943013A1 (en) * 2014-04-04 2015-10-08 F. Hoffmann-La Roche Ag Pyridine-2-amides useful as cb2 agonists
DK3386951T3 (en) * 2015-12-09 2020-04-27 Hoffmann La Roche Phenylderivater som cannabinoidreceptor-2-agonister
JP7300398B2 (ja) 2017-06-20 2023-06-29 エフ. ホフマン-ラ ロシュ アーゲー ピリジン誘導体
EP3995155A1 (en) 2018-06-27 2022-05-11 F. Hoffmann-La Roche AG Radiolabeled cannabinoid receptor 2 ligand
CN112074513B (zh) 2018-06-27 2024-06-14 豪夫迈·罗氏有限公司 作为优先大麻素2激动剂的吡啶和吡嗪衍生物
BR112020025013A2 (pt) * 2018-06-27 2021-03-23 F. Hoffmann-La Roche Ag novos compostos de piridina e pirazina como inibidores do receptor 2 de canabinoide
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
WO2022128050A1 (en) 2020-12-14 2022-06-23 Symrise Ag Medicament for fighting inflammation and pain

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7629346B2 (en) * 2006-06-19 2009-12-08 Hoffmann-La Roche Inc. Pyrazinecarboxamide derivatives as CB1 antagonists
EP2076499B1 (en) * 2006-10-04 2010-05-12 F.Hoffmann-La Roche Ag Pyrazine-2-carboxamide derivatives as cb2 receptor modulators
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

Also Published As

Publication number Publication date
PT2928882T (pt) 2017-03-16
CN104837830B (zh) 2018-07-20
AU2013354115B2 (en) 2017-10-05
HUE030836T2 (en) 2017-06-28
MA38217B1 (fr) 2017-11-30
CL2015001318A1 (es) 2015-10-02
MX2015006036A (es) 2015-08-07
PL2928882T3 (pl) 2017-07-31
CY1118808T1 (el) 2018-01-10
IN2015DN03145A (enExample) 2015-10-02
US9512141B2 (en) 2016-12-06
HK1208030A1 (en) 2016-02-19
PH12015501072B1 (en) 2015-08-03
ES2621958T3 (es) 2017-07-05
RS55951B1 (sr) 2017-09-29
IL237982A (en) 2017-06-29
JP6322646B2 (ja) 2018-05-09
SI2928882T1 (sl) 2017-05-31
TW201427960A (zh) 2014-07-16
MA38217A1 (fr) 2017-02-28
DK2928882T3 (en) 2017-02-20
BR112015009603A2 (pt) 2017-07-04
EP2928882B1 (en) 2017-01-18
SG11201504011UA (en) 2015-07-30
AU2013354115A1 (en) 2015-04-09
EA025840B1 (ru) 2017-02-28
CN104837830A (zh) 2015-08-12
JP2016505557A (ja) 2016-02-25
UA116894C2 (uk) 2018-05-25
US20150299220A1 (en) 2015-10-22
KR20150092156A (ko) 2015-08-12
LT2928882T (lt) 2017-03-27
EP2928882A1 (en) 2015-10-14
PE20151060A1 (es) 2015-07-25
WO2014086807A1 (en) 2014-06-12
CA2885418A1 (en) 2014-06-12
EA201590827A1 (ru) 2015-09-30
CR20150210A (es) 2015-05-29
PH12015501072A1 (en) 2015-08-03
AR093804A1 (es) 2015-06-24

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