JO3509B1 - معدلات p2x7 - Google Patents

معدلات p2x7

Info

Publication number
JO3509B1
JO3509B1 JOP/2014/0096A JOP20140096A JO3509B1 JO 3509 B1 JO3509 B1 JO 3509B1 JO P20140096 A JOP20140096 A JO P20140096A JO 3509 B1 JO3509 B1 JO 3509B1
Authority
JO
Jordan
Prior art keywords
pyridinyl
phenyl
formula
pyradizinyl
thiophenyl
Prior art date
Application number
JOP/2014/0096A
Other languages
English (en)
Inventor
A Rudolph Dale
A Letavic Michael
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Application granted granted Critical
Publication of JO3509B1 publication Critical patent/JO3509B1/ar

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/18Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

يوجه هذا الاختراع بصفة عامة إلى مركب بالصيغة (I)، الصيغة (I) حيث: n هو عدد صحيح من 0-1؛ X يمثل الميثيلين إذا كان n يساوي 0، أو X يمثل الميثيلين أو الأكسيجين إذا كان n يساوي 1؛ R1 هو الفينيل أو البيريدينيل، حيث يستبدل الفينيل أو البيريدينيل اختياريًا بهالوجين أو ألكيل؛ و R2 هو الفينيل أو البيريدينيل أو البيرازينيل أو البيريميدينيل أو البيروليل أو البيرازوليل أو الثيازوليل أو الثيوفينيل، حيث يستبدل الفينيل أو البيريدينيل أو البيرازينيل أو البيريميدينيل أو البيروليل أو البيرازوليل أو الثيازوليل أو الثيوفينيل اختياريًا بهالوجين أو ألكيل أو هيدروكسي أو ألكوكسي. كما يتعلق الاختراع أيضاً بتركيبات دوائية تتألف من مركبات الصيغة (I). كما تقع أيضًا طرق تحضير مركبات الصيغة (I) واستخدامها ضمن نطاق الاختراع.
JOP/2014/0096A 2013-03-14 2014-03-12 معدلات p2x7 JO3509B1 (ar)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361785558P 2013-03-14 2013-03-14

Publications (1)

Publication Number Publication Date
JO3509B1 true JO3509B1 (ar) 2020-07-05

Family

ID=50631041

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2014/0096A JO3509B1 (ar) 2013-03-14 2014-03-12 معدلات p2x7

Country Status (9)

Country Link
US (3) US9102686B2 (ar)
EP (2) EP2970287B1 (ar)
JP (1) JP6294954B2 (ar)
AR (1) AR095421A1 (ar)
ES (2) ES2652648T3 (ar)
JO (1) JO3509B1 (ar)
TW (1) TWI627174B (ar)
UY (1) UY35447A (ar)
WO (1) WO2014152621A1 (ar)

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Also Published As

Publication number Publication date
JP2016513702A (ja) 2016-05-16
ES2776654T3 (es) 2020-07-31
TWI627174B (zh) 2018-06-21
HK1218649A1 (en) 2017-03-03
US9540388B2 (en) 2017-01-10
EP2970287B1 (en) 2017-11-01
US10053462B2 (en) 2018-08-21
US20170088550A1 (en) 2017-03-30
UY35447A (es) 2014-09-30
US9102686B2 (en) 2015-08-11
AR095421A1 (es) 2015-10-14
US20140275056A1 (en) 2014-09-18
HK1254111A1 (en) 2019-07-12
JP6294954B2 (ja) 2018-03-14
EP2970287A1 (en) 2016-01-20
EP3309161B1 (en) 2019-12-18
ES2652648T3 (es) 2018-02-05
US20160039836A1 (en) 2016-02-11
EP3309161A1 (en) 2018-04-18
WO2014152621A1 (en) 2014-09-25
TW201522339A (zh) 2015-06-16

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