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MA37941A1 - Dérivés d'aryléthynyle - Google Patents

Dérivés d'aryléthynyle

Info

Publication number
MA37941A1
MA37941A1 MA37941A MA37941A MA37941A1 MA 37941 A1 MA37941 A1 MA 37941A1 MA 37941 A MA37941 A MA 37941A MA 37941 A MA37941 A MA 37941A MA 37941 A1 MA37941 A1 MA 37941A1
Authority
MA
Morocco
Prior art keywords
formula
fluorophenyl
compounds
derivatives
enantiome
Prior art date
Application number
MA37941A
Other languages
English (en)
Other versions
MA37941B1 (fr
Inventor
Heinz Stadler
Eric Vieira
Georg Jaeschke
Lothar Lindemann
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MA37941A1 publication Critical patent/MA37941A1/fr
Publication of MA37941B1 publication Critical patent/MA37941B1/fr

Links

Classifications

    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Otolaryngology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Epidemiology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La présente invention concerne des dérivés d'éthynyle de formule (i) dans laquelle • r est phényle, 3 -fluorophényle, 4-fluorophényle ou 2,5-di-fluorophényle, • ou un sel d'addition d'acide pharmaceutiquement acceptable, sous forme d'énantiome pur ayant la configuration absolue telle que représentée dans la formule (i). Il a été découvert de manière inattendue que les composés de formule générale i sont des modulateurs allostériques du récepteur de glutamate métabotropique de sous-type 5 (mglur5) qui sont utiles pour le traitement de la schizophrénie, des troubles cognitifs, du syndrome de l'x fragile ou de l'autisme et qui présentent des propriétés biochimiques, physico-chimiques et pharmacocinétiques avantageuses par rapport aux composés de l'art antérieur.
MA37941A 2012-09-27 2015-03-20 Dérivés d'aryléthynyle MA37941B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12186265 2012-09-27
PCT/EP2013/069674 WO2014056710A1 (fr) 2012-09-27 2013-09-23 Dérivés d'aryléthynyle

Publications (2)

Publication Number Publication Date
MA37941A1 true MA37941A1 (fr) 2016-04-29
MA37941B1 MA37941B1 (fr) 2016-11-30

Family

ID=47044829

Family Applications (1)

Application Number Title Priority Date Filing Date
MA37941A MA37941B1 (fr) 2012-09-27 2015-03-20 Dérivés d'aryléthynyle

Country Status (30)

Country Link
US (1) US9221802B2 (fr)
EP (1) EP2900659B1 (fr)
JP (1) JP6027251B2 (fr)
KR (1) KR101737245B1 (fr)
CN (1) CN104684911B (fr)
AR (1) AR092673A1 (fr)
AU (1) AU2013329739B2 (fr)
BR (1) BR112015006218A2 (fr)
CA (1) CA2885382A1 (fr)
CL (1) CL2015000707A1 (fr)
CR (1) CR20150139A (fr)
DK (1) DK2900659T3 (fr)
EA (1) EA025482B1 (fr)
ES (1) ES2594031T3 (fr)
HK (1) HK1207376A1 (fr)
HU (1) HUE029636T2 (fr)
IL (1) IL237596A (fr)
MA (1) MA37941B1 (fr)
MX (1) MX366136B (fr)
MY (1) MY171743A (fr)
NZ (1) NZ706283A (fr)
PE (1) PE20150708A1 (fr)
PH (1) PH12015500538A1 (fr)
PL (1) PL2900659T3 (fr)
SG (1) SG11201502449RA (fr)
SI (1) SI2900659T1 (fr)
TW (1) TWI476194B (fr)
UA (1) UA113779C2 (fr)
WO (1) WO2014056710A1 (fr)
ZA (1) ZA201501678B (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA113223C2 (xx) * 2012-08-13 2016-12-26 Арилетинілпіримідини
CN104603110B (zh) * 2012-10-18 2016-08-31 霍夫曼-拉罗奇有限公司 作为mGluR5受体活性的调节剂的乙炔基衍生物
SI3303316T1 (sl) 2015-06-03 2020-07-31 F. Hoffmann-La Roche Ag Derivati etinila

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
EP1809620B1 (fr) 2004-11-04 2010-12-29 Addex Pharma SA Nouveaux derives de tetrazole utilises comme modulateurs allosteriques positifs des recepteurs de glutamate metabotropiques
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
TW200811157A (en) * 2006-05-05 2008-03-01 Astrazeneca Ab mGluR5 modulators I
AU2008259776A1 (en) 2007-06-03 2008-12-11 Vanderbilt University Benzamide mGluR5 positive allosteric modulators and methods of making and using same
US8034806B2 (en) * 2007-11-02 2011-10-11 Vanderbilt University Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
TW201116532A (en) * 2009-08-05 2011-05-16 Merz Pharma Gmbh & Co Kgaa Metabotropic glutamate receptor modulators
US8586581B2 (en) * 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives

Also Published As

Publication number Publication date
CA2885382A1 (fr) 2014-04-17
WO2014056710A1 (fr) 2014-04-17
DK2900659T3 (en) 2016-10-03
AR092673A1 (es) 2015-04-29
MX2015003560A (es) 2015-06-22
SG11201502449RA (en) 2015-05-28
PL2900659T3 (pl) 2017-02-28
IL237596A0 (en) 2015-04-30
AU2013329739A1 (en) 2015-03-19
TWI476194B (zh) 2015-03-11
EP2900659B1 (fr) 2016-08-24
ZA201501678B (en) 2016-01-27
CN104684911B (zh) 2017-05-10
PH12015500538B1 (en) 2015-05-04
AU2013329739B2 (en) 2017-04-20
EP2900659A1 (fr) 2015-08-05
US20150197510A1 (en) 2015-07-16
SI2900659T1 (sl) 2016-12-30
HK1207376A1 (en) 2016-01-29
CL2015000707A1 (es) 2015-08-07
NZ706283A (en) 2018-07-27
US9221802B2 (en) 2015-12-29
ES2594031T3 (es) 2016-12-15
KR101737245B1 (ko) 2017-05-17
KR20150058477A (ko) 2015-05-28
BR112015006218A2 (pt) 2017-07-04
PH12015500538A1 (en) 2015-05-04
JP2015534556A (ja) 2015-12-03
MY171743A (en) 2019-10-27
HUE029636T2 (en) 2017-03-28
MX366136B (es) 2019-06-28
TW201418248A (zh) 2014-05-16
EA025482B1 (ru) 2016-12-30
UA113779C2 (xx) 2017-03-10
IL237596A (en) 2017-02-28
CN104684911A (zh) 2015-06-03
EA201590557A1 (ru) 2015-07-30
MA37941B1 (fr) 2016-11-30
CR20150139A (es) 2015-04-30
PE20150708A1 (es) 2015-05-15
JP6027251B2 (ja) 2016-11-16

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