MX366136B - Derivados de ariletinilo. - Google Patents

Derivados de ariletinilo.

Info

Publication number
MX366136B
MX366136B MX2015003560A MX2015003560A MX366136B MX 366136 B MX366136 B MX 366136B MX 2015003560 A MX2015003560 A MX 2015003560A MX 2015003560 A MX2015003560 A MX 2015003560A MX 366136 B MX366136 B MX 366136B
Authority
MX
Mexico
Prior art keywords
fluorophenyl
formula
compounds
derivatives
sydrome
Prior art date
Application number
MX2015003560A
Other languages
English (en)
Other versions
MX2015003560A (es
Inventor
Stadler Heinz
Vieira Eric
Jaeschke George
Lindemann Lothar
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 MX2015003560A publication Critical patent/MX2015003560A/es
Publication of MX366136B publication Critical patent/MX366136B/es

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

Abstract

La presente invención se refiere a derivados de etinilo de la fórmula (I) en donde R1 es fenilo, 3-fluorfenilo, 4- fluorfenilo o 2,5-di-fluor-fenilo; o a una sal de adición de ácido farmacéuticamente aceptable, en forma enantioméricamente pura con la configuración absoluta representada en la fórmula (I). Ahora se ha encontrado de modo sorprendente que los compuestos de la fórmula general 1 son moduladores alostéricos del receptor de glutamato metabotrópico del subtipo 5 (mGluR5), que posee propiedades bioquímicas, físico-químicas y farmacodinámicas ventajosas con respecto a los compuestos del arte previo.
MX2015003560A 2012-09-27 2013-09-23 Derivados de ariletinilo. MX366136B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12186265 2012-09-27
PCT/EP2013/069674 WO2014056710A1 (en) 2012-09-27 2013-09-23 Arylethynyl derivatives

Publications (2)

Publication Number Publication Date
MX2015003560A MX2015003560A (es) 2015-06-22
MX366136B true MX366136B (es) 2019-06-28

Family

ID=47044829

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015003560A MX366136B (es) 2012-09-27 2013-09-23 Derivados de ariletinilo.

Country Status (30)

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

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
PE20150733A1 (es) * 2012-10-18 2015-05-17 Hoffmann La Roche Derivados de etinilo como moduladores de la actividad del receptor mglur5
CR20170536A (es) * 2015-06-03 2018-02-01 Hoffmann La Roche Derivados de etinilo

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 (en) 2004-11-04 2010-12-29 Addex Pharma SA Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
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
JP5622568B2 (ja) 2007-06-03 2014-11-12 バンダービルト ユニバーシティ ベンズアミドmGluR5の正のアロステリック調節因子ならびにその作製および使用方法
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
ES2594031T3 (es) 2016-12-15
DK2900659T3 (en) 2016-10-03
NZ706283A (en) 2018-07-27
MX2015003560A (es) 2015-06-22
AU2013329739A1 (en) 2015-03-19
MA37941A1 (fr) 2016-04-29
EA201590557A1 (ru) 2015-07-30
US20150197510A1 (en) 2015-07-16
PL2900659T3 (pl) 2017-02-28
US9221802B2 (en) 2015-12-29
IL237596A0 (en) 2015-04-30
PE20150708A1 (es) 2015-05-15
MA37941B1 (fr) 2016-11-30
CR20150139A (es) 2015-04-30
AR092673A1 (es) 2015-04-29
ZA201501678B (en) 2016-01-27
PH12015500538B1 (en) 2015-05-04
EP2900659A1 (en) 2015-08-05
KR101737245B1 (ko) 2017-05-17
AU2013329739B2 (en) 2017-04-20
BR112015006218A2 (pt) 2017-07-04
JP6027251B2 (ja) 2016-11-16
IL237596A (en) 2017-02-28
HUE029636T2 (en) 2017-03-28
MY171743A (en) 2019-10-27
SI2900659T1 (sl) 2016-12-30
WO2014056710A1 (en) 2014-04-17
PH12015500538A1 (en) 2015-05-04
CL2015000707A1 (es) 2015-08-07
CA2885382A1 (en) 2014-04-17
HK1207376A1 (en) 2016-01-29
EA025482B1 (ru) 2016-12-30
SG11201502449RA (en) 2015-05-28
CN104684911A (zh) 2015-06-03
TWI476194B (zh) 2015-03-11
TW201418248A (zh) 2014-05-16
EP2900659B1 (en) 2016-08-24
UA113779C2 (xx) 2017-03-10
KR20150058477A (ko) 2015-05-28
JP2015534556A (ja) 2015-12-03
CN104684911B (zh) 2017-05-10

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