EA201590557A1 - Производные арилэтинила - Google Patents

Производные арилэтинила

Info

Publication number
EA201590557A1
EA201590557A1 EA201590557A EA201590557A EA201590557A1 EA 201590557 A1 EA201590557 A1 EA 201590557A1 EA 201590557 A EA201590557 A EA 201590557A EA 201590557 A EA201590557 A EA 201590557A EA 201590557 A1 EA201590557 A1 EA 201590557A1
Authority
EA
Eurasian Patent Office
Prior art keywords
formula
fluorophenyl
derivatives
compounds
aryl ethynyl
Prior art date
Application number
EA201590557A
Other languages
English (en)
Other versions
EA025482B1 (ru
Inventor
Георг Ешке
Лотар Линдеманн
Хайнц Штадлер
Эрик Виейра
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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 Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of EA201590557A1 publication Critical patent/EA201590557A1/ru
Publication of EA025482B1 publication Critical patent/EA025482B1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (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)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (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

Настоящее изобретение относится к этинилпроизводным формулы Iгде Rпредставляет собой фенил, 3-фторфенил, 4-фторфенил или 2,5-дифторфенил; или к фармацевтически приемлемой кислотно-аддитивной соли в энантиомерно чистом виде с абсолютной конфигурацией, как показано в формуле I. Неожиданно было обнаружено, что соединения общей формулы I являются аллостерическими модуляторами метаботропных глутаматных рецепторов подтипа 5 (mGluR5), которые проявляют улучшенные биохимические, физико-химические и фармакодинамические свойства по сравнению с соединениями, известными из уровня техники.
EA201590557A 2012-09-27 2013-09-23 Производные арилэтинила EA025482B1 (ru)

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
EA201590557A1 true EA201590557A1 (ru) 2015-07-30
EA025482B1 EA025482B1 (ru) 2016-12-30

Family

ID=47044829

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590557A EA025482B1 (ru) 2012-09-27 2013-09-23 Производные арилэтинила

Country Status (30)

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

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
MY171517A (en) * 2012-10-18 2019-10-16 Hoffmann La Roche Ethynyl derivatives as modulators of mglur5 receptor activity
PL3303316T3 (pl) 2015-06-03 2020-06-29 F. Hoffmann-La Roche Ag Pochodne etynylu

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
WO2008151184A1 (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
TWI476194B (zh) 2015-03-11
AR092673A1 (es) 2015-04-29
IL237596A (en) 2017-02-28
IL237596A0 (en) 2015-04-30
US9221802B2 (en) 2015-12-29
MX366136B (es) 2019-06-28
BR112015006218A2 (pt) 2017-07-04
TW201418248A (zh) 2014-05-16
PL2900659T3 (pl) 2017-02-28
JP2015534556A (ja) 2015-12-03
CA2885382A1 (en) 2014-04-17
AU2013329739A1 (en) 2015-03-19
WO2014056710A1 (en) 2014-04-17
EA025482B1 (ru) 2016-12-30
EP2900659A1 (en) 2015-08-05
AU2013329739B2 (en) 2017-04-20
CR20150139A (es) 2015-04-30
PH12015500538B1 (en) 2015-05-04
DK2900659T3 (en) 2016-10-03
CN104684911A (zh) 2015-06-03
HK1207376A1 (en) 2016-01-29
UA113779C2 (xx) 2017-03-10
PE20150708A1 (es) 2015-05-15
ZA201501678B (en) 2016-01-27
MA37941B1 (fr) 2016-11-30
MX2015003560A (es) 2015-06-22
CL2015000707A1 (es) 2015-08-07
SI2900659T1 (sl) 2016-12-30
EP2900659B1 (en) 2016-08-24
US20150197510A1 (en) 2015-07-16
HUE029636T2 (en) 2017-03-28
ES2594031T3 (es) 2016-12-15
KR101737245B1 (ko) 2017-05-17
NZ706283A (en) 2018-07-27
KR20150058477A (ko) 2015-05-28
JP6027251B2 (ja) 2016-11-16
MY171743A (en) 2019-10-27
MA37941A1 (fr) 2016-04-29
PH12015500538A1 (en) 2015-05-04
CN104684911B (zh) 2017-05-10
SG11201502449RA (en) 2015-05-28

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU