CA2610873C - Tetrahydroquinolinones et leur utilisation comme modulateurs de recepteurs metabotropique de glutamate - Google Patents

Tetrahydroquinolinones et leur utilisation comme modulateurs de recepteurs metabotropique de glutamate Download PDF

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Publication number
CA2610873C
CA2610873C CA2610873A CA2610873A CA2610873C CA 2610873 C CA2610873 C CA 2610873C CA 2610873 A CA2610873 A CA 2610873A CA 2610873 A CA2610873 A CA 2610873A CA 2610873 C CA2610873 C CA 2610873C
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Prior art keywords
quinolin
dihydro
dimethyl
ylethynyl
phenylethynyl
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Expired - Fee Related
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CA2610873A
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English (en)
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CA2610873A1 (fr
Inventor
Christopher Graham Raphael Parsons
Aigars Jirgensons
Ieva Jaunzeme
Ivars Kalvinsh
Markus Henrich
Maksims Vanejevs
Tanja Weil
Valerjans Kauss
Wojciech Danysz
Claudia Jatzke
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Merz Pharma GmbH and Co KGaA
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Merz Pharma GmbH and Co KGaA
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Publication of CA2610873A1 publication Critical patent/CA2610873A1/fr
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Publication of CA2610873C publication Critical patent/CA2610873C/fr
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
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    • 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
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
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    • 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
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
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    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
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    • 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
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
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    • 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
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/10Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • 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
    • C07D413/06Heterocyclic 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
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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
    • C07D413/14Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Anesthesiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2610873A 2005-08-24 2006-08-24 Tetrahydroquinolinones et leur utilisation comme modulateurs de recepteurs metabotropique de glutamate Expired - Fee Related CA2610873C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/GB2005/003285 WO2007023242A1 (fr) 2005-08-24 2005-08-24 Tétrahydroquinolinones et leur usage en tant que modulateurs des récepteurs de glutamate métabotropiques
GBPCT/GB2005/003285 2005-08-24
PCT/GB2006/003170 WO2007023290A1 (fr) 2005-08-24 2006-08-24 Tétrahydroquinolinones et leur utilisation comme modulateurs de récepteurs métabotropique de glutamate

Publications (2)

Publication Number Publication Date
CA2610873A1 CA2610873A1 (fr) 2007-03-01
CA2610873C true CA2610873C (fr) 2010-08-03

Family

ID=36273537

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2610873A Expired - Fee Related CA2610873C (fr) 2005-08-24 2006-08-24 Tetrahydroquinolinones et leur utilisation comme modulateurs de recepteurs metabotropique de glutamate

Country Status (15)

Country Link
EP (1) EP1931635A1 (fr)
JP (1) JP2009506018A (fr)
KR (1) KR20080031972A (fr)
CN (1) CN101223142A (fr)
AR (1) AR056044A1 (fr)
AU (1) AU2006283359B2 (fr)
BR (1) BRPI0615059A2 (fr)
CA (1) CA2610873C (fr)
EA (1) EA200800660A1 (fr)
IL (1) IL189617A (fr)
MX (1) MX2008001871A (fr)
NO (1) NO20081428L (fr)
TW (1) TWI329635B (fr)
WO (2) WO2007023242A1 (fr)
ZA (1) ZA200710668B (fr)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
CN102666551B (zh) 2009-12-18 2014-12-10 詹森药业有限公司 作为mglur5受体的变构调节剂的双环噻唑
WO2011073339A1 (fr) * 2009-12-18 2011-06-23 Janssen Pharmaceutica Nv Thiazoles bicycliques en tant que modulateurs allostériques des récepteurs mglur5
US8772301B2 (en) 2009-12-18 2014-07-08 Sunovion Pharmaceuticals, Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー CRF−1受容体アンタゴニストとしてのピラゾロ[5,1b]オキサゾール誘導体
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Crf受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
AR083475A1 (es) 2010-10-18 2013-02-27 Merz Pharma Gmbh & Co Kgaa Moduladores de receptores de glutamato metabotropicos
WO2012139876A1 (fr) 2011-04-14 2012-10-18 Merz Pharma Gmbh & Co. Kgaa Formulations entériques de modulateurs de récepteur de glutamate métabotropique
WO2012172093A1 (fr) * 2011-06-17 2012-12-20 Merz Pharma Gmbh & Co. Kgaa Dérivé de dihydroindolizine à titre de modulateurs des récepteurs métabotropes de glutamate
WO2013050527A1 (fr) 2011-10-05 2013-04-11 H. Lundbeck A/S Dérivés de quinazoline en tant qu'inhibiteurs de l'enzyme pde10a
EP2650284A1 (fr) * 2012-04-10 2013-10-16 Merz Pharma GmbH & Co. KGaA Dérivés hétérocycliques comme modulateurs de récepteurs du glutamate métabotropique
KR101418078B1 (ko) * 2013-01-23 2014-07-10 한국과학기술연구원 mGluR5 길항제로서의 2-(치환된에티닐)퀴놀린 유도체
JP6744218B2 (ja) 2013-11-15 2020-08-19 ザ ウィスター インスティテュート オブ アナトミー アンド バイオロジー Ebna1阻害剤およびそれらの使用方法
KR101579496B1 (ko) * 2014-07-03 2015-12-23 한국과학기술연구원 mGluR5의 표식용 방사성 조성물
WO2016154527A1 (fr) * 2015-03-26 2016-09-29 Merck Sharp & Dohme Corp. Dérivés de quinolizine substitués par un phosphate utiles en tant qu'inhibiteurs de l'intégrase du vih
BR112017024481B1 (pt) 2015-05-14 2020-11-17 The Wistar Institute Of Anatomy And Biology composto inibidor de ebna1, composição farmacêutica compreendendo dito composto e usos terapêuticos do mesmo
PL3303330T3 (pl) 2015-06-03 2019-10-31 Bristol Myers Squibb Co Agoniści 4 - hydroksy - 3 - ( heteroarylo ) pirydyno - 2 - onowi receptora apj do stosowania w leczeniu zaburzeń sercowo-naczyniowych
EP3459939A1 (fr) * 2017-09-26 2019-03-27 Pragma Therapeutics Nouveaux composés hétérocycliques comme modulateurs de mglur7
TW201946919A (zh) 2018-05-17 2019-12-16 威斯塔研究所 Ebna1抑制劑晶形、其製備方法及其使用方法
CA3155209A1 (fr) * 2019-10-21 2021-04-29 Chan Mi Joung Utilisation de composes d'imidazopyrimidine ou d'imidazotriazine pour la prevention, le soulagement ou le traitement de troubles cognitifs, ou pour ameliorer la fonction cognitive
CA3155013A1 (fr) * 2019-10-21 2021-04-29 Ki Ho Lee Utilisation de compose d'imidazopyrimidine ou d'imidazotriazine pour la prevention, le soulagement ou le traitement d'un trouble du developpement

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ20031145A3 (cs) * 2000-10-02 2003-12-17 Janssen Pharmaceutica N.V. Antagonisté metabotropního glutamátového receptoru
TWI301760B (en) * 2004-02-27 2008-10-11 Merz Pharma Gmbh & Co Kgaa Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors

Also Published As

Publication number Publication date
IL189617A0 (en) 2008-06-05
AU2006283359B2 (en) 2010-05-27
AR056044A1 (es) 2007-09-12
IL189617A (en) 2012-08-30
ZA200710668B (en) 2009-08-26
WO2007023290A1 (fr) 2007-03-01
CN101223142A (zh) 2008-07-16
EA200800660A1 (ru) 2008-06-30
BRPI0615059A2 (pt) 2011-04-26
CA2610873A1 (fr) 2007-03-01
TWI329635B (en) 2010-09-01
KR20080031972A (ko) 2008-04-11
MX2008001871A (es) 2008-04-09
JP2009506018A (ja) 2009-02-12
NO20081428L (no) 2008-03-18
TW200728283A (en) 2007-08-01
AU2006283359A1 (en) 2007-03-01
WO2007023242A1 (fr) 2007-03-01
EP1931635A1 (fr) 2008-06-18

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