EA200602154A1 - Пиридин-4-илэтинилимидазолы и -пиразолы как антагонисты рецептора mglu5 - Google Patents

Пиридин-4-илэтинилимидазолы и -пиразолы как антагонисты рецептора mglu5

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Publication number
EA200602154A1
EA200602154A1 EA200602154A EA200602154A EA200602154A1 EA 200602154 A1 EA200602154 A1 EA 200602154A1 EA 200602154 A EA200602154 A EA 200602154A EA 200602154 A EA200602154 A EA 200602154A EA 200602154 A1 EA200602154 A1 EA 200602154A1
Authority
EA
Eurasian Patent Office
Prior art keywords
ileetinilimidazoles
pyrazoles
pyridin
antagonists
mglu5 receptor
Prior art date
Application number
EA200602154A
Other languages
English (en)
Other versions
EA011722B1 (ru
Inventor
Бернд Бюттельманн
Симона Мария Чеккарелли
Георг Йэшке
Забине Кольчевски
Ричард Хью Филлип Портер
Эрик Фиайра
Пол Спурр
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
Priority claimed from PCT/EP2004/005881 external-priority patent/WO2004108701A1/en
Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Priority claimed from PCT/EP2005/005559 external-priority patent/WO2005118568A1/en
Publication of EA200602154A1 publication Critical patent/EA200602154A1/ru
Publication of EA011722B1 publication Critical patent/EA011722B1/ru

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    • 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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/14Drugs 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
    • A61P25/22Anxiolytics
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

В заявке описаны производные диазола общей формулы (I)в которой А, Е, R, Rи Rявляются такими, как определено в формуле изобретения и описании, их применение для приготовления лекарственных средств, предназначенных для лечения заболеваний, и способы их получения.
EA200602154A 2004-06-01 2005-05-23 Пиридин-4-илэтинилимидазолы и -пиразолы как антагонисты рецептора mglu5 EA011722B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/EP2004/005881 WO2004108701A1 (en) 2003-06-05 2004-06-01 Imidazole derivatives as glutmate receptor antagonists
EP04021216 2004-09-07
PCT/EP2005/005559 WO2005118568A1 (en) 2004-06-01 2005-05-23 Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists

Publications (2)

Publication Number Publication Date
EA200602154A1 true EA200602154A1 (ru) 2007-06-29
EA011722B1 EA011722B1 (ru) 2009-04-28

Family

ID=35758209

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200602154A EA011722B1 (ru) 2004-06-01 2005-05-23 Пиридин-4-илэтинилимидазолы и -пиразолы как антагонисты рецептора mglu5

Country Status (19)

Country Link
US (2) US20060030559A1 (ru)
JP (1) JP4690395B2 (ru)
KR (2) KR101057032B1 (ru)
AR (1) AR054072A1 (ru)
BR (1) BRPI0511678A (ru)
CR (1) CR8742A (ru)
CY (1) CY1108232T1 (ru)
DK (1) DK1756086T3 (ru)
EA (1) EA011722B1 (ru)
EC (1) ECSP067039A (ru)
ES (1) ES2307182T3 (ru)
HK (1) HK1105972A1 (ru)
HR (1) HRP20080363T3 (ru)
IL (1) IL179524A (ru)
MA (1) MA28602B1 (ru)
NZ (1) NZ551253A (ru)
PT (1) PT1756086E (ru)
SI (1) SI1756086T1 (ru)
TW (1) TWI297683B (ru)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8329703B2 (en) * 2005-02-15 2012-12-11 Xtl Biopharmaceuticals Ltd. Pyrazole compounds
US8334287B2 (en) * 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
US20120039999A1 (en) * 2010-08-11 2012-02-16 Ashish Chatterji Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists
US20120040008A1 (en) * 2010-08-11 2012-02-16 Ashish Chatterji Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists
WO2017117708A1 (en) * 2016-01-05 2017-07-13 Hua Medicine (Shanghai) Ltd. Pyrazole derivatives
CN108883104A (zh) 2016-03-30 2018-11-23 森泰克希斯公司 用于在治疗成熟脑损伤中使用的mGluR5的负性变构调节剂
AU2021285273A1 (en) 2020-06-05 2023-01-19 Noema Pharma Ag Methods of treatment of tuberous sclerosis complex
EP4188370A1 (en) * 2020-07-30 2023-06-07 Noema Pharma AG Methods of treatment of trigeminal neuralgia

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US3341548A (en) * 1964-04-29 1967-09-12 Hoffmann La Roche Nitroimidazoles and their preparation
DE2035905A1 (de) 1970-07-20 1972-02-03 Chemische Fabrik Stockhausen & Cie.,4150Krefeld Imidazolverbindungen und deren Herstellungsverfahren
CA1174673A (en) 1981-02-27 1984-09-18 Walter Hunkeler Imidazodiazepines
EP0079312A3 (de) 1981-11-11 1984-04-25 Ciba-Geigy Ag Heterocyclische Acetylenverbindungen
US4711962A (en) * 1984-10-18 1987-12-08 Stauffer Chemical Company Process for selective preparation of ratios of isomers formed on N-substitution of asymmetric imidazoles
DE69025473T2 (de) 1989-06-30 1996-10-17 Du Pont Substituierte imidazole und ihre verwendung als hemmmstoff fur angiotensin ii
TW544448B (en) 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
TR200000405T2 (tr) 1997-08-14 2000-08-21 F.Hoffmann-La Roche Ag Nörolojik rahatsızlıklara karşı heterosiklik vinileterler.
WO2001016121A1 (en) * 1999-08-31 2001-03-08 Merck & Co., Inc. Heterocyclic compounds and methods of use thereof
WO2001029012A2 (en) 1999-10-15 2001-04-26 F. Hoffmann-La Roche Ag Benzodiazepine derivatives as metabotropic glutamate receptor antagonists
IL136553A0 (en) 2000-06-05 2001-06-14 Compugen Ltd SPLICE VARIANT OF mGluR
EP1303495B1 (en) 2000-07-24 2010-05-26 Krenitsky Pharmaceuticals, Inc. Substituted 5-alkynyl pyrimidines having neurotrophic activity
ATE288898T1 (de) * 2000-12-04 2005-02-15 Hoffmann La Roche Phenylethenyl- oder phenylethinylderivate als glutamatrezeptorantagonisten
EP1238586A1 (en) 2001-03-09 2002-09-11 Basf Aktiengesellschaft Herbicidal 2-alkynyl-pyri(mi)dines
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Also Published As

Publication number Publication date
HRP20080363T3 (en) 2008-09-30
KR101057032B1 (ko) 2011-08-16
BRPI0511678A (pt) 2008-01-08
US8293916B2 (en) 2012-10-23
AR054072A1 (es) 2007-06-06
SI1756086T1 (sl) 2008-08-31
IL179524A (en) 2012-04-30
ECSP067039A (es) 2006-12-29
DK1756086T3 (da) 2008-08-04
CY1108232T1 (el) 2014-02-12
PT1756086E (pt) 2008-08-08
ES2307182T3 (es) 2008-11-16
KR100907108B1 (ko) 2009-07-09
KR20080089523A (ko) 2008-10-06
US20060030559A1 (en) 2006-02-09
TWI297683B (en) 2008-06-11
US20100048569A1 (en) 2010-02-25
JP4690395B2 (ja) 2011-06-01
NZ551253A (en) 2010-07-30
EA011722B1 (ru) 2009-04-28
CR8742A (es) 2007-08-28
KR20070021231A (ko) 2007-02-22
IL179524A0 (en) 2007-05-15
HK1105972A1 (en) 2008-02-29
MA28602B1 (fr) 2007-05-02
TW200609222A (en) 2006-03-16
JP2008500979A (ja) 2008-01-17

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