ECSP12011611A - Derivados de imidazol como antagonistas de mglur5 - Google Patents

Derivados de imidazol como antagonistas de mglur5

Info

Publication number
ECSP12011611A
ECSP12011611A EC2012011611A ECSP12011611A ECSP12011611A EC SP12011611 A ECSP12011611 A EC SP12011611A EC 2012011611 A EC2012011611 A EC 2012011611A EC SP12011611 A ECSP12011611 A EC SP12011611A EC SP12011611 A ECSP12011611 A EC SP12011611A
Authority
EC
Ecuador
Prior art keywords
lower alkyl
independently
alkoxyalkyl
hydrogen
hydroxyalkyl
Prior art date
Application number
EC2012011611A
Other languages
English (en)
Inventor
Georg Jaeschke
Jurgen Wichmann
Eric Vieira
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42358156&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP12011611(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ECSP12011611A publication Critical patent/ECSP12011611A/es

Links

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/32—Alcohol-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
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención, se refiere a derivados de imidazol de la fórmula general (I)en dondeR1, significa halógeno, alquilo inferior ó alcoxi inferior; R2, significa alquilo inferior, hidroxialquilo inferior, o alcoxialquilo inferior; R3, significa hidrógeno, alquilo inferior, hidroxialquilo inferior o alcoxialquilo; Q, significa ó -N= ó -CH=;R4, es un grupo de la formula IIa ó IIb en donde, X, Y y Z, son, de una forma independiente, -CH= ó -N=; y en donde, solamente una de entre las X ó Y, puede ser un átomo de nitrógeno;R5 y R6 son, de una forma independiente, hidrógeno, alquilo inferior, hidroxialquilo inferior, alcoxialquilo inferior, -(CH2)m-(CO)O-alquilo inferior, -(CH2)m-S(O)2-alquilo inferior, -(CH2)m-C(O)-NR'R'', y en donde, m = 0 - 3 y R' y R'' son, de una forma independiente, hidrógeno ó alquilo inferior, así como a las sales farmacéuticamente aceptables de éstos. Se ha encontrado ahora, de una forma sorprendente, el hecho de que, los compuestos de la fórmula general I, son antagonistas de los receptores metabotrópicos de glutamato. Éstos pueden utilizarse en el tratamiento o la prevención de trastornos mediatizados por el receptor mGluR5.
EC2012011611A 2009-07-17 2012-01-17 Derivados de imidazol como antagonistas de mglur5 ECSP12011611A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09165780 2009-07-17

Publications (1)

Publication Number Publication Date
ECSP12011611A true ECSP12011611A (es) 2012-02-29

Family

ID=42358156

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2012011611A ECSP12011611A (es) 2009-07-17 2012-01-17 Derivados de imidazol como antagonistas de mglur5

Country Status (34)

Country Link
US (1) US8334287B2 (es)
EP (1) EP2456765B1 (es)
JP (1) JP5667182B2 (es)
KR (1) KR101431347B1 (es)
CN (1) CN102471309B (es)
AR (1) AR077481A1 (es)
AU (1) AU2010272585B2 (es)
BR (1) BR112012001092A2 (es)
CA (1) CA2765921C (es)
CL (1) CL2012000102A1 (es)
CO (1) CO6400142A2 (es)
CR (1) CR20110659A (es)
CY (1) CY1114186T1 (es)
DK (1) DK2456765T3 (es)
EC (1) ECSP12011611A (es)
ES (1) ES2411467T3 (es)
HK (1) HK1169397A1 (es)
HR (1) HRP20130657T1 (es)
IL (1) IL216746A (es)
MA (1) MA33386B1 (es)
MX (1) MX2012000814A (es)
MY (1) MY156878A (es)
NZ (1) NZ596810A (es)
PE (1) PE20120397A1 (es)
PL (1) PL2456765T3 (es)
PT (1) PT2456765E (es)
RS (1) RS52901B (es)
RU (1) RU2527106C2 (es)
SG (1) SG178052A1 (es)
SI (1) SI2456765T1 (es)
TW (1) TWI423964B (es)
UA (1) UA107086C2 (es)
WO (1) WO2011006910A1 (es)
ZA (1) ZA201109451B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA113223C2 (xx) * 2012-08-13 2016-12-26 Арилетинілпіримідини
US20170173008A1 (en) * 2014-03-19 2017-06-22 President And Fellows Of Harvard College Antimicrobial agents and screening methods

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5965583A (en) * 1997-04-24 1999-10-12 Ortho-Mcneil Pharmaceutical, Inc. Substituted imidazoles useful in the treatment of inflammatory disease
KR100515549B1 (ko) 2000-12-04 2005-09-20 에프. 호프만-라 로슈 아게 글루타메이트 수용체 길항제로서의 페닐에테닐 또는페닐에티닐 유도체
GB0128996D0 (en) 2001-12-04 2002-01-23 Novartis Ag Organic compounds
TWI292318B (en) * 2003-03-10 2008-01-11 Hoffmann La Roche Imidazol-4-yl-ethynyl-pyridine derivatives
UA80888C2 (en) * 2003-06-05 2007-11-12 Hoffmann La Roche Imidazole derivatives as glutmate receptor antagonists
EP1670784B1 (en) * 2003-06-12 2011-01-12 F. Hoffmann-La Roche AG Heteroaryl-substituted imdazole derivatives as glutamate receptor antagonists
US7452909B2 (en) * 2003-09-04 2008-11-18 Hoffman-La Roche Inc. Imidazole derivatives
PL1756086T3 (pl) * 2004-06-01 2008-11-28 Hoffmann La Roche Pirydyn-4-ylo-etynylo-imidazole i pirazole jako antagoniści receptora mGlu5
BRPI0511678A (pt) * 2004-06-01 2008-01-08 Hoffmann La Roche piridin-4-il-etinil-imidazóis e pirazóis como antagonistas de receptor de mglu5
EP2578216A1 (en) 2006-11-22 2013-04-10 Seaside Therapeutics, Inc. Methods of treating fragile x syndrome

Also Published As

Publication number Publication date
PT2456765E (pt) 2013-06-20
KR101431347B1 (ko) 2014-08-19
CN102471309A (zh) 2012-05-23
RU2527106C2 (ru) 2014-08-27
PE20120397A1 (es) 2012-04-24
IL216746A (en) 2015-03-31
JP2012532913A (ja) 2012-12-20
CO6400142A2 (es) 2012-03-15
SG178052A1 (en) 2012-03-29
TW201116523A (en) 2011-05-16
CA2765921A1 (en) 2011-01-20
US8334287B2 (en) 2012-12-18
MA33386B1 (fr) 2012-06-01
WO2011006910A1 (en) 2011-01-20
HK1169397A1 (en) 2013-01-25
IL216746A0 (en) 2012-03-01
CN102471309B (zh) 2014-09-03
EP2456765A1 (en) 2012-05-30
CA2765921C (en) 2017-04-18
MX2012000814A (es) 2012-03-14
ZA201109451B (en) 2012-08-29
CR20110659A (es) 2012-03-02
JP5667182B2 (ja) 2015-02-12
DK2456765T3 (da) 2013-05-27
ES2411467T3 (es) 2013-07-05
US20110015202A1 (en) 2011-01-20
PL2456765T3 (pl) 2013-09-30
CY1114186T1 (el) 2016-08-31
NZ596810A (en) 2014-01-31
RU2012104399A (ru) 2013-08-27
TWI423964B (zh) 2014-01-21
SI2456765T1 (sl) 2013-06-28
BR112012001092A2 (pt) 2020-08-25
HRP20130657T1 (en) 2013-08-31
KR20120032033A (ko) 2012-04-04
CL2012000102A1 (es) 2012-09-07
EP2456765B1 (en) 2013-05-01
UA107086C2 (ru) 2014-11-25
MY156878A (en) 2016-04-15
RS52901B (en) 2014-02-28
AU2010272585B2 (en) 2013-11-07
AU2010272585A1 (en) 2012-01-19
AR077481A1 (es) 2011-08-31

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