CY1114186T1 - Παραγωγα ιμιδαζολιου ως ανταγωνιστες mglur5 - Google Patents

Παραγωγα ιμιδαζολιου ως ανταγωνιστες mglur5

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Publication number
CY1114186T1
CY1114186T1 CY20131100614T CY131100614T CY1114186T1 CY 1114186 T1 CY1114186 T1 CY 1114186T1 CY 20131100614 T CY20131100614 T CY 20131100614T CY 131100614 T CY131100614 T CY 131100614T CY 1114186 T1 CY1114186 T1 CY 1114186T1
Authority
CY
Cyprus
Prior art keywords
lower alkyl
alkyl
mglur5
iib
imidazoli
Prior art date
Application number
CY20131100614T
Other languages
English (en)
Inventor
Georg Jaeschke
Lothar Lindemann
Eric Vieira
Juergen Wichmann
Original Assignee
F. Hoffmann-La Roche Ag
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=CY1114186(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by F. Hoffmann-La Roche Ag filed Critical F. Hoffmann-La Roche Ag
Publication of CY1114186T1 publication Critical patent/CY1114186T1/el

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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
    • C07D401/04Heterocyclic 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
    • 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
    • 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
    • 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
    • A61P25/08Antiepileptics; 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
    • 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
    • A61P25/32Alcohol-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
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • 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
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Rheumatology (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

Η παρούσα εφεύρεση σχετίζεται με παράγωγα ιμιδαζολίου του γενικού τύπου I, όπου το R1 σημαίνει αλογόνο, κατώτερο αλκύλιο ή κατώτερο αλκοξύλιο· το R2 σημαίνει κατώτερο αλκύλιο, κατώτερο υδροξυαλκύλιο ή κατώτερο αλκοξυαλκύλιο· το R3 σημαίνει υδρογόνο, κατώτερο αλκύλιο, κατώτερο υδροξυαλκύλιο ή αλκοξυαλκύλιο· το Q σημαίνει είτε -Ν= ή -CH=· το R4 είναι μια ομάδα του τύπου IIα ή IIb(τύπος IIα και ΙΙb) όπου τα Χ, Υ και Ζ είναι ανεξαρτήτως -CH- ή -Ν= και όπου μόνο ένα από τα Χ ή Υ μπορεί να είναι άτομο αζώτου· τα R5 και R6 είναι ανεξαρτήτως υδρογόνο, κατώτερο αλκύλιο, κατώτερο υδροξυαλκύλιο, κατώτερο αλκοξυαλκύλιο, -(CH2)m-(CΟ)O- κατώτερο αλκύλιο, -(CΗ2)m-S(Ο)2-κατώτερο αλκύλιο, -(CΗ2)m-C(Ο)-ΝR’R’’ και όπου το m = 0-3 και τα R’ και R’’ είναι ανεξαρτήτως υδρογόνο ή κατώτερο αλκύλιο· καθώς και με φαρμακευτικώς αποδεκτά άλατα αυτών. Σήμερα εντελώς αναπάντεχα βρέθηκε ότι οι ενώσεις του γενικού τύπου (I) είναι ανταγωνιστές μεταβοτροπικού υποδοχέα γλουταμινικού. Μπορούν να χρησιμοποιηθούν στη θεραπευτική αντιμετώπιση ή την πρόληψη διαταραχών στις οποίες μεσολαβεί υποδοχέας mGluR5.
CY20131100614T 2009-07-17 2013-07-22 Παραγωγα ιμιδαζολιου ως ανταγωνιστες mglur5 CY1114186T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09165780 2009-07-17
EP10730192.1A EP2456765B1 (en) 2009-07-17 2010-07-14 Imidazole derivatives as mglur5 antagonists

Publications (1)

Publication Number Publication Date
CY1114186T1 true CY1114186T1 (el) 2016-08-31

Family

ID=42358156

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20131100614T CY1114186T1 (el) 2009-07-17 2013-07-22 Παραγωγα ιμιδαζολιου ως ανταγωνιστες mglur5

Country Status (34)

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

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
WO2002046166A1 (en) 2000-12-04 2002-06-13 F. Hoffmann-La Roche Ag Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists
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
ES2358512T3 (es) * 2003-06-12 2011-05-11 F. Hoffmann-La Roche Ag Derivados de imidazol, sustituidos por heteroarilo como antagonistas del receptor de glutamato.
US7452909B2 (en) * 2003-09-04 2008-11-18 Hoffman-La Roche Inc. Imidazole derivatives
NZ551253A (en) * 2004-06-01 2010-07-30 Hoffmann La Roche Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as MGLU5 receptor antagonists
EP1756086B1 (en) * 2004-06-01 2008-06-04 F.Hoffmann-La Roche Ag Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists
PT2083811T (pt) 2006-11-22 2017-01-23 Clinical Res Ass Llc Métodos de tratamento da síndrome de down, síndrome do x frágil e autismo

Also Published As

Publication number Publication date
AU2010272585B2 (en) 2013-11-07
AU2010272585A1 (en) 2012-01-19
EP2456765A1 (en) 2012-05-30
CN102471309B (zh) 2014-09-03
CA2765921C (en) 2017-04-18
HK1169397A1 (en) 2013-01-25
NZ596810A (en) 2014-01-31
WO2011006910A1 (en) 2011-01-20
PT2456765E (pt) 2013-06-20
MA33386B1 (fr) 2012-06-01
RS52901B (en) 2014-02-28
DK2456765T3 (da) 2013-05-27
CO6400142A2 (es) 2012-03-15
ECSP12011611A (es) 2012-02-29
US20110015202A1 (en) 2011-01-20
AR077481A1 (es) 2011-08-31
EP2456765B1 (en) 2013-05-01
CL2012000102A1 (es) 2012-09-07
MY156878A (en) 2016-04-15
RU2527106C2 (ru) 2014-08-27
SI2456765T1 (sl) 2013-06-28
CA2765921A1 (en) 2011-01-20
HRP20130657T1 (en) 2013-08-31
CN102471309A (zh) 2012-05-23
CR20110659A (es) 2012-03-02
TWI423964B (zh) 2014-01-21
IL216746A (en) 2015-03-31
ES2411467T3 (es) 2013-07-05
BR112012001092A2 (pt) 2020-08-25
SG178052A1 (en) 2012-03-29
PL2456765T3 (pl) 2013-09-30
KR20120032033A (ko) 2012-04-04
US8334287B2 (en) 2012-12-18
TW201116523A (en) 2011-05-16
RU2012104399A (ru) 2013-08-27
MX2012000814A (es) 2012-03-14
UA107086C2 (ru) 2014-11-25
KR101431347B1 (ko) 2014-08-19
JP2012532913A (ja) 2012-12-20
ZA201109451B (en) 2012-08-29
IL216746A0 (en) 2012-03-01
JP5667182B2 (ja) 2015-02-12
PE20120397A1 (es) 2012-04-24

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