AR064376A1 - Imidazoles sustituios como ligandos de taar, un proceso para su obtencion, y su uso en la preparacion de un medicamento para el tratamiento de enfermedades asociadas a la desregulacion de aminas traza. - Google Patents

Imidazoles sustituios como ligandos de taar, un proceso para su obtencion, y su uso en la preparacion de un medicamento para el tratamiento de enfermedades asociadas a la desregulacion de aminas traza.

Info

Publication number
AR064376A1
AR064376A1 ARP070105650A ARP070105650A AR064376A1 AR 064376 A1 AR064376 A1 AR 064376A1 AR P070105650 A ARP070105650 A AR P070105650A AR P070105650 A ARP070105650 A AR P070105650A AR 064376 A1 AR064376 A1 AR 064376A1
Authority
AR
Argentina
Prior art keywords
formula
compound
defined above
lower alkyl
meaning defined
Prior art date
Application number
ARP070105650A
Other languages
English (en)
Inventor
Guido Galley
Zbinden Katrin Groebke
Roger Nocross
Henri Stalder
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR064376A1 publication Critical patent/AR064376A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • 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
    • A61P25/06Antimigraine agents
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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

Abstract

Compuestos de la formula (1) en la que R es H, alquilo inferior o amino; X-R1 es -CH2-, -CH(alcoxi inferior)- o -CH(OH)- y Y-R2 es -CH2-, -CH(alquilo inferior)-, -CH(alcoxi inferior)-, -O-, -S-, -S(O)-, -S(O)2-, -CH(fenil)- o -C(alquilo inferior)2-; o X-R1 es NH- y Y-R2 es -CH2, -CH(alquilo inferior)-, -CH(alcoxi inferior)-, -CH(fenil)- o -C(alquilo inferior)2-. Reivindicacion 10: Un proceso de obtencion de los compuestos de la formula (1), dicho proceso consiste en: a) desproteger un compuesto de la formula (2) para obtener un compuesto de la formula (1) en las que las definiciones son las que se han indicado antes o b) hidrogenar un compuesto de formula (5) para obtener un compuesto de la formula (3) y desprotegerlo con arreglo al paso a) para obtener un compuesto de la formula (4) en las que Ar tiene el significado definido anteriormente y R2 es H, alquilo inferior o alcoxi inferior, o c) alquilar un compuesto de la formula (9) para obtener un compuesto de la formula (6) y desprotegerlo con arreglo al paso a) para obtener un compuesto de la formula (7) en las que Ar tiene el significado definido anteriormente; o d) hacer reaccionar un compuesto de la formula (11) y un compuesto de la formula ArOH para obtener un compuesto de la formula (8) y desprotegerlo con arreglo al paso a) para obtener un compuesto de la formula (10) en las que las definiciones son las descritas anteriormente o e) hacer reaccionar un compuesto de la formula (12) con acetonitrilo para obtener un compuesto de formula (13) y eliminar el grupo hidroxi para obtener un compuesto de la formula (14) en la que Ar tiene el significado definido anteriormente, o f) hacer reaccionar un compuesto de la formula (15) con un compuesto de formula (16) para obtener un compuesto de la formula (17) y desprotegerlo para obtener un compuesto de la formula (18) en la que R es alquilo inferior y Ar tiene el significado definido anteriormente, o g) hacer reaccionar un compuesto de la formula (11) y un compuesto de la formula ArSH para obtener un compuesto de la formula (19) y desprotegerlo con arreglo al paso a) para obtener un compuesto de la formula (20), en la que Ar tiene el significado definido anteriormente, o h) oxidar un compuesto de la formula (19) para obtener compuesto de las formulas (21), (22) y desprotegerlos con arreglo al paso a) para obtener compuestos de las formulas (23), (24), en las que Ar tiene el significado definido anteriormente; o i) reducir un compuesto de la formula (25) para obtener un compuesto de la formula (26) y desprotegerlo con arreglo al paso a) para obtener compuestos de la formula (27) en la que Ar tiene el significado definido anteriormente y PG es un grupo protector habitual de N; y, si se desea, convertir los compuestos obtenidos en sales de adicion de ácido farmacéuticamente aceptables.
ARP070105650A 2006-12-18 2007-12-17 Imidazoles sustituios como ligandos de taar, un proceso para su obtencion, y su uso en la preparacion de un medicamento para el tratamiento de enfermedades asociadas a la desregulacion de aminas traza. AR064376A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06126307 2006-12-18

Publications (1)

Publication Number Publication Date
AR064376A1 true AR064376A1 (es) 2009-04-01

Family

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Family Applications (1)

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ARP070105650A AR064376A1 (es) 2006-12-18 2007-12-17 Imidazoles sustituios como ligandos de taar, un proceso para su obtencion, y su uso en la preparacion de un medicamento para el tratamiento de enfermedades asociadas a la desregulacion de aminas traza.

Country Status (18)

Country Link
US (3) US20080146523A1 (es)
EP (1) EP2094668A2 (es)
JP (1) JP5175297B2 (es)
KR (1) KR101188992B1 (es)
CN (1) CN101578271B (es)
AR (1) AR064376A1 (es)
AU (1) AU2007336351A1 (es)
BR (1) BRPI0721291A2 (es)
CA (1) CA2671838A1 (es)
CL (1) CL2007003653A1 (es)
IL (1) IL198878A0 (es)
MX (1) MX2009006215A (es)
NO (1) NO20091936L (es)
PE (1) PE20081386A1 (es)
RU (1) RU2465269C2 (es)
TW (1) TWI345467B (es)
WO (1) WO2008074679A2 (es)
ZA (1) ZA200903841B (es)

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WO2012078817A1 (en) 2010-12-08 2012-06-14 Vanderbilt University Bicyclic pyrazole compounds as allosteric modulators of mglur5 receptors
WO2012125732A1 (en) * 2011-03-15 2012-09-20 Vanderbilt University Substituted imadazapyrinidin-5(6h)-ones as allosteric modulators of mglur5 receptors
US8865725B2 (en) 2011-03-15 2014-10-21 Vanderbilt University Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
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CA2671838A1 (en) 2008-06-26
US20120004230A1 (en) 2012-01-05
JP5175297B2 (ja) 2013-04-03
MX2009006215A (es) 2009-06-22
TWI345467B (en) 2011-07-21
JP2010513373A (ja) 2010-04-30
TW200833327A (en) 2008-08-16
CL2007003653A1 (es) 2008-07-11
CN101578271B (zh) 2013-06-19
KR20090081431A (ko) 2009-07-28
ZA200903841B (en) 2010-03-31
IL198878A0 (en) 2010-02-17
US20100204233A1 (en) 2010-08-12
EP2094668A2 (en) 2009-09-02
WO2008074679A3 (en) 2008-10-09
CN101578271A (zh) 2009-11-11
US20080146523A1 (en) 2008-06-19
US8399463B2 (en) 2013-03-19
WO2008074679A2 (en) 2008-06-26
KR101188992B1 (ko) 2012-10-08
NO20091936L (no) 2009-07-14
BRPI0721291A2 (pt) 2014-03-25
RU2465269C2 (ru) 2012-10-27
AU2007336351A1 (en) 2008-06-26
RU2009122665A (ru) 2011-01-27
PE20081386A1 (es) 2008-09-18

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