CL2010001467A1 - Compuestos derivados de fenil-imidazol sustituido con un heteroaromatico biciclico; composicion farmaceutica que los comprende; y su uso como inhibidores de la pde10a para tratar trastornos neurodegenerativos o psiquiatricos como alzheimer, demencia alcoholica, trastorno del aprendizaje, esquizofrenia, adiccion a las drogas. - Google Patents

Compuestos derivados de fenil-imidazol sustituido con un heteroaromatico biciclico; composicion farmaceutica que los comprende; y su uso como inhibidores de la pde10a para tratar trastornos neurodegenerativos o psiquiatricos como alzheimer, demencia alcoholica, trastorno del aprendizaje, esquizofrenia, adiccion a las drogas.

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Publication number
CL2010001467A1
CL2010001467A1 CL2010001467A CL2010001467A CL2010001467A1 CL 2010001467 A1 CL2010001467 A1 CL 2010001467A1 CL 2010001467 A CL2010001467 A CL 2010001467A CL 2010001467 A CL2010001467 A CL 2010001467A CL 2010001467 A1 CL2010001467 A1 CL 2010001467A1
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CL
Chile
Prior art keywords
subject
schizophrenia
alzheimer
inhibitors
pharmaceutical composition
Prior art date
Application number
CL2010001467A
Other languages
English (en)
Inventor
Jan Kehler
Andreas Ritzen
Jacob Nielsen
Morten Langgard
John Paul Kilburn
Mohamed M Farah
Original Assignee
H Lundbeck As
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 H Lundbeck As filed Critical H Lundbeck As
Publication of CL2010001467A1 publication Critical patent/CL2010001467A1/es

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    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P25/14—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
    • A61P25/28—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
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE DESCRIBE COMPUESTOS DE FÓRMULA (I), COMPOSICIÓN FARMACÉUTICA QUE COMPRENDE UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE LA INVENCIÓN Y UN PORTADOR FARMACÉUTICAMENTE ACEPTABLE. LA PRESENTE INVENCIÓN PROPORCIONA ADEMÁS UN MÉTODO PARA TRATAR UN SUJETO QUE SUFRE UN TRASTORNO NEURODEGENERATIVO, QUE COMPRENDE ADMINISTRAR AL SUJETO UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE FÓRMULA 1. LA PRESENTE INVENCIÓN ASIMISMO PROPORCIONA UN MÉTODO PARA TRATAR UN SUJETO QUE SUFRE UNA ADICCIÓN A LAS DROGAS, QUE COMPRENDE ADMINISTRAR AL SUJETO UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE FÓRMULA 1. LA PRESENTE INVENCIÓN TAMBIÉN PROPORCIONA UN MÉTODO PARA TRATAR UN SUJETO QUE SUFRE UN TRASTORNO PSIQUIÁTRICO, QUE COMPRENDE ADMINISTRAR AL SUJETO UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE FÓRMULA I; Y EL USO DE DICHOS COMO INHIBIDORES DE LA ENZIMA PDE10A PARA EL TRATAMIENTO DE TRASTORNOS NEURODEGENERATIVOS O PSIQUIÁTRICOS COMO ALZHEIMER, DEMENCIA ALCOHÓLICA, TRASTORNO DEL APRENDIZAJE, ESQUIZOFRENIA, ADICCIÓN A IAS DROGAS.
CL2010001467A 2008-06-20 2010-12-17 Compuestos derivados de fenil-imidazol sustituido con un heteroaromatico biciclico; composicion farmaceutica que los comprende; y su uso como inhibidores de la pde10a para tratar trastornos neurodegenerativos o psiquiatricos como alzheimer, demencia alcoholica, trastorno del aprendizaje, esquizofrenia, adiccion a las drogas. CL2010001467A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA200800855 2008-06-20
DKPA200900402 2009-03-24
DKPA200900519 2009-04-22

Publications (1)

Publication Number Publication Date
CL2010001467A1 true CL2010001467A1 (es) 2011-08-05

Family

ID=40902594

Family Applications (2)

Application Number Title Priority Date Filing Date
CL2010001467A CL2010001467A1 (es) 2008-06-20 2010-12-17 Compuestos derivados de fenil-imidazol sustituido con un heteroaromatico biciclico; composicion farmaceutica que los comprende; y su uso como inhibidores de la pde10a para tratar trastornos neurodegenerativos o psiquiatricos como alzheimer, demencia alcoholica, trastorno del aprendizaje, esquizofrenia, adiccion a las drogas.
CL2011003205A CL2011003205A1 (es) 2008-06-20 2011-12-16 Compuesto 5,8-dimetil-2-[2-(1-metil-4-fenil-1h-imidazol-2-il)-etil]-[1,2,4]triazolo[1,5-a]pirazina; composicion farmaceutica; y su uso para el tratamiento de un trastorno neurodegenerativo, tales como alzheimer y demencias.

Family Applications After (1)

Application Number Title Priority Date Filing Date
CL2011003205A CL2011003205A1 (es) 2008-06-20 2011-12-16 Compuesto 5,8-dimetil-2-[2-(1-metil-4-fenil-1h-imidazol-2-il)-etil]-[1,2,4]triazolo[1,5-a]pirazina; composicion farmaceutica; y su uso para el tratamiento de un trastorno neurodegenerativo, tales como alzheimer y demencias.

Country Status (27)

Country Link
US (1) US8841297B2 (es)
EP (1) EP2318394B1 (es)
JP (1) JP5930714B2 (es)
KR (3) KR20170016523A (es)
CN (2) CN102124002B (es)
AR (1) AR072199A1 (es)
AU (1) AU2009259209B2 (es)
BR (1) BRPI0915383B8 (es)
CA (1) CA2728335C (es)
CL (2) CL2010001467A1 (es)
CO (1) CO6321263A2 (es)
CY (1) CY1115001T1 (es)
DK (1) DK2318394T3 (es)
EA (2) EA018880B1 (es)
ES (1) ES2456349T3 (es)
HR (1) HRP20140232T1 (es)
IL (1) IL209834A (es)
MX (1) MX2010014136A (es)
MY (1) MY152949A (es)
NZ (1) NZ589926A (es)
PL (1) PL2318394T3 (es)
PT (1) PT2318394E (es)
RS (2) RS53226B (es)
SI (1) SI2318394T1 (es)
TW (1) TWI501965B (es)
WO (1) WO2009152825A1 (es)
ZA (1) ZA201100109B (es)

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US20120190685A1 (en) 2012-07-26
EP2318394A1 (en) 2011-05-11
EP2318394B1 (en) 2014-01-22
CN102482262B (zh) 2014-06-25
TW201000481A (en) 2010-01-01
BRPI0915383B8 (pt) 2021-05-25
CO6321263A2 (es) 2011-09-20
KR102025487B1 (ko) 2019-09-25
CN102124002A (zh) 2011-07-13
PL2318394T3 (pl) 2014-09-30
CA2728335A1 (en) 2009-12-23
BRPI0915383B1 (pt) 2020-09-15
IL209834A0 (en) 2011-02-28
EA018880B1 (ru) 2013-11-29
JP5930714B2 (ja) 2016-06-08
RS53704B1 (sr) 2015-04-30
TWI501965B (zh) 2015-10-01
NZ589926A (en) 2011-09-30
AU2009259209A1 (en) 2009-12-23
SI2318394T1 (sl) 2014-07-31
US8841297B2 (en) 2014-09-23
CN102124002B (zh) 2014-06-25
AU2009259209B2 (en) 2013-08-01
ES2456349T3 (es) 2014-04-22
EA201170061A1 (ru) 2011-08-30
CN102482262A (zh) 2012-05-30
BRPI0915383A2 (pt) 2015-11-03
KR20110020845A (ko) 2011-03-03
AR072199A1 (es) 2010-08-11
PT2318394E (pt) 2014-04-03
CY1115001T1 (el) 2016-12-14
EA201270046A1 (ru) 2012-05-30
KR20170016523A (ko) 2017-02-13
HRP20140232T1 (hr) 2014-04-11
WO2009152825A1 (en) 2009-12-23
HK1159632A1 (en) 2012-08-03
ZA201100109B (en) 2012-03-28
DK2318394T3 (en) 2014-03-24
MY152949A (en) 2014-12-15
EA021410B1 (ru) 2015-06-30
CL2011003205A1 (es) 2012-06-22
RS53226B (sr) 2014-08-29
CA2728335C (en) 2016-05-24
IL209834A (en) 2014-02-27
KR20170134781A (ko) 2017-12-06
KR101703938B1 (ko) 2017-02-07
MX2010014136A (es) 2011-01-21
JP2011524381A (ja) 2011-09-01

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