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AR069849A1 - Derivados de heteroarilo como antagonistas de receptor de orexina - Google Patents

Derivados de heteroarilo como antagonistas de receptor de orexina

Info

Publication number
AR069849A1
AR069849A1 ARP080105570A ARP080105570A AR069849A1 AR 069849 A1 AR069849 A1 AR 069849A1 AR P080105570 A ARP080105570 A AR P080105570A AR P080105570 A ARP080105570 A AR P080105570A AR 069849 A1 AR069849 A1 AR 069849A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
substituted
halogen
phenyl
heteroaryl group
Prior art date
Application number
ARP080105570A
Other languages
English (en)
Inventor
Olivier Roche
Mark Rogers-Evans
Emmanuel Pinard
Matthias Nettekoven
Henner Knust
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 AR069849A1 publication Critical patent/AR069849A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • 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
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    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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Abstract

La presente se refiere a compuestos de la formula (1) en la que Ar es un grupo arilo o heteroarilo sustituido o sin sustituir, dicho grupo arilo o heteroarilo puede estar sustituido por uno o más sustituyentes R2; R2 es hidroxi, halogeno, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior, alcoxi inferior sustituido por halogeno, C(O)-alquilo inferior, nitro, NR'Rö, ciano, S-alquilo inferior, SO2-alquilo inferior, cicloalquilo, heterocicloalquilo, feniloxi, benciloxi, fenilo, NH-fenilo o heteroarilo, dicho grupo fenilo o heteroarilo está sin sustituir o sustituido por uno o más sustituyentes elegidos entre alquilo inferior y halogeno; R'/R'' con independencia entre sí son hidrogeno o alquilo inferior; R1 es hidrogeno o alquilo inferior; Het es un resto heteroarilo sin sustituir o sustituido por uno o más sustituyentes elegidos entre R3; R3 es hidroxi, halogeno, =O, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior, fenilo, alcoxi inferior sustituido por halogeno, nitro, ciano, SO2-alquiIo inferior, cicloalquilo o heterocicloalquilo; n es el numero 1 o 2; o a sales de adicion de ácido farmacéuticamente aceptables, enantiomeros opticamente puros, racematos o mezclas diastereoméricas de los mismos. Se ha encontrado que los compuestos de la formula (1) son antagonistas de receptor de orexina y los compuestos en cuestion pueden ser utiles para el tratamiento de la apnea nocturna, la narcolepsia, el insomnio, la parasomnia, el síndrome de la diferencia horaria (jet Iag), el trastorno del ritmo circadiano o los trastornos del sueno asociados con enfermedades neurologicas. Reivindicacion 1: Un compuesto de la formula (1) en la que Ar es un grupo arilo o heteroarilo sustituido o sin sustituir, dicho grupo arilo o heteroarilo puede estar sustituido por uno o más sustituyentes R2; R2 es hidroxi, halogeno, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior, alcoxi inferior sustituido por halogeno, C(O)-alquilo inferior, nitro, NR'R'', ciano, S-alquilo inferior, SO2-alquilo inferior, cicloalquilo, heterocicloalquilo, feniloxi, benciloxi, fenilo, NH-fenilo o heteroarilo, dicho grupo fenilo o heteroarilo está sin sustituir o sustituido por uno o más sustituyentes elegidos entre alquilo inferior y halogeno; R'/R'' con independencia entre sí son hidrogeno o alquilo inferior; R1 es hidrogeno o alquilo inferior; Het es un resto heteroarilo sin sustituir o sustituido por uno o más sustituyentes elegidos entre R3; R3 es hidroxi, halogeno, =O, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior, fenilo, alcoxi inferior sustituido por halogeno, nitro, ciano, SO2-alquilo inferior, cicloalquilo o heterocicloalquilo; n es el numero 1 o 2; o sales de adicion de ácido farmacéuticamente aceptables, enantiomeros opticamente puros, racematos o mezclas diastereoméricas del mismo.
ARP080105570A 2007-12-21 2008-12-19 Derivados de heteroarilo como antagonistas de receptor de orexina AR069849A1 (es)

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EP07150294 2007-12-21

Publications (1)

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AR069849A1 true AR069849A1 (es) 2010-02-24

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Country Status (14)

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US (1) US7897627B2 (es)
EP (1) EP2234999A1 (es)
JP (1) JP5395808B2 (es)
KR (1) KR101204213B1 (es)
CN (1) CN101903372B (es)
AR (1) AR069849A1 (es)
AU (1) AU2008340421B2 (es)
BR (1) BRPI0821141A2 (es)
CA (1) CA2705411A1 (es)
CL (1) CL2008003787A1 (es)
IL (1) IL205665A (es)
PE (1) PE20091173A1 (es)
TW (1) TW200930362A (es)
WO (1) WO2009080533A1 (es)

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PE20091173A1 (es) 2009-08-03
BRPI0821141A2 (pt) 2015-06-16
IL205665A0 (en) 2010-11-30
TW200930362A (en) 2009-07-16
WO2009080533A1 (en) 2009-07-02
CA2705411A1 (en) 2009-07-02
KR20100082807A (ko) 2010-07-19
CL2008003787A1 (es) 2010-02-19
US20090163485A1 (en) 2009-06-25
CN101903372A (zh) 2010-12-01
AU2008340421B2 (en) 2013-12-19
JP5395808B2 (ja) 2014-01-22
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KR101204213B1 (ko) 2012-11-26
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