AR086121A1 - Derivados de oxazina y una composicion farmaceutica para inhibir bace1 que los contienen - Google Patents

Derivados de oxazina y una composicion farmaceutica para inhibir bace1 que los contienen

Info

Publication number
AR086121A1
AR086121A1 ARP120101461A ARP120101461A AR086121A1 AR 086121 A1 AR086121 A1 AR 086121A1 AR P120101461 A ARP120101461 A AR P120101461A AR P120101461 A ARP120101461 A AR P120101461A AR 086121 A1 AR086121 A1 AR 086121A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
alkylsulfinyl
alkenyl
acyl
Prior art date
Application number
ARP120101461A
Other languages
English (en)
Original Assignee
Shionogi & Co
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 Shionogi & Co filed Critical Shionogi & Co
Publication of AR086121A1 publication Critical patent/AR086121A1/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
    • 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
    • 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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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

Abstract

Este compuesto tiene un efecto de inhibición de la producción de b amiloide, en especial un efecto de inhibición de BACE1 y que es de utilidad como un agente terapéutico o preventivo para enfermedades inducidas por producción, secreción y/o deposición de proteínas b amiloides.Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), en donde -X= es -CR7= o -N=; el anillo B es un carbociclo sustituido o no sustituido o un heterociclo sustituido o no sustituido; R1 es alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, acilo sustituido o no sustituido, ciano, carboxi, alcoxicarbonilo sustituido o no sustituido, alqueniloxicarbonilo sustituido o no sustituido, alquiniloxicarbonilo sustituido o no sustituido, carbamoilo sustituido o no sustituido, tiocarbamoilo sustituido o no sustituido, un grupo carbocíclico sustituido o no sustituido o un grupo heterocíclico sustituido o no sustituido; R2a y R2b son cada uno, de modo independiente, hidrógeno, alquilo sustituido o no sustituido, acilo sustituido o no sustituido, alcoxicarbonilo sustituido o no sustituido o carbamoilo sustituido o no sustituido; R3 y R4 son cada uno, de modo independiente, hidrógeno, halógeno, hidroxi, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, alcoxi sustituido o no sustituido, alqueniloxi sustituido o no sustituido, alquiniloxi sustituido o no sustituido, alquiltio sustituido o no sustituido, alqueniltio sustituido o no sustituido, alquiniltio sustituido o no sustituido, acilo sustituido o no sustituido, aciloxi sustituido o no sustituido, ciano, nitro, carboxi, alcoxicarbonilo sustituido o no sustituido, alqueniloxicarbonilo sustituido o no sustituido, alquiniloxicarbonilo sustituido o no sustituido, amino sustituido o no sustituido, carbamoilo sustituido o no sustituido, tiocarbamoilo sustituido o no sustituido, sulfamoilo sustituido o no sustituido, alquilsulfinilo sustituido o no sustituido, alquenilsulfinilo sustituido o no sustituido, alquinilsulfinilo sustituido o no sustituido, alquilsulfonilo sustituido o no sustituido, alquenilsulfonilo sustituido o no sustituido, alquinilsulfonilo sustituido o no sustituido, un grupo carbocíclico sustituido o no sustituido, carbocicliloxi sustituido o no sustituido, carbocicliltio sustituido o no sustituido, carbociclilalquilo sustituido o no sustituido, carbociclilalcoxi sustituido o no sustituido, carbocicliloxicarbonilo sustituido o no sustituido, carbociclilsulfinilo sustituido o no sustituido, carbociclilsulfonilo sustituido o no sustituido, un grupo heterocíclico sustituido o no sustituido, heterocicliloxi sustituido o no sustituido, heterocicliltio sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, heterociclilalcoxi sustituido o no sustituido, heterocicliloxicarbonilo sustituido o no sustituido, heterociclilsulfinilo sustituido o no sustituido o heterociclilsulfonilo sustituido o no sustituido; R5 es hidrógeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido o acilo sustituido o no sustituido; cada R6 es, de modo independiente, halógeno, hidroxi, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, alcoxi sustituido o no sustituido, alqueniloxi sustituido o no sustituido, alquiniloxi sustituido o no sustituido, alquiltio sustituido o no sustituido, alqueniltio sustituido o no sustituido, alquiniltio sustituido o no sustituido, acilo sustituido o no sustituido, aciloxi sustituido o no sustituido, ciano, nitro, carboxi, alcoxicarbonilo sustituido o no sustituido, alqueniloxicarbonilo sustituido o no sustituido, alquiniloxicarbonilo sustituido o no sustituido, amino sustituido o no sustituido, carbamoilo sustituido o no sustituido, tiocarbamoilo sustituido o no sustituido, sulfamoilo sustituido o no sustituido, alquilsulfinilo sustituido o no sustituido, alquenilsulfinilo sustituido o no sustituido, alquinilsulfinilo sustituido o no sustituido, alquilsulfonilo sustituido o no sustituido, alquenilsulfonilo sustituido o no sustituido o alquinilsulfonilo sustituido o no sustituido; R7 es hidrógeno, halógeno, hidroxi, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, alcoxi sustituido o no sustituido, alqueniloxi sustituido o no sustituido, alquiniloxi sustituido o no sustituido, alquiltio sustituido o no sustituido, alqueniltio sustituido o no sustituido, alquiniltio sustituido o no sustituido, acilo sustituido o no sustituido, aciloxi sustituido o no sustituido, ciano, nitro, carboxi, alcoxicarbonilo sustituido o no sustituido, alqueniloxicarbonilo sustituido o no sustituido, alquiniloxicarbonilo sustituido o no sustituido, amino sustituido o no sustituido, carbamoilo sustituido o no sustituido, tiocarbamoilo sustituido o no sustituido, sulfamoilo sustituido o no sustituido, alquilsulfinilo sustituido o no sustituido, alquenilsulfinilo sustituido o no sustituido, alquinilsulfinilo sustituido o no sustituido, alquilsulfonilo sustituido o no sustituido, alquenilsulfonilo sustituido o no sustituido o alquinilsulfonilo sustituido o no sustituido; y p es un número entero de 0 a 3; o una de sus sales farmacéuticamente aceptables.
ARP120101461A 2011-04-26 2012-04-26 Derivados de oxazina y una composicion farmaceutica para inhibir bace1 que los contienen AR086121A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2011098121 2011-04-26
JP2011127185 2011-06-07
JP2011274039 2011-12-15

Publications (1)

Publication Number Publication Date
AR086121A1 true AR086121A1 (es) 2013-11-20

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ARP120101461A AR086121A1 (es) 2011-04-26 2012-04-26 Derivados de oxazina y una composicion farmaceutica para inhibir bace1 que los contienen

Country Status (7)

Country Link
US (1) US8883779B2 (es)
EP (1) EP2703399A4 (es)
JP (1) JPWO2012147763A1 (es)
CN (1) CN103608345A (es)
AR (1) AR086121A1 (es)
TW (1) TW201247635A (es)
WO (1) WO2012147763A1 (es)

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