EA201291435A1 - Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace) - Google Patents

Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)

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Publication number
EA201291435A1
EA201291435A1 EA201291435A EA201291435A EA201291435A1 EA 201291435 A1 EA201291435 A1 EA 201291435A1 EA 201291435 A EA201291435 A EA 201291435A EA 201291435 A EA201291435 A EA 201291435A EA 201291435 A1 EA201291435 A1 EA 201291435A1
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EA
Eurasian Patent Office
Prior art keywords
beta
bace
oxazin
dementia
compounds
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EA201291435A
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English (en)
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EA021240B1 (ru
Inventor
Андрес Авелино Трабанко-Суарес
Фредерик Ян Рита Ромбаутс
Гэри Джон Тресадерн
Михиль Люк Мария Ван Гол
Грегор Джеймс Макдональд
Каролина Мартинес Ламенка
Хенрикус Якобус Мария Гейсен
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Янссен Фармацевтика Нв
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Publication of EA201291435A1 publication Critical patent/EA201291435A1/ru
Publication of EA021240B1 publication Critical patent/EA021240B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic 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
    • A61P25/14—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
    • A61P25/28—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
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings

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

Abstract

Настоящее изобретение относится к новым производным 5,6-дигидро-2Н-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы, также известной как фермент, расцепляющий амилоид в бета-участке, ВАСЕ, ВАСЕ1, Asp2 или мемапсин 2. Изобретение также относится к фармацевтическим композициям, содержащим такие соединения, к способам получения таких соединений и композиций и к применению таких соединений и композиций для предотвращения и лечения нарушений, в которые вовлечена бета-секретаза, таких как болезнь Альцгеймера (AD), умеренное когнитивное нарушение, старость, деменция, деменция с тельцами Леви, синдром Дауна, деменция, ассоциированная с инсультом, деменция, ассоциированная с болезнью Паркинсона, и деменция, ассоциированная с бета-амилоидом.
EA201291435A 2010-06-09 2011-06-08 Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace) EA021240B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP10165335 2010-06-09
EP11152314 2011-01-27
EP11157765 2011-03-10
EP11164999 2011-05-05
PCT/EP2011/059441 WO2011154431A1 (en) 2010-06-09 2011-06-08 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)

Publications (2)

Publication Number Publication Date
EA201291435A1 true EA201291435A1 (ru) 2013-05-30
EA021240B1 EA021240B1 (ru) 2015-05-29

Family

ID=44317911

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201291435A EA021240B1 (ru) 2010-06-09 2011-06-08 Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)

Country Status (22)

Country Link
US (2) US20130109683A1 (ru)
EP (1) EP2580200B1 (ru)
JP (1) JP5711813B2 (ru)
KR (1) KR101730937B1 (ru)
CN (1) CN102933564B (ru)
AR (1) AR081587A1 (ru)
AU (1) AU2011263797B2 (ru)
BR (1) BR112012031094A2 (ru)
CA (1) CA2799640C (ru)
CL (1) CL2012003428A1 (ru)
CO (1) CO6602112A2 (ru)
DK (1) DK2580200T3 (ru)
EA (1) EA021240B1 (ru)
ES (1) ES2607083T3 (ru)
HK (1) HK1182098A1 (ru)
IL (1) IL223423A (ru)
MX (1) MX339640B (ru)
NZ (1) NZ603427A (ru)
SG (1) SG185651A1 (ru)
TW (1) TWI537263B (ru)
WO (1) WO2011154431A1 (ru)
ZA (1) ZA201209297B (ru)

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