EA201692048A1 - Дигидротиазин и дигидрооксазин производные, обладающие ингибирующей bace1 активностью - Google Patents

Дигидротиазин и дигидрооксазин производные, обладающие ингибирующей bace1 активностью

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Publication number
EA201692048A1
EA201692048A1 EA201692048A EA201692048A EA201692048A1 EA 201692048 A1 EA201692048 A1 EA 201692048A1 EA 201692048 A EA201692048 A EA 201692048A EA 201692048 A EA201692048 A EA 201692048A EA 201692048 A1 EA201692048 A1 EA 201692048A1
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EA
Eurasian Patent Office
Prior art keywords
dihydrotiazin
owned
dihydro
substituted
alkyl
Prior art date
Application number
EA201692048A
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English (en)
Inventor
Кен-ити Кусакабе
Гента Тадано
Кадзуо Комано
Коуки Футино
Кендзи Накахара
Original Assignee
Сионоги Энд Ко., Лтд.
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Publication date
Application filed by Сионоги Энд Ко., Лтд. filed Critical Сионоги Энд Ко., Лтд.
Publication of EA201692048A1 publication Critical patent/EA201692048A1/ru

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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
    • 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
    • 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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • 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
    • C07D413/14—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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Настоящее изобретение относится к соединению, которое обладает ингибирующим продуцирование β-амилоида действием, в частности ингибирующим ВАСЕ1 действием, и которое может быть использовано в качестве терапевтического или профилактического средства при заболеваниях, вызванных путем продуцирования, секреции и/или депонирования β-амилоидных белков. Соединение формулы (I)где X представляет собой -S- или -O-, Rпредставляет собой алкил, галогеналкил или тому подобное, Rпредставляет собой Н, галоген, алкилокси, галогеналкилокси или тому подобное, Rпредставляет собой Н или тому подобное, Rпредставляет собой Н или алкил, кольцо А и кольцо В, каждое независимо, представляют собой замещенный или незамещенный ароматический карбоцикл, замещенный или незамещенный ароматический гетероцикл или тому подобное, и Rпредставляет собой замещенный или незамещенный алкил или тому подобное, или его фармацевтически приемлемая соль.
EA201692048A 2014-04-11 2015-04-10 Дигидротиазин и дигидрооксазин производные, обладающие ингибирующей bace1 активностью EA201692048A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2014081524 2014-04-11
PCT/JP2015/062314 WO2015156421A1 (en) 2014-04-11 2015-04-10 Dihydrothiazine and dihydrooxazine derivatives having bace1 inhibitory activity

Publications (1)

Publication Number Publication Date
EA201692048A1 true EA201692048A1 (ru) 2017-04-28

Family

ID=53284477

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201692048A EA201692048A1 (ru) 2014-04-11 2015-04-10 Дигидротиазин и дигидрооксазин производные, обладающие ингибирующей bace1 активностью

Country Status (15)

Country Link
US (1) US20170073337A1 (ru)
EP (1) EP3129370A1 (ru)
JP (1) JP2017510587A (ru)
KR (1) KR20160141849A (ru)
CN (1) CN106414431A (ru)
AR (1) AR100049A1 (ru)
AU (1) AU2015244702A1 (ru)
CA (1) CA2945272A1 (ru)
EA (1) EA201692048A1 (ru)
IL (1) IL248228A0 (ru)
MX (1) MX2016013035A (ru)
PH (1) PH12016501891A1 (ru)
SG (1) SG11201607999VA (ru)
TW (1) TW201623295A (ru)
WO (1) WO2015156421A1 (ru)

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Also Published As

Publication number Publication date
SG11201607999VA (en) 2016-10-28
AR100049A1 (es) 2016-09-07
US20170073337A1 (en) 2017-03-16
MX2016013035A (es) 2017-01-09
PH12016501891A1 (en) 2016-12-19
JP2017510587A (ja) 2017-04-13
IL248228A0 (en) 2016-11-30
KR20160141849A (ko) 2016-12-09
CA2945272A1 (en) 2015-10-15
AU2015244702A1 (en) 2016-10-06
TW201623295A (zh) 2016-07-01
EP3129370A1 (en) 2017-02-15
CN106414431A (zh) 2017-02-15
WO2015156421A1 (en) 2015-10-15

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