EA201390932A1 - ПРОИЗВОДНЫЕ 5,6-ДИГИДРОИМИДАЗО[1,2-а]ПИРАЗИН-8-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ) - Google Patents

ПРОИЗВОДНЫЕ 5,6-ДИГИДРОИМИДАЗО[1,2-а]ПИРАЗИН-8-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ)

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Publication number
EA201390932A1
EA201390932A1 EA201390932A EA201390932A EA201390932A1 EA 201390932 A1 EA201390932 A1 EA 201390932A1 EA 201390932 A EA201390932 A EA 201390932A EA 201390932 A EA201390932 A EA 201390932A EA 201390932 A1 EA201390932 A1 EA 201390932A1
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EA
Eurasian Patent Office
Prior art keywords
dementia
beta
dihydroimidazo
bace
compounds
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EA201390932A
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English (en)
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EA022409B1 (ru
Inventor
Андрес Авелино Трабанко-Суарес
Франсиска Дельгадо-Хименес
Хуан Антонио Вега Рамиро
Гэри Джон Тресадерн
Хенрикус Якобус Мария Гейсен
Дэниел Оельрих
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Янссен Фармацевтика Нв
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Publication of EA201390932A1 publication Critical patent/EA201390932A1/ru
Publication of EA022409B1 publication Critical patent/EA022409B1/ru

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    • 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
    • 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
    • A61P25/28—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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение относится к новым производным 5,6-дигидроимидазо[1,2-а]пиразин-8-иламина в качестве ингибиторов бета-секретазы, также известной как фермент расщепления амилоида по бета-сайту, ВАСЕ, ВАСЕ1, Asp2 или мемапсин 2. Изобретение также относится к фармацевтическим композициям, содержащим такие соединения, способам получения таких соединений и композиций и к применению таких соединений и композиций для профилактики и лечения заболеваний, в которые вовлечена бета-секретаза, таких как болезнь Альцгеймера (AD), умеренные когнитивные нарушения, старение, деменция, деменция с тельцами Леви, церебральная амилоидная ангиопатия, мультиинфарктная деменция, синдром Дауна, деменция, ассоциированная с инсультом, деменция, ассоциированная с болезнью Паркинсона, или деменция, ассоциированная с бета-амилоидом.
EA201390932A 2010-12-22 2011-12-21 Производные 5,6-дигидроимидазо[1,2-а]пиразин-8-иламина, пригодные в качестве ингибиторов бета-секретазы (васе) EA022409B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10196568 2010-12-22
PCT/EP2011/073522 WO2012085038A1 (en) 2010-12-22 2011-12-21 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

Publications (2)

Publication Number Publication Date
EA201390932A1 true EA201390932A1 (ru) 2013-11-29
EA022409B1 EA022409B1 (ru) 2015-12-30

Family

ID=43923528

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201390932A EA022409B1 (ru) 2010-12-22 2011-12-21 Производные 5,6-дигидроимидазо[1,2-а]пиразин-8-иламина, пригодные в качестве ингибиторов бета-секретазы (васе)

Country Status (20)

Country Link
US (1) US9840507B2 (ru)
EP (1) EP2655376B1 (ru)
JP (1) JP5834091B2 (ru)
KR (1) KR101866987B1 (ru)
CN (1) CN103403007B (ru)
AU (1) AU2011347377B2 (ru)
BR (1) BR112013015430A2 (ru)
CA (1) CA2819175C (ru)
CO (1) CO6721049A2 (ru)
EA (1) EA022409B1 (ru)
ES (1) ES2648143T3 (ru)
HK (1) HK1189221A1 (ru)
IL (1) IL227054A (ru)
MX (1) MX347912B (ru)
MY (1) MY170715A (ru)
NZ (1) NZ610948A (ru)
SG (1) SG191097A1 (ru)
UA (1) UA109459C2 (ru)
WO (1) WO2012085038A1 (ru)
ZA (1) ZA201304646B (ru)

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ZA201304646B (en) 2014-12-23
MX347912B (es) 2017-05-17
IL227054A (en) 2016-09-29
UA109459C2 (xx) 2015-08-25
US9840507B2 (en) 2017-12-12
CA2819175A1 (en) 2012-06-28
CA2819175C (en) 2019-01-08
US20130274266A1 (en) 2013-10-17
JP2014500293A (ja) 2014-01-09
SG191097A1 (en) 2013-08-30
EA022409B1 (ru) 2015-12-30
EP2655376A1 (en) 2013-10-30
AU2011347377A1 (en) 2013-06-13
JP5834091B2 (ja) 2015-12-16
KR101866987B1 (ko) 2018-07-19
AU2011347377B2 (en) 2016-03-03
KR20130132556A (ko) 2013-12-04
MY170715A (en) 2019-08-27
WO2012085038A1 (en) 2012-06-28
CN103403007A (zh) 2013-11-20
MX2013007294A (es) 2013-08-26
NZ610948A (en) 2014-06-27
ES2648143T3 (es) 2017-12-28
BR112013015430A2 (pt) 2016-09-20
CN103403007B (zh) 2015-12-09
EP2655376B1 (en) 2017-08-23
CO6721049A2 (es) 2013-07-31
HK1189221A1 (zh) 2014-05-30

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