EA201390419A1 - ПРОИЗВОДНЫЕ 4,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-6-ИЛАМИНА, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ) - Google Patents

ПРОИЗВОДНЫЕ 4,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-6-ИЛАМИНА, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ)

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Publication number
EA201390419A1
EA201390419A1 EA201390419A EA201390419A EA201390419A1 EA 201390419 A1 EA201390419 A1 EA 201390419A1 EA 201390419 A EA201390419 A EA 201390419A EA 201390419 A EA201390419 A EA 201390419A EA 201390419 A1 EA201390419 A1 EA 201390419A1
Authority
EA
Eurasian Patent Office
Prior art keywords
beta
dihydropyrazolo
bace
dementia
derivatives
Prior art date
Application number
EA201390419A
Other languages
English (en)
Other versions
EA021723B1 (ru
Inventor
Андрес Авелино Трабанко-Суарес
Гэри Джон Тресадерн
Франсиска Дельгадо-Хименес
Original Assignee
Янссен Фармацевтика Нв
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 Янссен Фармацевтика Нв filed Critical Янссен Фармацевтика Нв
Publication of EA201390419A1 publication Critical patent/EA201390419A1/ru
Publication of EA021723B1 publication Critical patent/EA021723B1/ru

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Classifications

    • 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
    • A61P25/28—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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 4,7-дигидропиразоло[1,5-а]пиразин-6-ил-амина, используемым в качестве ингибиторов бета-секретазы, известной также в качестве фермента, расщепляющего бета-сайт амилоида, ВАСЕ, ВАСЕ1, Asp2 или мемапсина 2. Изобретение относится также 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 которых принимает участие бета-секретаза, таких как болезнь Альцгеймера (AD), умеренное когнитивное расстройство, старение, деменция, деменция с тельцами Леви, синдром Дауна, деменция, связанная с инсультом, деменция, связанная с болезнью Паркинсона, или деменция, связанная с бета-амилоидом.
EA201390419A 2010-09-22 2011-09-20 ПРОИЗВОДНЫЕ 4,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-6-ИЛАМИНА, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ) EA021723B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10178315 2010-09-22
EP11157858 2011-03-11
PCT/EP2011/066343 WO2012038438A1 (en) 2010-09-22 2011-09-20 4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

Publications (2)

Publication Number Publication Date
EA201390419A1 true EA201390419A1 (ru) 2013-07-30
EA021723B1 EA021723B1 (ru) 2015-08-31

Family

ID=45873470

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201390419A EA021723B1 (ru) 2010-09-22 2011-09-20 ПРОИЗВОДНЫЕ 4,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-6-ИЛАМИНА, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ)

Country Status (21)

Country Link
US (1) US8609660B2 (ru)
EP (1) EP2619207B1 (ru)
JP (1) JP5797756B2 (ru)
KR (1) KR101962216B1 (ru)
CN (1) CN103097389B (ru)
AU (1) AU2011306941B2 (ru)
BR (1) BR112013006353A2 (ru)
CA (1) CA2807904C (ru)
CL (1) CL2013000782A1 (ru)
CO (1) CO6660450A2 (ru)
EA (1) EA021723B1 (ru)
ES (1) ES2529641T3 (ru)
HK (1) HK1182391A1 (ru)
IL (1) IL225349A (ru)
IN (1) IN2013MN00782A (ru)
MX (1) MX2013003246A (ru)
MY (1) MY160138A (ru)
NZ (1) NZ606848A (ru)
SG (1) SG188338A1 (ru)
WO (1) WO2012038438A1 (ru)
ZA (1) ZA201302128B (ru)

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ES2476027T3 (es) 2005-10-25 2014-07-11 Shionogi & Co., Ltd. Derivados de aminodihidrotriazina
ES2476605T3 (es) 2007-04-24 2014-07-15 Shionogi & Co., Ltd. Derivados de aminohidrotiazina sustituidos con grupos cíclicos
WO2008133273A1 (ja) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
AU2009258496B8 (en) 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
WO2011154431A1 (en) 2010-06-09 2011-12-15 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
EP2634186A4 (en) 2010-10-29 2014-03-26 Shionogi & Co naphthyridine
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
AU2011347377B2 (en) 2010-12-22 2016-03-03 Janssen Pharmaceutica Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
ES2534973T3 (es) 2011-03-09 2015-04-30 Janssen Pharmaceutica N.V. Derivados de 3,4-dihidro-pirrolo[1,2-a]pirazin-1-ilamina útiles como inhibidores de beta-secretasa (BACE)
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
US9771617B2 (en) 2011-06-27 2017-09-26 Eisai R&D Management Co., Ltd. Microrna biomarkers indicative of alzheimer's disease
WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
CN105452251B (zh) 2013-06-12 2017-12-26 詹森药业有限公司 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑5,6‑二氢咪唑并[1,5‑A]吡嗪‑3(2H)‑酮衍生物
EP3008066B1 (en) 2013-06-12 2018-08-15 Janssen Pharmaceutica N.V. 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
CN105324383B (zh) 2013-06-12 2017-10-31 詹森药业有限公司 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物
EP3233834B1 (en) 2014-12-18 2019-11-13 Janssen Pharmaceutica NV 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
WO2019025250A1 (en) 2017-08-04 2019-02-07 Basf Se SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI
CN108440320A (zh) * 2018-05-09 2018-08-24 上海凌凯医药科技有限公司 一种高手性选择性合成α-双取代α-氨基酸的方法

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BR0317525A (pt) * 2002-12-20 2005-11-16 Pharmacia Corp Compostos pirazol acìclico, composição terapêutica e farmacêutica, kit, bem como respectivos usos
KR20080028881A (ko) 2005-06-14 2008-04-02 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제, 이의제조방법 및 용도
TW200804290A (en) * 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
WO2011002409A1 (en) * 2009-07-02 2011-01-06 Astrazeneca Ab 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase

Also Published As

Publication number Publication date
KR20130110161A (ko) 2013-10-08
CO6660450A2 (es) 2013-04-30
CA2807904A1 (en) 2012-03-29
IL225349A0 (en) 2013-06-27
NZ606848A (en) 2015-01-30
AU2011306941A1 (en) 2013-02-28
BR112013006353A2 (pt) 2024-01-16
EP2619207A1 (en) 2013-07-31
US20130190318A1 (en) 2013-07-25
JP5797756B2 (ja) 2015-10-21
HK1182391A1 (zh) 2013-11-29
EA021723B1 (ru) 2015-08-31
EP2619207B1 (en) 2014-11-12
ZA201302128B (en) 2014-08-27
US8609660B2 (en) 2013-12-17
CN103097389B (zh) 2015-10-14
AU2011306941B2 (en) 2014-06-12
MY160138A (en) 2017-02-28
SG188338A1 (en) 2013-04-30
CA2807904C (en) 2018-09-11
CL2013000782A1 (es) 2013-08-09
ES2529641T3 (es) 2015-02-24
MX2013003246A (es) 2013-05-22
CN103097389A (zh) 2013-05-08
IL225349A (en) 2016-07-31
KR101962216B1 (ko) 2019-03-26
IN2013MN00782A (ru) 2015-06-12
WO2012038438A1 (en) 2012-03-29
JP2013540740A (ja) 2013-11-07

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU