EA201690787A1 - Соединения и их применение в качестве ингибиторов фермента расщепления бета-сайта app (bace) - Google Patents

Соединения и их применение в качестве ингибиторов фермента расщепления бета-сайта app (bace)

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EA201690787A1
EA201690787A1 EA201690787A EA201690787A EA201690787A1 EA 201690787 A1 EA201690787 A1 EA 201690787A1 EA 201690787 A EA201690787 A EA 201690787A EA 201690787 A EA201690787 A EA 201690787A EA 201690787 A1 EA201690787 A1 EA 201690787A1
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dementia
alzheimer
disease
bace
connections
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EA201690787A
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EA032687B1 (ru
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Габор Черньик
Софиа Карлстрем
Анника Керс
Карин Колмодин
Мартин Нюлеф
Лиселотте Эхберг
Ласло Ракош
Ларс Сандберг
Фернандо Сехгельмебле
Петер Седерман
Бритт-Марие Свахн
Берг Стефан Фон
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Астразенека Аб
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Abstract

Изобретение относится к соединениям формулы (I) и их фармацевтическим композициям. Кроме того, настоящее изобретение относится к терапевтическим способам для лечения и/или предупреждения Аβ-ассоциированных патологий, таких как синдром Дауна, β-амилоидная ангиопатия, например, церебральная амилоидная ангиопатия или наследственная церебральная геморрагия, но ими не ограничиваясь, расстройств, ассоциированных с когнитивным нарушением, таких как MCI ("умеренное когнитивное нарушение"), болезнь Альцгеймера, потеря памяти, симптомы дефицита внимания, ассоциированные с болезнью Альцгеймера, нейродегенерация, ассоциированная с такими заболеваниями, как болезнь Альцгеймера или деменция, в том числе деменция смешанного сосудистого и дегенеративного происхождения, пресенильная деменция, сенильная деменция и деменция, ассоциированная с болезнью Паркинсона, но ими не ограничиваясь.
EA201690787A 2010-12-22 2011-12-21 СОЕДИНЕНИЕ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ПРИМЕНЕНИЕ СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ ИЛИ ПРЕДУПРЕЖДЕНИЯ Аβ-АССОЦИИРОВАННОЙ ПАТОЛОГИИ И СПОСОБ ЛЕЧЕНИЯ ИЛИ ПРЕДУПРЕЖДЕНИЯ Аβ-АССОЦИИРОВАННОЙ ПАТОЛОГИИ EA032687B1 (ru)

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US201061425852P 2010-12-22 2010-12-22
US201161529620P 2011-08-31 2011-08-31

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EA201690787A1 true EA201690787A1 (ru) 2017-02-28
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EA201690787A EA032687B1 (ru) 2010-12-22 2011-12-21 СОЕДИНЕНИЕ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ПРИМЕНЕНИЕ СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ ИЛИ ПРЕДУПРЕЖДЕНИЯ Аβ-АССОЦИИРОВАННОЙ ПАТОЛОГИИ И СПОСОБ ЛЕЧЕНИЯ ИЛИ ПРЕДУПРЕЖДЕНИЯ Аβ-АССОЦИИРОВАННОЙ ПАТОЛОГИИ
EA201390830A EA025746B9 (ru) 2010-12-22 2011-12-21 Соединения и их применение в качестве ингибиторов фермента расщепления бета-сайта app (bace)

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Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011106414A1 (en) 2010-02-24 2011-09-01 Dillard Lawrence W Inhibitors of beta-secretase
US8415483B2 (en) * 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
EP2780321B1 (en) 2011-10-10 2015-12-30 Astrazeneca AB Mono-fluoro beta-secretase inhibitors
US8779355B2 (en) 2011-12-28 2014-07-15 Quest Diagnostics Investments, Inc. Methods for detecting lacosamide by mass spectrometry
SG11201403956VA (en) 2012-01-26 2014-10-30 Hoffmann La Roche Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
TWI557112B (zh) * 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β-分泌酶抑制劑
AU2013267555A1 (en) 2012-05-30 2014-12-04 Comentis, Inc. Chromane compounds
US9000182B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine compounds and their use as BACE inhibitors
US9000183B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000184B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000185B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
US10548882B2 (en) * 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt
TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β-分泌酶抑制劑
WO2014052398A1 (en) * 2012-09-28 2014-04-03 Vitae Pharmaceuticals, Inc. Inhibitor of beta-secretase
EP3653609B1 (en) 2013-02-12 2024-04-03 Buck Institute for Research on Aging Hydantoins that modulate bace-mediated app processing
AR102202A1 (es) 2014-10-07 2017-02-08 Astrazeneca Ab Compuestos de oxazol y su uso como inhibidores de bace de oxazol
EP3429620A1 (en) 2016-03-15 2019-01-23 AstraZeneca AB Combination of a bace inhibitor and an antibody or antigen-binding fragment for the treatment of a disorder associated with the accumulation of amyloid beta
AR107783A1 (es) 2016-03-15 2018-06-06 Lilly Co Eli Terapia de combinación
JPWO2017169503A1 (ja) * 2016-04-01 2019-02-14 国立大学法人千葉大学 含窒素芳香族アミドの製造方法、ピロール・イミダゾールポリアミドの製造方法、及び化合物
CN107892697B (zh) 2016-12-26 2020-11-03 郑州泰基鸿诺医药股份有限公司 一种[1,3]噻嗪-2-胺类化合物及应用,药物组合物
CN107954927A (zh) * 2017-10-30 2018-04-24 广东莱佛士制药技术有限公司 一种3-溴-5-(丙炔-1-基)吡啶的制备方法
WO2019122268A1 (en) 2017-12-21 2019-06-27 Astrazeneca Ab Processes for the stereoselective preparation of bace inhibitors
WO2019122421A1 (en) 2017-12-22 2019-06-27 Astrazeneca Ab Stereoselective ketone reduction using a ketoreductase enzyme
WO2019129750A1 (en) 2017-12-29 2019-07-04 Astrazeneca Ab Processes for the racemization of dihydroimidazole ring systems
WO2019129755A1 (en) 2017-12-29 2019-07-04 Astrazeneca Ab Ketal hydrogenation
CN110615751B (zh) * 2018-06-19 2021-08-17 上海医药工业研究院 一种2-氧代硫代丙酰胺的制备方法
CN113573709A (zh) 2019-03-14 2021-10-29 阿斯利康(瑞典)有限公司 用于体重减轻的兰比斯特
CN111253427A (zh) * 2020-03-13 2020-06-09 苏州大学 正丁基锂在催化醛和硅烷的氰硅化反应中的应用
CN114989103A (zh) * 2022-06-09 2022-09-02 杭州科巢生物科技有限公司 一种2-甲氧基-3-(1-甲基-1h-1,2,4-三唑-3-基)苯胺的制备方法

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100452491B1 (ko) 2001-03-29 2004-10-12 한미약품 주식회사 신규한 결정형 암로디핀 캠실레이트 염 및 그의 제조방법
WO2002098462A1 (fr) * 2001-06-01 2002-12-12 Ono Pharmaceutical Co., Ltd. Remedes contenant un inhibiteur d'aldose reductase en tant qu'agent actif destines a des troubles de demyelinisation ou des troubles associes a la demyelinisation
US7592348B2 (en) * 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
ATE445399T1 (de) 2004-03-22 2009-10-15 Lilly Co Eli Pyridyl-derivate und ihre verwendung als mglu5- rezeptorantagonisten
US7868000B2 (en) 2005-06-14 2011-01-11 Schering Corporation Aspartyl protease inhibitors
CN101360716A (zh) 2005-11-21 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基-咪唑-4-酮化合物及其在制备用于治疗认知缺损、阿尔茨海默病、神经变性和痴呆的药物中的用途
WO2007076247A1 (en) 2005-12-21 2007-07-05 Boehringer Ingelheim International Gmbh Pyrimidine derivatives useful as inhibitors of pkc-theta
WO2007100536A1 (en) 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
UA96598C2 (ru) * 2006-06-22 2011-11-25 Астразенека Аб Замещенные изоиндолы как ингибиторы васе и их применение
WO2008076044A1 (en) * 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5, 5-diaryl-imidazol-4-ones
US20090325993A1 (en) * 2007-02-01 2009-12-31 Nadia Mamoona Ahmad GLYT1 Transporter Inhibitors and Uses Thereof in Treatment of Neurological and Neuropsychiatric Disorders
KR20100017573A (ko) * 2007-05-07 2010-02-16 쉐링 코포레이션 감마 세크레타제 조정인자
EP2249646A4 (en) 2008-02-06 2013-09-25 Glaxo Group Ltd PDE4 muscarinic Antagonist-DOPPELPHARMACOPHOREN
FR2929943B1 (fr) 2008-04-15 2010-09-24 Inst Rech Developpement Ird Sels de quinoleines 2-substituees
CA2731209A1 (en) 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
US8450308B2 (en) 2008-08-19 2013-05-28 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
MX2011002705A (es) 2008-09-11 2011-09-09 Amgen Inc Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso.
KR20120001756A (ko) 2009-03-13 2012-01-04 비타이 파마슈티컬즈, 인코포레이티드 베타세크리타아제 저해제
UY32751A (es) 2009-07-02 2011-01-31 Astrazeneca Ab Imidazoles sustituidos y uso de los mismos
UY32750A (es) 2009-07-02 2011-01-31 Astrazeneca Ab Imidazoles sustituidos y uso de los mismos
WO2011106414A1 (en) 2010-02-24 2011-09-01 Dillard Lawrence W Inhibitors of beta-secretase
AR080865A1 (es) 2010-03-31 2012-05-16 Array Biopharma Inc Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer.
WO2011130741A1 (en) 2010-04-16 2011-10-20 Array Biopharma Inc. Compounds for treating neurodegenerative diseases
EP2601197B1 (en) 2010-08-05 2014-06-25 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
UY33627A (es) 2010-09-24 2013-04-30 Array Biopharma Inc Compuestos para tratar enfermedades neurodegenerativas
AR083953A1 (es) 2010-11-22 2013-04-10 Array Biopharma Inc Compuestos para tratar enfermedades neurodegenerativas
US8415483B2 (en) 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
EP2780321B1 (en) 2011-10-10 2015-12-30 Astrazeneca AB Mono-fluoro beta-secretase inhibitors
US9000182B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine compounds and their use as BACE inhibitors
US9000184B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000183B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000185B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
US10548882B2 (en) 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt

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