EA200201030A1 - Карбаматные ингибиторы каспазы и их использование - Google Patents

Карбаматные ингибиторы каспазы и их использование

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Publication number
EA200201030A1
EA200201030A1 EA200201030A EA200201030A EA200201030A1 EA 200201030 A1 EA200201030 A1 EA 200201030A1 EA 200201030 A EA200201030 A EA 200201030A EA 200201030 A EA200201030 A EA 200201030A EA 200201030 A1 EA200201030 A1 EA 200201030A1
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EA
Eurasian Patent Office
Prior art keywords
caspase
carbamatic
caspase inhibitors
inhibitors
snson
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EA200201030A
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English (en)
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EA005740B1 (ru
Inventor
Дэвид Беббингтон
Жан-Дамиен Шаррьер
Дэвид Кэй
Рональд Негтел
Джулиан Голек
Майкл Мортимор
Джон Стадли
Original Assignee
Вертекс Фармасьютикалз Инкорпорейтед
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Application filed by Вертекс Фармасьютикалз Инкорпорейтед filed Critical Вертекс Фармасьютикалз Инкорпорейтед
Publication of EA200201030A1 publication Critical patent/EA200201030A1/ru
Publication of EA005740B1 publication Critical patent/EA005740B1/ru

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Abstract

Настоящее изобретение относится к ингибиторам каспазы формулы Iгде Z представляет кислород или серу; Rпредставляет водород, -CHN, -R, -CHOR, -CHSR или -СН; Y представляет электроотрицательную уходящую группу; Rпредставляет СОН, СНСОН или их сложные эфиры, амиды или изостеры; Rпредставляет группу, способную встраиваться в S2-субсайт каспазы; Rи R, взятые вместе с находящимся между ними азотом, образуют гетероциклическое кольцо и R имеет значения, указанные в описании. Соединения являются эффективными ингибиторами апоптоза и секреции IL-1β.Отчет о международном поиске был опубликован 2002.05.23.
EA200201030A 2000-03-29 2001-03-29 Карбаматные ингибиторы каспазы и их использование EA005740B1 (ru)

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US19282600P 2000-03-29 2000-03-29
PCT/US2001/010182 WO2001072707A2 (en) 2000-03-29 2001-03-29 Carbamate caspase inhibitors and uses thereof

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EA200201030A1 true EA200201030A1 (ru) 2003-02-27
EA005740B1 EA005740B1 (ru) 2005-06-30

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WO2000061542A1 (en) 1999-04-09 2000-10-19 Cytovia, Inc. Caspase inhibitors and the use thereof
IL148426A0 (en) 1999-08-27 2002-09-12 Cytovia Inc α-HYDROXY ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
ATE384695T1 (de) * 2000-03-29 2008-02-15 Vertex Pharma Carbamat caspase inhibitoren und deren verwendung
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
US20040192889A1 (en) * 2001-03-30 2004-09-30 Dale Bredesen Cytotoxic peptides and peptidomimetics based thereon, and methods for use thereof
CA2447999C (en) 2001-05-23 2011-04-26 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
US7410956B2 (en) 2002-02-11 2008-08-12 Vertex Pharmaceuticals Incorporated Caspase inhibitor prodrugs
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