RU94015842A - Пептидные кетоны, фармацевтическая композиция и способ ингибирования интерлейкин-1 протеазы - Google Patents

Пептидные кетоны, фармацевтическая композиция и способ ингибирования интерлейкин-1 протеазы

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Publication number
RU94015842A
RU94015842A RU94015842/04A RU94015842A RU94015842A RU 94015842 A RU94015842 A RU 94015842A RU 94015842/04 A RU94015842/04 A RU 94015842/04A RU 94015842 A RU94015842 A RU 94015842A RU 94015842 A RU94015842 A RU 94015842A
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Russia
Prior art keywords
protease
aryl
pharmaceutical composition
heteroaryl
compounds
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RU94015842/04A
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English (en)
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RU2133251C1 (ru
Inventor
И.Долли Роланд
Л.Грейбилл Тодд
Дж.Спейр Гэри
П.Проути Кэтерин
Дж.Шмидт Стейнли
Original Assignee
Стерлинг Уинтроп Инк.
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Priority claimed from US08/060,197 external-priority patent/US5462939A/en
Application filed by Стерлинг Уинтроп Инк. filed Critical Стерлинг Уинтроп Инк.
Publication of RU94015842A publication Critical patent/RU94015842A/ru
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Publication of RU2133251C1 publication Critical patent/RU2133251C1/ru

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Claims (1)

  1. Раскрываются соединения формулы I и их фармацевтически приемлемые соли
    Figure 00000001

    в которой R1 - (CR5R6)n, (CR6R6)n-арил, (CR5R6)n-гетероарил, X-(CR5R6)n, X-(CR5R6)n-арил или X-(CR5R6)n-гетероарил, при этом арил и гетероарил необязательно могут быть замещены; X - О или NR5; R5 и R6 независимо - Н или низший алкил; R2 - Н, галоген, низший алкил или (CR5R6)n-арил; R3 и R4 независимо - Н или алкил; А - D-или α -изомер аминокислоты, выбираемой из группы, состоящей из аланина, валина, лейцина, изолейцина, пролина, фенилаланина, глицина, тирозина, метионина, аспарагина, глутамина, аспарагиновой кислоты, глутаминовой кислоты, лизина, аргинина, гистидина и b -тиенилаланина; Z - CH2 или О; n = 0 - 4; фармацевтические композиции, содержащие такие соединения, и способ ингибирования активности интерлейкин-1β-протеазы у млекопитающих с использованием упомянутых соединений и композиций.
RU94015842A 1993-05-07 1994-05-06 ПЕПТИДНЫЕ КЕТОНЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ ИНТЕРЛЕЙКИН-1βПРОТЕАЗЫ RU2133251C1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US060197 1993-05-07
US08/060,197 US5462939A (en) 1993-05-07 1993-05-07 Peptidic ketones as interleukin-1β-converting enzyme inhibitors

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RU94015842A true RU94015842A (ru) 1996-01-10
RU2133251C1 RU2133251C1 (ru) 1999-07-20

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RU94015842A RU2133251C1 (ru) 1993-05-07 1994-05-06 ПЕПТИДНЫЕ КЕТОНЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ ИНТЕРЛЕЙКИН-1βПРОТЕАЗЫ

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US (2) US5462939A (ru)
EP (1) EP0623606B1 (ru)
JP (1) JPH0725839A (ru)
AT (1) ATE161849T1 (ru)
AU (1) AU668465B2 (ru)
CA (1) CA2123055A1 (ru)
CZ (1) CZ108394A3 (ru)
DE (1) DE69407654T2 (ru)
DK (1) DK0623606T3 (ru)
ES (1) ES2113606T3 (ru)
FI (1) FI942107A (ru)
GR (1) GR3026556T3 (ru)
HK (1) HK1008146A1 (ru)
HU (1) HU217070B (ru)
IL (1) IL109585A0 (ru)
NO (1) NO941675L (ru)
NZ (1) NZ260477A (ru)
PH (1) PH30362A (ru)
RU (1) RU2133251C1 (ru)
SK (1) SK282270B6 (ru)
TW (1) TW377350B (ru)

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RU2171807C2 (ru) * 1995-09-14 2001-08-10 Мерк Патент Гмбх Биотиновые производные, способ их получения, фармацевтические композиции и способ их получения

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