UA96126C2 - Соединение для ингибирования активности rho киназы, фармацевтическая композиция, которая содержит такое соединение, и способ ингибирования активности rho киназы - Google Patents

Соединение для ингибирования активности rho киназы, фармацевтическая композиция, которая содержит такое соединение, и способ ингибирования активности rho киназы

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UA96126C2
UA96126C2 UAA200711701A UAA200711701A UA96126C2 UA 96126 C2 UA96126 C2 UA 96126C2 UA A200711701 A UAA200711701 A UA A200711701A UA A200711701 A UAA200711701 A UA A200711701A UA 96126 C2 UA96126 C2 UA 96126C2
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rhokinase
activity
compound
inhibiting
inhibition
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UAA200711701A
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English (en)
Ukrainian (uk)
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Алессандра Бартолоцци
Стюарт Кемпбелл
Хоуп Фудулакис
Брайян Кирк
Сия Рам
Пол Свитнем
Хемалатха Сешадри
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Сьёрфейс Лоджикс, Инк.
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Application filed by Сьёрфейс Лоджикс, Инк. filed Critical Сьёрфейс Лоджикс, Инк.
Publication of UA96126C2 publication Critical patent/UA96126C2/ru

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Abstract

Данное изобретение касается ингибиторов ROCK1 и ROCK2 и способов модуляции фармакокинетических и/или фармакодинамических свойств таких соединений.Также описаны способы ингибирования ROCK1 и или ROCK2, которые применяются для лечения заболевания.
UAA200711701A 2005-03-25 2006-03-27 Соединение для ингибирования активности rho киназы, фармацевтическая композиция, которая содержит такое соединение, и способ ингибирования активности rho киназы UA96126C2 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US66516505P 2005-03-25 2005-03-25

Publications (1)

Publication Number Publication Date
UA96126C2 true UA96126C2 (ru) 2011-10-10

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UAA200711701A UA96126C2 (ru) 2005-03-25 2006-03-27 Соединение для ингибирования активности rho киназы, фармацевтическая композиция, которая содержит такое соединение, и способ ингибирования активности rho киназы

Country Status (21)

Country Link
US (6) US8357693B2 (ru)
EP (1) EP1865958B1 (ru)
JP (2) JP2008534518A (ru)
KR (1) KR20080081122A (ru)
CN (1) CN101208094B (ru)
AU (1) AU2006230159A1 (ru)
BR (1) BRPI0622285A2 (ru)
CA (1) CA2602254C (ru)
CR (1) CR9465A (ru)
EA (1) EA022875B1 (ru)
EC (1) ECSP077836A (ru)
ES (1) ES2549397T3 (ru)
GE (1) GEP20105029B (ru)
IL (1) IL186299A0 (ru)
MX (1) MX2007011859A (ru)
NO (1) NO20075145L (ru)
NZ (1) NZ562083A (ru)
SG (1) SG155163A1 (ru)
UA (1) UA96126C2 (ru)
WO (1) WO2006105081A2 (ru)
ZA (1) ZA200708858B (ru)

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