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PHARMACEUTICAL COMPOSITIONS OF METABOTROPIC GLUTAMATE RECEPTOR 5 ANTAGONISTS (MGLU5)
专利权人:
Ф. ХОФФМАНН-ЛЯ РОШ АГ (CH)
发明人:
ЧЭТТЕРДЖИ Ашиш (US),ХУАН Цзинцзюнь (US),КЁННИНГС Штефани (CH),ЛИНДЕНСТРУТ Кай (DE),СЭНДХУ Харприт К. (US),ШАХ Навнит Харговиндас (US)
申请号:
RU2013108056/15
公开号:
RU2013108056A
申请日:
2011.08.08
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A pharmaceutical composition in the form of multilayer pellets, comprising a) an inert core; b) a layer containing a compound of formula I: wherein one of A or E is N and the other C; R- is a halogen or cyano group; R- represents lower alkyl; R- represents aryl or heteroaryl, each of which is optionally substituted with one, two or three substituents selected from halogen, lower alkyl, lower alkoxy group, cycloalkyl, lower haloalkyl, lower haloalkoxy group, cyano group or NR'R '', or 1-morpholinyl, 1-pyr rolidinyl, which is optionally substituted by (CH) OR, piperidinyl, which is optionally substituted (CH) OR, 1,1-dioxo-thiomorpholinyl, piperazinyl, which is optionally substituted by lower alkyl or a group (CH) -cycloalkyl; R is hydrogen, lower alkyl or (CH) -cycloalkyl; R 'and R' 'are independently selected from hydrogen, lower alkyl, (CH) -cycloalkyl or (CH) OR; m = 0 or 1; n = 1 or 2; and R is CHF, CF, C (O) H or CHR, where R is hydrogen, OH, C-C-alkyl or C-C-cycloalkyl; and its pharmaceutically acceptable salts; c) a release control layer containing a polymer that controls speed, and d) a layer containing a pH-dependent polymer. 2. A composition according to claim 1, comprising: a) an inert core; b) a layer containing a compound of formula I; c) optionally a separation layer; d) a release control layer containing a speed controlling polymer; e) a pH dependent layer polymer; and f) possibly a layer containing a non-thermoplastic polymer. 3. The composition according to claim 1, characterized in that the inert core is selected from the group consisting of: sugar balls, microcrystalline cellulose granules and starch granules. Composition1. Фармацевтическая композиция в форме многослойных пеллет, включающаяa) инертное ядро;b) слой, содержащий соединение формулы I:,где один из А или Е представляет собой N, а другой С;R- представляет собой галоген или циано-группу;R- представляет собой низший алкил;R- представляет собой арил или гетероарил, каждый из которых возмо
来源网站:
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