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Pharmaceutical compositions of metabotropic glutamate receptor 5 antagonists (mglu5)
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
CHATTERJI ASHISH,HUANG JINGJUN,KOENNINGS STEPHANIE,LINDENSTRUTH KAI,SANDHU HARPREET K.,SHAH NAVNIT HARGOVINDAS
申请号:
ARP110102884
公开号:
AR082602A1
申请日:
2011.08.09
申请国别(地区):
AR
年份:
2012
代理人:
摘要:
Antagonistic synthesis of glutamate 5 metabolite receptor (mGlu5) or pharmaceutically acceptable salt. The compounds contain therapeutically active compounds as well as nonionic polymers, ionic polymers, polymers and fillers, whether matrix pellet,Matrix plate or ball cladding. These components provide a free and ldqoe, in vitro and rdqoe profile; unlike pH, 70% NMT in 1 hour, 85% NMT in 4 hours and 80% NLT in 8 hours. Compounds contribute to the treatment of IPCC disorders, such as therapeutic depression (TRD) and fragile X. require syndrome: one drug ingredient contains a formula compound (1), in which a or E is n and another C; R1 is halogen or cyanogen; R2 is lower tar; R3 is arilo or heterosexual, each of which can be replaced by an alternative,Two to three alternatives are selected from halogen, low tar, low oxygen, epoxy, low halogen, low halogen, low halogen, cyanogen and NR rsqoe; R rsqoe; rsqoe;,or by 1-morpholinyl, 1-pyrrolidinyl, optionally substituted by (CH2) mOR, piperidinyl, optionally substituted by (CH2) mOR, 1,1-dioxo-thiomorpholinyl or piperazinyl, optionally substituted by lower alkyl or (CH2) m-cycloalkyl ; R is hydrogen, lower alkyl or (CH2) m-cycloalkyl; R and R are independently hydrogen, lower alkyl, (CH2) m-cycloalkyl or (CH2) nOR; m is the number 0 or 1; n is the number 1 or 2; and R4 is CHF2, CF3, C (O) H or CH2R5, wherein R5 is hydrogen, OH, C1-6 alkyl or C3-12 cycloalkyl; and its pharmaceutically acceptable salts,Requirements 15: the composition on one of the requirements of 1-11 and 14, which is 2-Chloro-4 - [1 - (4-fluoro-phenyl) - 2, 5-dimethyl-1h-imidazol-4-iletinil] - piridina Claim 26: the speed controlling polymer is selected from a group consisting of polyethylene, hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, vinyl acetate copolymer / crotonico, acrylic acid (MET) acrylic acid.(vinyl acetate)Ethylene cellulose, acetic anhydride / methyl ether and ethylene copolymer, polyvinyl chloride copolymer an
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