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NEW DIHYDRO- OXAZOLOBENZODIAZ EPINONE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
专利权人:
发明人:
申请号:
IN550/DEL/2012
公开号:
IN292522B
申请日:
2012.02.28
申请国别(地区):
IN
年份:
2018
代理人:
摘要:

Dihydro-oxazolobenzodiazepinone derivatives (I) are new. Dihydro-oxazolobenzodiazepinone derivatives of formula (I) and their positional isomers, enantiomers, diastereoisomers or addition salts with acids, solvates, complexes or adducts, are new. R1 : H or 1-4C alkyl R2 : 1-4C alkyl and R3 : (hetero)aryl. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Neuroleptic Antidepressant Neuroprotective Nootropic Antiparkinsonian Anticonvulsant Tranquilizer Vulnerary Cerebroprotective. MECHANISM OF ACTION : gamma -Aminobutyric acid (GABA) receptor agonist. The GABA receptor agonistic activity of (I) was tested in human embryonic kidney (HEK-293) cells. The result showed that 5-(6-fluoro-1-benzothien-2-yl)-8-methyl-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one exhibited an IC 5 0value of 100 nM.

[EP2497774A1]
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