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Heterocyklylamidsubstituerte imidazoler
专利权人:
AiCuris GmbH & Co KG
发明人:
Kern, Armin,Radtke, Martin,Hendrix, Martin,Rosentreter, Ulrich,Lang, Dieter,Zimmermann, Holger,Brueckner, David,Henninger, Keistin,Keldenich, Joerg,Paulsen, Daniela
申请号:
NO20074780
公开号:
NO338997B1
申请日:
2007.09.19
申请国别(地区):
NO
年份:
2016
代理人:
摘要:
Heterocyclylamide-substituted imidazole compound (I) or its salt, or solvate or its salt, is new. Heterocyclylamide-substituted imidazole compound of formula (I) or its salt, or solvate or its salt is new. R 1>piperazine compound of formula (II) or diazepane compounds of formula (III) asterisk : attachment at carbonyl group T : halo, hydroxy, oxo, NO 2, CN, CF 3, CHF 2, CF 3O, CHF 2O, monofluoromethoxy, trifluoromethoxy, 1-6C alkyl, 1-6C (alkoxy) carbonyl, hydroxy carbonyl, amino, 1-6C alkylamino (carbonyl) or aminocarbonyl R 4>, R 5>phenyl or 5-6 membered heteroaryl (optionally substituted with 1-3 substituents of T) R 6>, R 7>H, CH 3 or C 2H 5 R 2>1-6C alkyl optionally substituted by 3-6C cycloalkyl, 6-10C aryl or 5-6 membered heteroaryl (all optionally substituted with T) and R 3>phenyl substituted with 1-3 substituents of halo, hydroxy, CF 3, CHF 2, CF 3O, CHF 2O, monofluoromethoxy, trifluoromethoxy, trifluoromethyl thio, 1-6C alkyl or 1-6C alkoxy. Independent claims are included for: (1) the preparation of (I) and (2) a medicament comprising (I) in combination with at least an inert and not-toxic auxiliary material. [Image] ACTIVITY : Virucide. The ability of (I) to treat human cytomegalic virus cytopathogene was tested in human skin fibroblast. The results that N-(1-methyl-2-{[4-(5-methylpyridin-2-yl)piperazin-1-yl]carbonyl}-1H-imidazol-4-yl)-N-[4-(trifluoromethoxy)phenyl] urea exhibited an EC 50 value of 0.75 nM. MECHANISM OF ACTION : None given.
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