发明名称 THIA(DIA)ZOLES AS QUICK-DISSOCIATING ANTAGONISTS OF DOPAMINE 2 RECEPTOR
摘要 FIELD: biotechnologies.SUBSTANCE: invention relates to derivatives of [1-(benzyl)piperydine-4-yl]-([1,3,4]thiadiazole- 2-yl)amine and [1-(benzyl)piperydine-4-yl]-(thiazole-2-yl)amine of the formula (I) or their pharmaceutically acceptable salts, or their pharmaceutically acceptable salts, where R means hydrogen; Rmeans phenyl, substituted with 1, 2 or 3 substitutes, each of them is independently selected from a group containing halogen, cyano, Calkyl, perfluoroCalkyl and perfluoroCalkoxy; Rmeans hydrogen or Calkyl; Rmeans hydrogen, trifluoromethyl or cyano; X means N or CR, where Ris trifluoromethyl. Also the invention relates to a pharmaceutical composition containing compounds of the formulaas an active ingredient. The following derivatives are presented: derivatives of [1-(benzyl)piperydine-4-yl]-([1,3,4]thiadiazole-2-yl)amine and [1-(benzyl)piperydine-4-yl]-(thiazole-2-yl)amine of the formula (I) representing quick-dissociating antagonists of dopamine 2 receptors and used as medicinal agents for treatment or prevention of central nervous system.EFFECT: improved properties of compounds.7 cl, 22 ex
申请公布号 RU2489431(C2) 申请公布日期 2013.08.10
申请号 RU20090142981 申请日期 2008.04.18
申请人 JANSSEN FARMATSEVTIKA N.V. 发明人 MAKDONAL'D GREGOR DZHEJMS;BARTOLOME-NEBREDA KHOSE MANUEHL';VAN GOL MIKHIL' LJUK MARIJA
分类号 C07D417/12;A61K31/454;A61P25/18;C07D277/42;C07D285/12 主分类号 C07D417/12
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