发明名称 Heteroaryl substituted derivatives of 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one, process and intermediates for their preparation and pharmaceutical preparations containing thereof
摘要 In the present invention there are disclosed 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one heteroaryl substituted derivatives of the general formula I, in which A and B together represent a bivalent radical of the general formula -N=CH- (a), -CH=N- (b), -CHi2-CHi2- (c), -CH=CH- (d), -C(=O)-CHi2- (e) or -CHi2-C(=O)- (f), whereby in the bivalent radical of the formula (a) or (b) the hydrogen atom can be optionally substituted with an alkyl group containing 1 to 6 carbon atoms and in the bivalent radical of the formulas (c), (d), (e) or (f) one or two hydrogen atoms can be optionally substituted with alkyl groups containing 1 to 6 carbon atoms, Re1 represents a hydrogen atom, an alkyl group containing 1 to 6 carbon atoms or a halogen, Re2 represents a hydrogen atom or a halogen atom, Re3 represents a hydrogen atom, an alkyl group containing 1 to 8 carbon atoms, a cycloalkyl group containing 3 to 6 carbon atoms or an alkyl group containing 1 to 8 carbon atoms being substituted with hydroxyl, an oxo group a cycloalkyl containing 3 to 6 carbon atoms or an aryl group, Het represents a heterocyclic radical being defined in the Claims and the aryl group is represented by phenyl being optionally substituted with alkyl containing 1 to 6 carbon atoms or with a halogen, further their N-oxides, stereochemically isomeric forms and pharmaceutically acceptable acid addition salts, intermediates of the general formula III in which Re1, Re2 and Het are as specified above and W represents a leaving group such as halogen or sulfonyloxy and their acid addition salts or stereochemically isomeric forms, further process for preparing the compounds of the general formula I as well as pharmaceutical preparations based thereon. The compounds of the general formula are suitable for treating hyperlipemia.
申请公布号 CZ286476(B6) 申请公布日期 2000.04.12
申请号 CZ19970001198 申请日期 1995.10.19
申请人 JANSSEN PHARMACEUTICA N. V. 发明人 HEERES JAN;BACKX LEO JACOBUS JOZEF;HENDRICKX ROBERT JOZEF MARIA;VAN DER EYCKEN LUC ALFONS LEO;DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L
分类号 C07D405/12;A61K31/41;A61K31/495;A61P3/06;A61P9/12;C07D405/14;C07D413/14;C07D417/14;(IPC1-7):C07D405/14;A61P1/00 主分类号 C07D405/12
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