发明名称 CINNAMIC ACID NITRILE METHOD OF PRODUCTION AND USE THEREOF
摘要 The invention relates to substituted cinnamic acid nitriles of the formula (I) wherein X = CN, COOR<4>, CONR<5>R<6>, COaryl, COalkyl, aryl, heteroaryl, R<1> = H, alkyl, arylalkyl, [4-(2-alkoxyphenyl)-1-piperazinyl]alkyl, R<2> and R<3> = independent of each other H, hydroxy, alkoxy, benzyl, R<4> = H, alkyl, [4-(2-alkoxyphenyl)-1-piperazinyl]alkyl, R<5> = H, alkyl, alkoxyalkyl, alkoxy-oxoalkyl, diakylaminoalkyl, amino-oxoalkyl, aryl, arylalkyl, [4-(2-alkoxyphenyl)-1-piperazinyl]alkyl, morpholinoalkyl, furanyalkyl, thienylalkyl, R<6> = H, alkyl, or NR<5>R<6> together = cyclic amines such as pyrrolidine, morpholine, piperidine, subst. piperazine, whereby at least one of the radicals R<1>, R<4> or R<5> is a [4-(2-alkoxyphenyl)-1-piperazinyl]alkyl-radical, in addition to the addition thereof with pharmacologically compatible acids. The compounds are active as prophylactic and therapeutic medicaments for the treatment of benign prostatahyperplasia. A method for the production of cinnamic acid nitrile is also disclosed; an appropriately substituted benzaldehyde is reacted with a substituted acetonitrile in a Knoevenagel-condensation reaction.
申请公布号 WO0116124(A1) 申请公布日期 2001.03.08
申请号 WO2000EP08419 申请日期 2000.08.29
申请人 DR. WILLMAR SCHWABE GMBH & CO.;HAUER, HERMANN;KOCH, EGON;CHATTERJEE, SHYAM, SUNDER 发明人 HAUER, HERMANN;KOCH, EGON;CHATTERJEE, SHYAM, SUNDER
分类号 C07D211/22;C07D211/62;C07D227/04;C07D295/088;C07D295/092;C07D295/13;C07D295/185 主分类号 C07D211/22
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