发明名称 AMINOSULFONYL SUBSTITUTED 4-(AMINOMETHYL)-PIPERIDINE BENZAMIDES AS AHT-ANTAGONISTS
摘要 The present invention is concerned with novel aminosulfonyl substituted 4-(aminonethyl) piperidine benzamides of formula (I)stereochemically isomeric forms thereof, an N-oxide form thereof, or a pharmaceutically acceptable acid or base addition salt thereof, wherein – R-R-is a bivalent radical of formula: -O-CH- CH-O-or - O- CH- CH- CH-;Ris hydrogen, halo, Calkyl or Calkyloxy ;Ris hydrogen, halo, Calkyl; cyano, amino or mono or di (Calkyl)amino ;Ris hydrogen or Calkyl, and the –ORradical is situated at the 3-or 4-position of the piperidine moiety;L is a radical of formula- Alk-R, -Alk-C(=O)-NH-SO-R, -Alk-SO-NH-SO-R, wherein each Alk is Calkanediyl ;and Ris aminosulfonyl optionally substituted with Calkyl or phenyl;and Ris Calkyl or phenyl.The compounds of formula (I) having 5HT-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine for the treatment of gastrointestinal diseases.
申请公布号 EA009259(B1) 申请公布日期 2007.12.28
申请号 EA20060000060 申请日期 2004.06.10
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 BOSMANS JEAN-PAUL, RENE, MARIE, ANDRE;GIJSEN HENRICUS, JACOBUS, MARIA;MEVELLEC LAURENCE, ANNE
分类号 C07D405/12;A61K31/445;A61P1/00 主分类号 C07D405/12
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