发明名称 4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders
摘要 The present invention of compounds of formula (I)a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, -R1-R2- is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula -Alk-R6-, Alk-X-R7, -Alk-Y-C(=O)-R9, or -Alk-Y-C(=O)-NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond or NR10; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating or preventing gastrointestinal disorders.
申请公布号 US6544997(B1) 申请公布日期 2003.04.08
申请号 US20010857905 申请日期 2001.06.08
申请人 JANSSEN PHARMACEUTICA, N.V. 发明人 BOSMANS JEAN-PAUL RENE MARIE ANDRE;MEULEMANS ANN LOUISE GABRIELLE;DE CLEYN MICHEL ANNA JOZEF;GIJSEN HENRICUS JACOBUS MARIA
分类号 A61K31/4523;A61K31/4525;A61K31/453;A61K31/454;A61K31/519;A61P1/04;A61P1/08;A61P1/10;A61P1/14;C07D405/12;C07D405/14;C07D417/14;C07D513/04;(IPC1-7):C07D405/12;A61K31/445;A61P1/100 主分类号 A61K31/4523
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