发明名称 GASTROKINETIC MONOCYCLIC BENZAMIDES OF 3- OR 4-SUBSTITUTED 4-(AMINOMETHYL)-PIPERIDINE DERIVATIVES
摘要 <p>The present invention of compounds of formula (I), a stereochemically isomer ic form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2- 6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkynyl, or L is a radical of formula -A1-R6-, A1-X-R7, -A1-Y-C(=O)-R9, or -A1-Y-C(-O)-NR11R12 wherein each A1 is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3- 6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ring system; R7 is hydrogen, C1-6alkyl, hydroxy C1-6alkyl, C3-6cycloalkyl, or a heterocyclic ring system; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; 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 conditionswhich are related to impairment of gastric emptying.</p>
申请公布号 CA2295087(C) 申请公布日期 2007.05.15
申请号 CA19982295087 申请日期 1998.07.07
申请人 JANSSEN PHARMACEUTICA, N.V. 发明人 BOSMANS, JEAN-PAUL RENE MARIE ANDRE;DE CLEYN, MICHAEL ANNA JOZEF;SURKYN, MICHAEL
分类号 C07D211/42;A61K31/4427;A61K31/443;A61K31/445;A61K31/4523;A61K31/4525;A61K31/453;A61K31/454;A61K31/4545;A61K31/497;A61K31/501;A61K31/502;A61P1/00;A61P1/10;A61P1/14;A61P43/00;C07C229/60;C07D211/44;C07D401/06;C07D405/06;C07D405/12;C07D405/14;C07D417/14;C07D513/04 主分类号 C07D211/42
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