发明名称 GASTROKINETIC BICYCLIC BENZAMIDES OF 3- OR 4-SUBSTITUTED 4-(AMINOMETHYL)-PIPERIDINE DERIVATES
摘要 <p>The present invention of compounds of formula (I), a stercochemically isomer ic form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radical one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, 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, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, 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 or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 ea ch independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substitut ed pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as amedicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.</p>
申请公布号 CA2295088(C) 申请公布日期 2007.10.23
申请号 CA19982295088 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, MICHEL ANNA JOZEF;SURKYN, MICHEL
分类号 C07D405/12;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;A61P1/12;A61P1/14;A61P43/00;C07C229/60;C07D211/40;C07D211/42;C07D211/44;C07D401/06;C07D405/06;C07D405/14;C07D417/14;C07D513/04 主分类号 C07D405/12
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