发明名称 Bicyclic benzamides of 3-or 4-substituted 4-(aminomethyl)-piperidine derivatives
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 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals 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 ring-system; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, 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 conditions which are related to impairment of gastric emptying.
申请公布号 USRE40793(E1) 申请公布日期 2009.06.23
申请号 US20050259719 申请日期 2005.10.26
申请人 JANSSEN PHARMACEUTICA, N.V. 发明人 BOSMANS JEAN-PAUL RENE MARIE ANDRE;DECLEYN MICHEL ANNA JOZEF;SURKYN MICHEL
分类号 A61K31/495;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;C07D211/06;C07D211/42;C07D211/44;C07D237/28;C07D401/00;C07D401/06;C07D405/06;C07D405/12;C07D405/14;C07D417/14;C07D513/04 主分类号 A61K31/495
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