发明名称 ESTERS OF 3-HYDROXY-PIPERIDINEMETHANOL 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 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may 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; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R5- Alk-X-R6, -Alk-Y-C(=O)-R8, or -Alk-Y-C(=O)-NR10R11 wherein each Alk is C1-12alkanediyl ; and R5 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R6 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3- 6cycloalkyl, aryl or heterocyclic ringsystem; X is O, S, SO2 or NR7; said R7 being hydrogen, C1-6alkyl or aryl; R8 is hydrogen, C1-6alkyl, C3-6cycloalkyl, aryl, arylC1-6alkyl, di(aryl)methyl, C1-6alkyloxy or hydroxy ; Y is NR9 or a direct bond; said R9 being hydrogen, C1-6alkyl or aryl; R10 and R11 each independently are hydrogen, C1-6alkyl, C3- 6cycloalkyl, aryl or arylC1-6alkyl, or R10 and R11 combined with the nitrogen atom bearing R10 and R11 may form a pyrrolidinyl or piperidinyl rin g both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R10 and R11 combined with the nitrogen bearing R10 and R11 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl. 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 CA2235133(C) 申请公布日期 2006.04.04
申请号 CA19972235133 申请日期 1997.02.07
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 DECLEYN, MICHEL ANNA JOZEF;LOVE, CHRISTOPHER JOHN;BOSMANS, JEAN-PAUL RENE MARIE;D'HAEN, HENRI ELISABETH FRANS
分类号 C07D513/04;A61K31/445;A61K31/495;A61K31/535;C07D211/42;C07D401/06;C07D401/12;C07D405/06;C07D405/12;C07D405/14 主分类号 C07D513/04
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