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 ring 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 MX9803601(A) 申请公布日期 1998.09.30
申请号 MX19980003601 申请日期 1998.05.06
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 JEAN-PAUL R. M. A. BOSMANS;CHRISTOPHER J. LOVE;MICHEL A. J. DECLEYN;HENRI E. F. D'HAEN
分类号 A61K31/445;C07D211/42;C07D401/06;C07D401/12;C07D405/06;C07D405/12;C07D405/14;C07D513/04;(IPC1-7):C07D211/42 主分类号 A61K31/445
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