NOVEL N-SUBSTITUTED 4-((4'-AMINOBENZOYL)-OXYMETHYL)-PIPERIDINES HAVING GASTRIC PROKINETIC PROPERTIES

摘要

This invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R<1> is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyloxy; R<2> is hydrogen or C1-6alkyloxy, or when taken together R<1> and R<2> may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R<3> is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R<4>, -Alk-NR<5>R<6>, 1-R<6>-4-piperidinyl, Alk-X-R<7>, -Alk-Y-C(=O)-R<9> or -Alk-Y-C(=O)-NR<11>R<12>, wherein each Alk is C1-12alkanediyl; R<4> is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar-, di(Ar)methyl, Ar-oxy- or Het<1>; R<5> is hydrogen or C1-6alkyl; R<6> is Het<2>; R<7> is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl or Ar or Het<2>; X is O, S, SO2 or NR<8>; said R<8> being hydrogen, C1-6alkyl or Ar; R<9> is hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar, ArC1-6alkyl, di(Ar)methyl, C1-6alkyloxy or hydroxy; Y is NR<10> or a direct bond; said R<10> being hydrogen, C1-6alkyl or Ar; R<11> and R<12> each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar or ArC1-6alkyl, or R<11> and R<12> combined with the nitrogen atom bearing R<11> and R<12> may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R<11> and R<12> combined with the nitrogen bearing R<11> and R<12> 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.