N-substituted 4-((-4'-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties

   
   

This invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-26 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl, R.sup.3 is hydrogen or halo; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula --Alk--R.sup.4, --Alk--NR.sup.5 R.sup.6, 1-R.sup.6 -4-piperidinyl, Alk--X--R.sup.7, --Alk--Y--C(.dbd.O)--R.sup.9, or --Alk--Y--C(.dbd.O)--NR.sup.11 R.sup.12 wherein each Alk is C.sub.1-12 alkanediyl; R.sup.4 is hydrogen, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, Ar--, di(Ar)methyl, Ar-oxy- or Het.sup.1 ; R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.6 is Het.sup.2 ; R.sup.7 is hydrogen, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, Ar or Het.sup.2 ; X is O, S, SO.sub.2 or NR.sup.8 ; said R.sup.8 being hydrogen, C.sub.1-6 alkyl or Ar; R.sup.9 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cyclo-alkyl, Ar, ArC.sub.1-6 alkyl, di(Ar)methyl, C.sub.1-6 alkyloxy or hydroxy; Y is NR.sup.10 or a direct bond; said R.sup.10 being hydrogen, C.sub.1-6 alkyl or Ar; R.sup.11 and R.sup.12 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, Ar or ArC.sub.1-6 alkyl, or R.sup.11 and R.sup.12 combined with the nitrogen atom bearing R.sup.11 and R.sup.12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C.sub.1-6 alkyl, amino or mono or di(C.sub.1-6 alkyl)amino, or said R.sup.11 and R.sup.12 combined with the nitrogen bearing R.sup.11 and R.sup.12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C.sub.1-6 alkyl. 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.

 
Web www.patentalert.com

< Integrated circuit configuration and method of fabricating a dram structure with buried bit lines or trench capacitors

< A/D conversion method and apparatus therefor

> Antidepressant indolealkyl derivatives of heterocycle-fused benzodioxan methylamines

> Method and system for generation of medical reports from data in a hierarchically-organized database

~ 00135