| abstract |
1. A gastrokinetic 3- or 4-substituted 4- (aminomethyl) piperazine bicyclic benzamide of formula (H wherein R 1 and R 2 taken together represent a bivalent radical of the formula -O-CH 2 -O- (a-1), -O -CH 2 -CH 2 - (a-2), -O-CH2 -CH2 -O- (a-3), -OC H 2 -CH 2 -CH 2 - (a-4), -O-CH2 - CH 2 -CH 2 -O- (a-5), where in these divalent radicals one or two hydrogen atoms can be replaced by C 1-6 -alkyl. R 3 is halogen; R 4 is hydrogen or C 1 - 6-alkyl, R5 is a hydrogen atom; L is a radical of the formula -Alk-R6 (b-1), -Alk-X-R7 (b-2), -Alk-YC (= O) -R9 (b- 3), or -Alk-YC (= O) -NR11R12 (b-4) where each Alk is C1-1 2-alkylene. 1 R6 is hydrogen, hydroxy, cyano, C1-6 -alkylsulfonylamino, C3-6 -cycloalkyl or Het1, R7 is hydrogen, C1-6-alkyl, hydroxyC1-6-alkyl or Het2; X is O or NH; R9 is C1-6-alkyl Y is NR12 or a direct bond, wherein R is C1-6alkyl; R 1 1 and R 1 2 linked to the nitrogen atom to which they are attached may form a pyrrolidinyl ring, Het1 and Het2 are independently selected from the group consisting of tetrahydrofuran; C1-6alkyl substituted tetrahydrofuran; dioxolane; C1-6alkyl substituted dioxolane; dioxane, C 1-6 alkyl substituted dioxane, tetrahydropyran; C1-6 alkyl substituted tetrahydropyran; pyridazinyl, pyridazinyl substituted with C1-6-akyl; pyrazinyl; pyrazinyl substituted with one or two substituents, each substituent selected from the group consisting of halogen, hydroxy, C1-6alkyl; Het 1 may also be a radical of formula (c-1) (c 3) (c-4) wherein R 1 3 is C 1-4 alkyl, a stereochemically isomeric form or a pharmaceutically acceptable acid addition salt or base thereof. PL PL PL |