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GASTROKINETIC MONOCYCLIC BENZAMIDES OF 3- OR 4-SUBSTITUTED 4-(AMINOMETHYL)-PIPERIDINE DERIVATIVES

机译:3-或4-取代的4-(氨基甲酰基)-哌啶碱衍生物的胃肠动力学单环苯甲酰胺

摘要

The present invention of compounds of formula (I), a stereochemically isomericform thereof, an N-oxide form thereof or apharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkylC1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 ishydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone,C2-6alkynyl, or L is a radical of formula -A1-R6-, A1-X-R7, -A1-Y-C(=O)-R9, or-A1-Y-C(-O)-NR11R12 wherein each A1 isC1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ring system;R7 is hydrogen, C1-6alkyl, hydroxy C1-6alkyl, C3-6cycloalkyl, or aheterocyclic ring system; X is O, S, SO2 or NR8; said R8 being hydrogenor C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy orhydroxy; Y is NR10 or a direct bond; said R10 being hydrogen,or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atommay form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products,formulations comprising said products and their use as a medicine aredisclosed, in particular for treating conditions which are related toimpairment of gastric emptying.
机译:立体化学异构体式(I)的化合物的本发明其形式,N-氧化物形式或其药学上可接受的酸加成盐,R1为C1-6烷氧基,C2-6烯基氧基或C 2-6炔基氧基; R 2是氢,C 1-6烷基C 1-6烷氧基; R3是氢或卤素; R4是氢或C1-6烷基; R5是氢或C 1-6烷基; L为C3-6环烷基,C5-6环烷酮C 2-6炔基,或L为式-A1-R6-,A1-X-R7,-A1-Y-C(= O)-R9的基团,或-A1-Y-C(-O)-NR11R12,其中每个A1为C1-12烷二基; R6是氢,氰基,C1-6烷基磺酰基氨基,C3-6环烷基,C5-6环烷酮或杂环系统;R 7是氢,C 1-6烷基,羟基C 1-6烷基,C 3-6环烷基或杂环系统X为O,S,SO 2或NR 8;说R8是氢或C 1-6烷基; R 9是氢,C 1-6烷基,C 3-6环烷基,C 1-6烷氧基或羟基Y为NR10或直接键;说R10是氢,或C 1-6烷基; R11和R12各自独立地是氢,C1-6烷基,C3-6环烷基,或R11和R12与氮原子结合可以形成任选取代的吡咯烷基,哌啶基,哌嗪基或4-吗啉基环。制备所述产品的过程,包含所述产品的制剂及其作为药物的用途是公开的,特别是用于治疗与胃排空障碍。

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