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(BENZODIOXAN, BENZOFURAN OR BENZOPYRAN) DERIVATIVES HAVING FUNDIC RELAXATION PROPERTIES

机译:(苯并二恶英,苯并呋喃或苯并吡喃)具有基团松弛特性的衍生物

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, wherein Alk.sup. 1 is C.sub.1-6 alkanediyl optionally substituted with hydroxy, C.sub.1-4 alkyloxy or C. sub.1-4 alkylcarbonyloxy; --Z.sup.1 --Z.sup.2 -- is a bivalent radical; R. sup.1, R.sup.2 and R.sup.3 are each independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, halo and the like; or when R.sup.1 and R.sup.2 are on adjacent carbon atoms, R.sup.1 and R.sup. 2 taken together may form a bivalent radical; R.sup.4 is hydrogen or C. sub.1-6 alkyl; A is a bivalent radical of formula --NR.sup.6 --Alk.sup.2 - - (b-1), or -- Npiperidinyl--(CH.sub.2).sub.m (b-2) wherein m is 0 or 1; R.sup.5 is a radical of formula ##STR1## wherein n is 1 or 2; p.sup.1 is 0, and p.sup. 2 is 1 or 2; or p.sup.1 is 1 or 2, and p.sup.2 is 0; X is oxygen, sulfur or NR.sup.9 ; Y is oxygen or sulfur; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl or phenylmethyl; R.sup.8 is C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl phenyl or phenylmethyl; R.sup.9 is cyano, C. sub.1-6 alkyl, C.sub.3-6 cyclo-alkyl, C.sub.1-6 alkyloxycarbonyl or aminocarbonyl; R.sup.10 is hydrogen or C.sub.1-6 alkyl; and Q is a bivalent radical. 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 impaired fundic relaxation.
机译:式(I)化合物的本发明是其立体化学异构形式,其N-氧化物形式或其药学上可接受的酸加成盐,其中Alkup。 1是任选被羟基,C 1-4烷氧基或C 1-4烷基羰氧基取代的C 1-6烷二基; --Z.supl --Z.sup.2-是二价基团; R.sup.1,R.sup.2和R.sup.3各自独立地选自氢,C 1-6烷基,羟基,卤素等。或当R 1和R 2在相邻的碳原子上时,R 1和R 2。 2一起可以形成一个二价基团; R 4是氢或C 1-6烷基; A是式--NR 6-烷基2--(b-1)或-N-哌啶基-(CH 2)m(b-2 ),其中m是0或1; R 5为式## STR1 ##的基团,其中n为1或2; p.sup.1为0,p.sup。 2是1或2;或p.sup.1为1或2,而p.sup.2为0; X为氧,硫或NR 9; Y是氧或硫; R 7是氢,C 1-6烷基,C 3-6环烷基,苯基或苯甲基; R 8是C 1-6烷基,C 3-6环烷基苯基或苯甲基; R 9是氰基,C 1-6烷基,C 3-6环烷基,C 1-6烷氧羰基或氨基羰基; R 10是氢或C 1-6烷基; Q是二价基团。公开了制备所述产品的方法,包含所述产品的制剂及其作为药物的用途,特别是用于治疗与基础松弛相关的病症。

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