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Compounds for impaired gastric fundus relaxation treatment

机译:胃底松弛疗法受损的化合物

摘要

"COMPOSITIONS FOR HARMFUL RELAXATION TREATMENT OF THE GASTRIC BACKGROUND". The present invention relates to compounds of formula (I), a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a ^ 1 ^ = a ^ 2 ^ -a ^ 3 ^ = a ^ 4 ^ - is a bivalent radical wherein one or two of a ^ 1 ^ aa ^ 4 ^ are nitrogen and the remainder of a ^ 1 ^ aa ^ 4 ^ are -CH =; -Z ^ 1 ^ -Z ^ 2 ^ - is a bivalent radical; A is a bivalent radical of the formula -N (R 6 6) - Alk 2 2 - and a 5-, 6- or 7-membered saturated heterocycle containing one or two nitrogen atoms; R 1, R 2 and R 3 are each independently selected from hydrogen, C 1-6 alkyl, hydroxy, halo and the like; Alk4-1 and Alk2-2 are optionally substituted C1-6 alkanediyl; R 5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p ^ 1 ^ is 0 and p ^ 2 ^ is 1 or 2, or p ^ 1 ^ i 1 or p ^ 2 ^ is 0; X is oxygen, sulfur or = NR 9 9; Y ^ 2 ^ is oxygen or sulfur; R 7 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 18 is C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 9 is cyano, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxycarbonyl or aminocarbonyl; R 10 is hydrogen or C 1-6 alkyl; and Q is a bivalent radical. Processes for preparing the products, formulations comprising these products and their use as a medicament are described, in particular for treating conditions that are related to disturbed accommodation of the gastric fundus.
机译:“用于胃背景的严格松弛治疗的组合物”。本发明涉及式(I)的化合物,其立体化学异构体形式,其N-氧化物形式或其药学上可接受的酸加成盐,其中-a ^ 1 ^ = a ^ 2 ^ -a ^ 3 ^ = a ^ 4 ^-是二价基团,其中a ^ 1 ^ aa ^ 4 ^中的一个或两个为氮,其余^ 1 ^ aa ^ 4 ^为-CH =; -Z ^ 1 ^ -Z ^ 2 ^-是二价基团; A为式-N(R 6 6)-Alk 2 2-和含有一个或两个氮原子的5元,6元或7元饱和杂环的二价基团; R 1,R 2和R 3各自独立地选自氢,C 1-6烷基,羟基,卤素等。 Alk4-1和Alk2-2是任选取代的C 1-6烷二基; R 5为式(d-1),(d-2),(d-3),(d-4),(d-5)的基团,其中n为1或2; p ^ 1 ^为0,p ^ 2 ^为1或2,或者p ^ 1 ^ i 1或p ^ 2 ^为0; X是氧,硫或= NR 9 9; Y ^ 2 ^是氧或硫; R 7为氢,C 1-6烷基,C 3-6环烷基,苯基或苯甲基; R 18为C 1-6烷基,C 3-6环烷基,苯基或苯甲基; R 9为氰基,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为氢或C 1-6烷基; Q是二价基团。描述了制备产物的方法,包含这些产物的制剂以及它们作为药物的用途,特别是用于治疗与胃底适应性障碍有关的病症。

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