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compounds for the treatment of impaired fundischen relaxation

机译:用于治疗基底膜松弛的化合物

摘要

The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -aSUP1/SUP=aSUP2/SUP-aSUP3/SUP=aSUP4/SUP- is a bivalent radical wherein one or two of aSUP1 /SUPto aSUP4 /SUPare nitrogen and the remaining aSUP1 /SUPto aSUP4 /SUPare -CH-; -ZSUP1/SUP-ZSUP2/SUP- is a bivalent radical; -A- is a bivalent radical of formula -N(RSUP6/SUP)-AlkSUP2/SUP- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; RSUP1/SUP, RSUP2 /SUPand RSUP3 /SUPare each independently selected from hydrogen, CSUB1-6/SUBalkyl, hydroxy, halo and the like; AlkSUP1 /SUPand AlkSUP2 /SUPare optionally substituted CSUB1-6/SUBalkanediyl; RSUP5 /SUPis a radical of formula wherein n is 1 or 2; pSUP1 /SUPis 0, and pSUP2 /SUPis 1 or 2; or pSUP1 /SUPis 1 or 2, and pSUP2 /SUPis 0; X is oxygen, sulfur or -NRSUP9/SUP; YSUP2 /SUPis oxygen or sulfur; RSUP7 /SUPis hydrogen, CSUB1-6/SUBalkyl, CSUB3-6/SUBcycloalkyl, phenyl or phenylmethyl; RSUP8 /SUPis CSUB1-6/SUBalkyl, CSUB3-6/SUBcycloalkyl phenyl or phenylmethyl; RSUP9 /SUPis cyano, CSUB1-6/SUBalkyl, CSUB3-6/SUBcycloalkyl, CSUB1-6/SUBalkyloxycarbonyl or aminocarbonyl; RSUP10 /SUPis hydrogen or CSUB1-6/SUBalkyl; 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 disturbed fundic accomodation.
机译:本发明涉及式(I)的化合物的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 到a 4 是氮,其余的 1 至a 4 是-CH-; -Z 1 -Z 2 -是二价基团; -A-是式-N(R 6 )-Alk 2 -或含有一个或两个氮原子的5、6或7元饱和杂环的二价基团; R 1 ,R 2 和R 3 分别独立地选自氢,C 1-6 烷基,羟基,光环之类; Alk 1 和Alk 2 是可选取代的C 1-6 烷二基; R 5 是下式的基团,其中n是1或2; p 1 为0,p 2 为1或2;或p 1 为1或2,而p 2 为0; X是氧,硫或-NR 9 ; Y 2 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以及它们作为药物的用途,特别是用于治疗与不适的基础适应症有关的病症。

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