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Piperazine derivatives which bind to 5-HT1A serotonergic receptors - used to treat neuromuscular dysfunctions of lower urinary tract

机译:与5-HT1A血清素能受体结合的哌嗪衍生物-用于治疗下尿路的神经肌肉功能障碍

摘要

Piperazine derivatives of formula (I) and their salts and N-oxides and active metabolites are used for the treatment of neuromuscular dysfunction of the lower urinary tract. n = 1 or 2; Het = monocyclic heteroaryl; R = cycloalkyl or monocyclic heteroaryl; R3 = H or lower alkyl; Z = a bond, CH2, CH2CH2, CH2C(O), CH2CH(OH), O, OCH2,or CO; B' = optionally substituted aryl or heteroaryl; R1 = H, halo, alkoxy, NO2, NH2, acylamino or alkylsulphonylamino and R2 = halo, alkoxy, polyfluoroalkoxy, CN or carbamoyl. (I) are new provided that when Z = a bond, B' = a substituted phenyl of formula (a); and if R1 is not acylamino or alkylsulphonylamino, then R2 = polyfluoroalkoxy. 14 Compounds (I) are specifically claimed e.g: 1-[N-cyclohexylcarbonyl-N-(2-pyridyl)-2-aminoethyl]-4-(2-trifluoromethoxyphenyl)-piperazine.
机译:式(I)的哌嗪衍生物及其盐和N-氧化物以及活性代谢物用于治疗下尿路的神经肌肉功能障碍。 n = 1或2; Het =单环杂芳基; R =环烷基或单环杂芳基; R3 = H或低级烷基; Z =键,CH2,CH2CH2,CH2C(O),CH2CH(OH),O,OCH2或CO; B'=任选取代的芳基或杂芳基; R 1 = H,卤素,烷氧基,NO 2,NH 2,酰基氨基或烷基磺酰基氨基,R 2 =卤素,烷氧基,多氟烷氧基,CN或氨基甲酰基。 (I)是新的,条件是当Z =键时,B′=式(a)的取代苯基;如果R1不是酰基氨基或烷基磺酰基氨基,则R2 =多氟烷氧基。 14.具体要求保护的化合物(I),例如:1- [N-环己基羰基-N-(2-吡啶基)-2-氨基乙基] -4-(2-三氟甲氧基苯基)-哌嗪。

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