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Novel 1- 1- (hetero) aryl-1-perhydroxyalkylmethyl -piperazine Compounds, Methods for Making the Same, and Drugs Containing the Compounds

机译:新型1- [1-(1-杂)芳基-1-过羟基烷基甲基]-哌嗪化合物,其制备方法和含有该化合物的药物

摘要

1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives (I) are new. Also new are 1-unsubstituted analog intermediates (II). 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives of formula (I) and their acid addition salts are new. A = naphthyl, phenyl (optionally substituted by OH), mono- or bi-cyclic heteroaryl or 3-6C alkenyl (optionally substituted by phenyl); Q = (CHOR1)k-(CHOR2)l-(CHOR3)m-(CHOR4)n-CH2OR5 ; R1-R5 = H or lower alkanoyl, or two of R1-R5 = CO, CS or CH2 (optionally substituted by lower alkyl or 4-5C alkylene), completing a 5- or 6-membered ring; k, l, m, n = 0 or 1, and R6, R7 = H or halo. Independent claims are also included for: (1) the preparation of (I), and (2) new piperazine derivative intermediates of formula (II).
机译:1-(1-(杂)芳基)-1-(聚羟基烷基)-甲基-4-(4-(N-甲基苯甲酰胺)-3-苯基丁基)-哌嗪衍生物(I)是新的。 1-未被取代的类似物中间体(II)也是新的。式(I)的1-(1-(杂)芳基)-1-(聚羟基烷基)-甲基)-4-(4-(N-甲基苯甲酰胺邻)-3-苯基丁基)-哌嗪衍生物及其酸加成盐是新。 A =萘基,苯基(可选被OH取代),单环或双环杂芳基或3-6C烯基(可选被苯基取代); Q =(CHOR1)k-(CHOR2)1-(CHOR3)m-(CHOR4)n-CH2OR5; R1-R5 = H或低级烷酰基,或R1-R5 = CO,CS或CH2中的两个(任选被低级烷基或4-5C亚烷基取代),形成5或6元环; k,l,m,n = 0或1,R6,R7 = H或卤素。还包括以下方面的独立权利要求:(1)制备(I),和(2)新的式(II)的哌嗪衍生物中间体。

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