首页> 外国专利> Bis- (piperazinyl or homopiperazinyl) -alkanes and acid addition salts thereof, process for their preparation, to pharmaceutical compositions containing the compounds, processes for preparing such compositions and the use of the compounds for the preparation of a pharmaceutical composition having anti-allergic and anti-inflammatory action

Bis- (piperazinyl or homopiperazinyl) -alkanes and acid addition salts thereof, process for their preparation, to pharmaceutical compositions containing the compounds, processes for preparing such compositions and the use of the compounds for the preparation of a pharmaceutical composition having anti-allergic and anti-inflammatory action

机译:双(哌嗪基或高哌嗪基)-烷烃及其酸加成盐,其制备方法,包含所述化合物的药物组合物,制备此类组合物的方法以及所述化合物在制备具有抗过敏和抗过敏作用的药物组合物中的用途抗炎作用

摘要

1. Bis-(piperazinyl- or homopiperazinyl) alkanes of the general formula I see diagramm : EP0122488,P21,F1 wherein R1 , R2 , R3 and R4 which may be identical to or different from each other, are each hydrogen, alkyl having 1 to 4 carbon atoms, hydroxyl, alkoxy having 1 to 4 carbon atoms, alkanoyloxy having up to 4 carbon atoms, halogen, trihalomethyl, di-C1-4 alkylamino, C1-4 alkoxycarbonyl, nitro, cyano or acyl having 1 to 3 carbon atoms ; R5 and R6 , which may be identical to or different from each other, are each hydrogen, methyl, hydroxyl, carboxyl, C1-4 alkoxycarbonyl, hydroxymethyl, phenyl or p-chlorophenyl, R7 and R8 are each hydrogen or methyl ; j and k are integers from 0 to 3, their sum being no more than 4 ; m and n are integers from 0 to 3, their sum being no more than 4 ; A is -CH2 - or -CH2 CH2 - ; or R5 and R7 together or R6 and R8 together are oxo, provided k or m is other than O ; or R5 and R7 together and R6 and R8 together are oxo, provided k or m are other than O ; R9 and R10 , which may be the same or different, represent hydrogen or from one to four methyl substituents on the carbon atoms of the piperazine ring (A = -CH2 -) ; R11 , R12 , R13 and R14 , which may be identical to or different from each other, are each hydrogen or methyl ; or R11 and R12 together and/or R13 and R14 together are oxo ; and X is alkylene of 1 to 2 carbon atoms, optionally hydroxy-substituted with the proviso that when A = -CH2 -, R1 to R14 are hydrogen and j, k, m and n are each zero, then X cannot be 1,2-ethylenediol, and physiologically acceptable acid addition salts thereof.
机译:1.通式I的双-(哌嗪基-或高哌嗪基)烷烃,见图:EP0122488,P21,F1其中R 1,R 2,R 3和R 4彼此相同或不同,分别为氢,具有1的烷基1-4个碳原子,羟基,具有1-4个碳原子的烷氧基,具有至多4个碳原子的烷酰氧基,卤素,三卤甲基,二-C1-4烷基氨基,C1-4烷氧基羰基,硝基,氰基或具有1-3个碳原子的酰基; R 5和R 6彼此相同或不同,分别为氢,甲基,羟基,羧基,C 1-4烷氧羰基,羟甲基,苯基或对氯苯基,R 7和R 8分别为氢或甲基。 j和k是0到3的整数,它们的和不超过4; m和n是0到3的整数,它们的和不超过4; A为-CH 2-或-CH 2 CH 2-;如果k或m不是O,则R5和R7一起或R6和R8一起是氧代。如果k或m不是O,则R5和R7一起以及R6和R8一起是氧代。 R9和R10可以相同或不同,代表氢或哌嗪环碳原子上的1-4个甲基取代基(A = -CH2-);彼此相同或不同的R 11,R 12,R 13和R 14分别为氢或甲基;或R11和R12一起和/或R13和R14一起是氧代;并且X是具有1至2个碳原子的亚烷基,其任选地被羟基取代,条件是当A = -CH 2-时,R 1至R 14为氢并且j,k,m和n各自为零,则X不能为1,2 -乙二醇及其生理上可接受的酸加成盐。

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