首页> 外国专利> N-aryl and N-heteroaryl-1,2-diaminocyclobutene-3,4-diones with smooth (N-Aryl and N-heteroaryl-1,2-diaminocyclobutene- muscle relaxing activities)

N-aryl and N-heteroaryl-1,2-diaminocyclobutene-3,4-diones with smooth (N-Aryl and N-heteroaryl-1,2-diaminocyclobutene- muscle relaxing activities)

机译:具有平滑性的N-芳基和N-杂芳基-1,2-二氨基环丁烯-3,4-二酮(N-芳基和N-杂芳基-1,2-二氨基环丁烯-肌肉松弛活性)

摘要

A compound of formula (I) or a pharmaceutically acceptable salt thereof.;Wherein R 1 is hydrogen, C 1-10 linear or branched alkyl, C 3-10 cyclic or acyclic alkyl, C 2-7 alkanoyl, C 1-7 alkylsulfonyl, C 7-12 Arylalkanoyl having 9 to 20 carbon atoms, arylsulfonyl having 6 to 12 carbon atoms, arylalkanoyl having 8 to 12 carbon atoms or arylalkylsulfonyl having 7 to 12 carbon atoms; R 2 is hydrogen, C 1-10 linear or branched alkyl or C 3-10 cyclic or acyclic alkyl; A is a group Wherein R 7 and R 8 are independently of each other selected from the group consisting of cyano, nitro, amino, C 1-6 alkyl, C 1-6 perfluoroalkyl, C 1-6 alkoxy, C 1-6 perfluoroalkoxy, Amino, C 1-12 mono- or dialkylamino, sulfonamido, C 1-6 alkylsulfonamido, C 6-12 arylsulfonamido, C 2-6 alkylcarboxamido, C 7-12 arylcar carboxamide amido, C 1-6 alkylsulfonyl, C 1-6 alkylsulfonyl as a perfluoroalkyl, C 6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl, Carboxyalkoxy of 2 to 7 carbon atoms, hydroxyl or hydrogen), or A is Het is; Wherein R 9 is selected from the group consisting of hydrogen, C 1-6 alkyl, C 1-6 perfluoroalkyl, C 1-6 alkoxy, C 1-6 perfluoroalkoxy, amino, C 1-12 mono- or dialkylamino , C 1-6 alkylsulfonamido, C 2-6 alkylcarboxamido, nitro, cyano, carboxyl, chloro, bromo, fluoro or iodo; n is an integer from 0 to 6; R 3 and R 4 are, independently of each other, hydrogen, C 1-10 linear or branched alkyl or C 3-10 cyclic or acyclic alkyl; C 1-10 perfluoroalkyl, C 1-10 hydroxyalkyl, C 2-10 alkoxyalkyl, fluoro; Or together form a spirocyclic ring having 3 to 7 total carbon atoms; R 5 and R 6 independently of each other are selected from the group consisting of cyano, nitro, amino, C 1-6 alkyl, C 1-6 perfluoroalkyl, C 1-6 alkoxy, C 1-6 perfluoroalkoxy, amino, C 1 - 12 mono- or dialkylamino, sulfonamide, C 1-6 alkyl sulfonamido, C 6-12 aryl sulfonamido, C 2-6 alkyl, carboxamido, C 7-12 aryl carboxamido , C 1-6 alkyl sulfonyl, alkyl sulfonyl, C 6-12 arylsulfonyl, chloro, bromo, fluoro C 1-6 perfluoroalkyl, iodo, 1-imidazolyl, carboxyl, C 2- 7 carboalkoxy, hydroxyl or hydrogen.
机译:式(I)的化合物或其药学上可接受的盐;其中R 1 是氢,C 1-10 直链或支链烷基,C 3- 10环状或无环烷基,C 2-7烷酰基,C 1-7烷基磺酰基,C 7-12碳原子数为9至20的芳基烷酰基,芳基磺酰基具有6至12个碳原子,芳基烷酰基为8至12个碳原子或具有7至12个碳原子的芳基烷基磺酰基; R 2 是氢,C 1-10 直链或支链烷基或C 3-10 环状或无环烷基; A是其中R 7 和R 8 彼此独立的基团,其选自氰基,硝基,氨基,C 1-6 烷基,C 1-6 全氟烷基,C 1-6 烷氧基,C 1-6 全氟烷氧基,氨基,C 1 -12 单或二烷基氨基,磺酰胺基,C 1-6 烷基磺酰胺基,C 6-12 芳基磺酰胺基,C 2-6 烷基羧酰胺基,C 7-12 芳基羧酰胺酰胺,C 1-6 烷基磺酰基,C 1-6 烷基磺酰基为全氟烷基,C 6-12 芳基磺酰基,氯,溴,氟,碘,1-咪唑基,羧基,具有2至7个碳原子的羧基烷氧基,羟基或氢),或其中R 9 选自氢,C 1-6 烷基,C 1-6 全氟烷基,C 1 -6 烷氧基,C 1-6 全氟烷氧基,氨基,C 1-12 单或二烷基氨基,C 1-6 烷基磺酰胺基,C 2-6 烷基甲酰胺基,硝基,氰基,羧基,氯,溴,氟或碘; n是0至6的整数; R 3 和R 4 彼此独立地是氢,C 1-10 直链或支链烷基或C 3- 10 环状或无环烷基; C 1-10 全氟烷基,C 1-10 羟烷基,C 2-10 烷氧基烷基,氟;或一起形成总碳原子数为3至7的螺环;彼此独立的R 5 和R 6 选自氰基,硝基,氨基,C 1-6 烷基,C 1-6 全氟烷基,C 1-6 烷氧基,C 1-6 全氟烷氧基,氨基,C 1-12 单或二烷基氨基,磺酰胺,C 1-6 烷基磺酰胺基,C 6-12 芳基磺酰胺基,C 2-6 烷基,羧酰胺基,C 7-12 芳基甲酰胺基,C 1-6 烷基磺酰基,烷基磺酰基,C 6-12 芳基磺酰基,氯,溴,氟C 1-6 全氟烷基,碘,1-咪唑基,羧基,C 2-7 碳烷氧基,羟基或氢。

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