申请人:AMERICAN HOME PRODUCTS CORPORATION
公开号:EP0050916A2
公开(公告)日:1982-05-05
Compounds of formula
in which R represents one of the following:
wherein X is the anion of a strong acid having a pKa below 2; R1 and R2 are, independently, hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, perfluoroalkyl of 1 to 3 carbon atoms, nitro, alkanoyl of 2 to 4 carbon atoms or alkoxycarbonyl of 2 to 4 carbon atoms; R is hydrogen, halo, nitro or alkanoyl of 2 to 4 carbon atoms; R4 is hydrogen, halo, nitro or perfluoroalkyl of 1 to 3 carbon atoms; R5 and R6 are, independently, hydrogen or methyl; and R7 and R8 are, independently, alkyl of 1 to 4 carbon atoms, or when taken with the nitrogen atom to which they are attached form a piperidinyl, pyrolidinyl, morpholinyl, N-alkyl piperazinyl in which the alkyl group contains from 1 to 6 carbon atoms or N-phenylpiperazinyl group; or a pharmaceutically acceptable acid addition salt thereof are disclosed which have CNS stimulant and antihypertensive activity. Processes for their preparation and pharmaceutical compositions are also described.
式化合物
其中 R 代表下列之一:
其中 X 是 pKa 低于 2 的强酸阴离子;R1 和 R2 独立地是氢、1 至 6 个碳原子的烷基、1 至 6 个碳原子的烷氧基、卤代、1 至 3 个碳原子的全氟烷基、硝基、2 至 4 个碳原子的烷酰基或 2 至 4 个碳原子的烷氧羰基;R 是氢、卤代、硝基或 2 至 4 个碳原子的烷酰基;R4 是氢、卤代、硝基或 1 至 3 个碳原子的全氟烷基;R5 和 R6 独立地为氢或甲基;以及 R7 和 R8 独立地为 1 至 4 个碳原子的烷基,或与所连接的氮原子形成哌啶基、吡咯烷基、吗啉基、N-烷基哌嗪基(其中烷基含有 1 至 6 个碳原子)或 N-苯基哌嗪基;或其药学上可接受的酸加成盐。此外,还描述了其制备方法和药物组合物。