Diorthosubstituted benzene derivatives, especially for use in a method of therapy, processes for their preparation, and pharmaceutical compositions containing them
申请人:Kabi AB
公开号:EP0000826A1
公开(公告)日:1979-02-21
New compounds of the general formula I
wherein R' and R2 each independently represent an alkyl group containing 1 to 4 carbon atoms, or an alkoxy group containing 1 to 3 carbon atoms, or halogen, R' represents hydrogen, halogen, an alkyl group containing 1 to 4 carbon atoms, an alkoxv group containing 1 to 3 carbon atoms, an amino group or a nitro group, A represents
which is bonded to the benzene ring by its sulphu r or nitrogen atom and in which R' is hydrogen or an alkyl group containing to 4 carbon atoms; together with salts thereof with I physiologically acceptable acids and, when R' is hydrogen, with physiologically acceptable bases are described. The compounds are of use in inhibiting thrombosis formation, in treating thrombosis and in fibronolytic therapy. Various methods of producing the new compound are described involving the building up of the -A-CH2 -CH2-S-CH2 CH2 -NH2 side chain from aromatic precursors having an imcomplete side chain or by introducing at least one of R1, R or R'substituents into a precursor lacking that substituent or from an amino-protected precursor.
通式 I 的新化合物
其中 R' 和 R2 各自独立地代表含有 1 至 4 个碳原子的烷基或含有 1 至 3 个碳原子的烷氧基或卤素,R' 代表氢、卤素、含有 1 至 4 个碳原子的烷基、含有 1 至 3 个碳原子的烷氧基、氨基或硝基,A 代表
其中 R'为氢或含有至 4 个碳原子的烷基;以及其与 I 生理上可接受的酸的盐,当 R'为氢时,与生理上可接受的碱的盐。这些化合物可用于抑制血栓形成、治疗血栓和纤维溶解疗法。描述了生产新化合物的各种方法,包括从具有不完整侧链的芳香族前体中建立-A-CH2 -CH2-S-CH2 CH2 -NH2侧链,或将R1、R或R'中的至少一个取代基引入缺乏该取代基的前体中,或从氨基保护的前体中建立-A-CH2 -CH2-S-CH2 CH2 -NH2侧链。