Methyladamantyl hydrazines, their pharmaceutically acceptable salts and pharmaceutical compositions containing them
申请人:Teva Pharmaceutical Industries Limited
公开号:EP0002065A1
公开(公告)日:1979-05-30
The invention provides novel 1- or 2-adamantylmethyl hydrazines of the general formulaA
In this formula Ad is 1- or 2-adamantyl, R1 and R2 are the same or different and are each hydrogen or a lower unsubstituted or substituted alkyl group of 1-4 carbon atoms; R, and R4 are the same or different and are each hydrogen, an unsubstituted or substituted radical being a lower alkyl group of 1-4 carbon atoms, a lower alkanoic acid radical of 2-4 carbon atoms or a lower alkyl ester thereof, adamantyl, aryl, aralkyl in which the alkyl moiety has 1-4 carbon atoms or an unsubstituted or substituted heterocyclic radical of aromatic character; or R3 and R4 together with the nitrogen atom to which they are attached form a cyclic radical of non-aromatic character.
The invention further provides pharmaceutically acceptable acid addition salts of the above compounds.
Several methods of preparation of the new compounds are described.
The novel compounds according to the invention possess valuable antifungal (human and plant), antiviral, antiprotozoal and antimicrobial properties.
本发明提供了一般式A的新型1-或2-金刚烷基甲基肼化合物。在该式中,Ad为1-或2-金刚烷基,R1和R2相同或不同,均为氢原子或1-4个碳原子的低级未取代或取代烷基基团;R3和R4相同或不同,均为氢原子、未取代或取代的低级烷基基团、2-4个碳原子的低级烷基酸基团或其低级烷基酯、金刚烷基、芳基、芳基烷基(其中烷基部分有1-4个碳原子)或芳香性质的未取代或取代的杂环基团;或R3和R4与它们所连接的氮原子一起形成非芳香性质的环状基团。本发明还提供了上述化合物的药学上可接受的酸加成盐。描述了几种制备新化合物的方法。根据本发明,新型化合物具有有价值的抗真菌(人类和植物)、抗病毒、抗原虫和抗微生物性质。