申请人:IMPERIAL CHEMICAL INDUSTRIES PLC
公开号:EP0125093A1
公开(公告)日:1984-11-14
A diaz(ep)ine bis(N-amidinoamidine) derivative of the formula:-
or a tautomeric form thereof, wherein R10, R", R12. R13, R", R15, R16 and R17, which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 3-18C cycloalkyl or cycloalkylalkyl radical, or an optionally-substituted phenyl (1-4C alkyl) radical, or R'°, R" and the nitrogen atom to which they are attached, or R12 and R" and the nitrogen atom to which they are attached, or R14 and R15 and the nitrogen atom to which they are attached, or R16 and R17 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical, or R10 and R14 together with the two nitrogen atoms to which they are attached and the intervening carbon atom, or R12 and R16 together with the two nitrogen atoms to which they are attached and the intervening carbon atom, each forms a 1,3-diazaheterocyclic radical of 5 to 7 atoms, which heterocyclic radicals may be the same or different; and m is 2 or 3; provided that R'°, R", R12, R13, R14, R'5, R" and R17 togethercontain 16to 28 carbon atoms, and the acid addition salts thereof, processes for their manufacture and antibacterial and antifungal compositions and methods using said compounds.
式中的重氮(表)烯双(N-脒基脒)衍生物
或其同分异构体,其中 R10、R"、R12.R13、R"、R15、R16 和 R17(可以相同或不同)各自为氢、1-16C 烷基、3-18C 环烷基或环烷基烷基、或任选取代的苯基(1-4C 烷基)基,或 R'°、R "和它们所连接的氮原子、或 R12 和 R "及其所连接的氮原子,或 R14 和 R15 及其所连接的氮原子,或 R16 和 R17 及其所连接的氮原子,它们可以相同或不同、各自是 1-氮杂环丁基、1-吡咯烷基、哌啶基、六亚甲基亚氨基、七亚甲基亚氨基、吗啉基或 4-(1-8C 烷酰基)-1-哌嗪基,或 R10 和 R14 连同它们所连接的两个氮原子和中间的碳原子、或 R12 和 R16 与它们所连接的两个氮原子和中间的碳原子一起,各自形成 5 至 7 个原子的 1,3-二氮杂环基,这些杂环基可以相同或不同;m为2或3;条件是R'°、R"、R12、R13、R14、R'5、R "和R17一起含有16至28个碳原子,以及它们的酸加成盐、它们的制造工艺和使用所述化合物的抗菌和抗真菌组合物和方法。