申请人:IMPERIAL CHEMICAL INDUSTRIES PLC
公开号:EP0126558A1
公开(公告)日:1984-11-28
This invention relates to a bisbiguanide of the formula: R1R1N.C(:NR5)NH.C(:NH)NH-X-NH.
or a tautomeric form thereof, wherein each of R1, R2, R3, and R4, which may be the same or different, is hydrogen, an alkyl radical of up to 5 carbon atoms (1-5C) such that R1, R2, R3 and R4 together contain 4 to 12 carbon atoms, or a 3-5C alkenyl radical; or R1, R2 and the nitrogen atom to which they are attached, or R3 and R4 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, each of which may bear 1-3C alkyl substituents; provided that at least one of R1, R2, R3, and R4 is other than hydrogen; R5 and R6 are each hydrogen or a 1-8C alkyl radical; and X is a 7-20C linking group which is a straight chain alkylene radical, or a straight chain alkylene radical bearing one or more 1-3C alkyl substituents, of which any pair or pairs which are attached to different carbon atoms may be joined so as to form, together with the intervening carbon atom or atoms of the alkylene radical, a cycloalkyl radical or radicals; and the acid addition salts thereof; to processes for the manufacture thereof; and to compositions and methods of use thereof.
本发明涉及一种式中的双胍:R1R1N.C(:NR5)NH.C(:NH)NH-X-NH.
或其同分异构体形式,其中 R1、R2、R3 和 R4(可以相同或不同)各自为氢、最多 5 个碳原子(1-5C)的烷基,这样 R1、R2、R3 和 R4 共含有 4 至 12 个碳原子,或 3-5C 烯基;或 R1、R2 及其所连接的氮原子,或 R3 和 R4 及其所连接的氮原子(可以相同或不同)各自为 1-氮杂环丁基、1-吡咯烷基、哌啶基、六亚甲基、七亚甲基、吗啉基或 4-(1-8C烷酰基)-1-哌嗪基,其中每个基团可带有 1-3C 烷基取代基;条件是 R1、R2、R3 和 R4 中至少有一个不是氢;R5 和 R6 各为氢或 1-8C 烷基;X 为 7-20C 连接基团,它是直链亚烷基,或带有一个或多个 1-3C 烷基取代基的直链亚烷基,其中连接到不同碳原子上的任何一对或多对可连接起来,以便与亚烷基的中间碳原子一起形成一个或多个环烷基;及其酸加成盐;其制造工艺;以及其组合物和使用方法。