申请人:Botti, Paolo
公开号:EP1905454A1
公开(公告)日:2008-04-02
This invention relates to the use of a cyclic compound of formula (I)
wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p-(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p-(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition further comprising a pharmaceutically or diagnostically active agent, said active agent comprising one or more protonated primary and/or protonated secondary amino groups and/or a protonated guanidinium groups, wherein (a) transmembrane and/or transmucosal delivery; (b) solubility in non-aqueous solvents; and/or (c) stability of said active agent are improved.
本发明涉及使用公式(I)的环状化合物,其中A,B分别在每次出现时为具有k个碳原子的烷基-i,j-二基,i和j分别独立于k,k选择从1到10,其中所述烷基-i,j-二基(i)可以包括一个或多个双键;(ii)可选地被取代;和/或(iii)包括一个环,其中所述化合物中的环状糖的总数选择从0到4,并且小于p-(n+m);X,Y分别在每次出现时是至少包含一个氧原子或两个硫原子的生物相容性功能基团;n,m彼此独立地选择从0到20;p选择从1到10;n+m等于1或更大;p-(n+m)选择从3到30;其中所述化合物能够与质子化的一级和/或质子化的二级氨基基团和/或质子化的鸟氨酸基团形成复合物,用于制造制药或诊断组合物,进一步包括药物学或诊断学活性剂,所述活性剂包括一个或多个质子化的一级和/或质子化的二级氨基基团和/或质子化的鸟氨酸基团,其中(a)跨膜和/或经黏膜递送;(b)在非水溶剂中的溶解度;和/或(c)所述活性剂的稳定性得到改善。