申请人:LIFE TECHNOLOGIES CORPORATION
公开号:US20150190522A1
公开(公告)日:2015-07-09
Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure:
wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH
2
)
l
, or (CH
2
)
i
—Y—(CH
2
)
j
}
k
, wherein Y is selected from the group consisting of CH
2
, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X
1
-L′-X
2
—Z or —Z; R
1
R
6
, independently of one another, are selected from the group consisting of H, —(CH
2
)
p
-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and wherein at least one of R
1
, R
3
, R
4
and R
6
is a straight chain or branched, cyclic, alkyl, alkenyl, alkynyl or aryl group; and anyone of R
1
, R
3
, R
4
and/or R
6
may optionally be covalently linked with each other, with Y or with L when L is C or CH to form a cyclic moiety; Z is selected from the group consisting of amine, spermiyl, carboxyspermiyl, guanidyl, spermidinyl, putricinyl, diaminoalkyl, pyridyl, piperidinyl, pyrrolidinyl, polyamine, amino acid, peptide, and protein; X
1
and X
2
, independently of one another, are selected from the group consisting of NH, O, S, alkylene, and arylene; L′ is selected from the group consisting of alkylene, alkenylene, alkynylene, arylene, alkylene ether, and polyether; D is Q or a bond; A
1
and A
2
, independently of one another, are selected from the group consisting of CH
2
O, CH
2
S, CH
2
NH, C(O), C(NH), C(S) and (CH
2
)t; X is a physiologically acceptable anion; m, n, r, s, u, v, w and y are 0 or 1, with the proviso that when both m and n are 0 at least one of r, s, u and y is other than 0; i, j, k, l, p and are integers from 0 to about 100; q is an integer from 1 to about 1000; and a is the number of positive charge divided by the valence of the anion.