Disclosed are compounds capable of facilitating transport of biologically
active agents or substances into cells having the general structure:
##STR00001## 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.sub.2).sub.1, or
{(CH.sub.2).sub.i--Y--(CH.sub.2).sub.j}.sub.k, wherein Y is selected from
the group consisting of CH.sub.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.sub.1--L'--X.sub.2--Z or --Z; R.sub.1 R.sub.6,
independently of one another, are selected from the group consisting of
H, --CH.sub.2).sub.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.sub.1, R.sub.3, R.sub.4
and R.sub.6 is a straight chain or branched, cyclic, alkyl, alkenyl,
alkynyl or aryl group; and any one of R.sub.1, R.sub.3, R.sub.4 and/or
R.sub.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.sub.1 and
X.sub.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.sub.1 and A.sub.2,
independently of one another, are selected from the group consisting of
CH.sub.2O, CH.sub.2S, CH.sub.2NH, C(O), C(NH), C(S) and (CH.sub.2).sub.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 t 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.