Compounds, compositions and methods for binding bio-affecting substances to surface membranes of bio-particles

A compound having the formula:

• wherein B represents a chemotherapeutic substance;
• R and R.sub.1 are substituents independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, alkaryl and aralkyl, the hydrocarbon chains of which having from 1 to about 30 carbon atoms, and being linear or branched, said substituents being unsubstituted or substituted with one or more non-polar functional groups, one of R or R.sub.1 having at least 12 linear carbon atoms, and the sum of the linear carbon atoms in R and R.sub.1 being sufficient to impart a membrane binding stability of at least 30% to said compound;
• R.sub.2 represents a spacer moiety of the formula:
• --(R.sub.3).sub.p --Q--(R.sub.4 --Q').sub.q --(R.sub.5 --Q"),--(R.sub.6 --Q"').sub.a --(R.sub.7 Q"").sub..tau. --
• wherein R.sub.3 represents an aliphatic hydrocarbon, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently selected from the group consisting of aliphatic, alicyclic or aromatic hydrocarbons, heterocycles, and CH.sub.2 C(CO.sub.2 M)=CH, Q and Q', Q", Q"' and Q"" are independently selected from the group of functional linkages consisting of amide, thiourea, hydrazone, acyl hydrazone, ketal, acetal, orthoester, ester, anhydride, disulfide, urea, carbamate, imine, amine, ether, carbonate, thioether, sulfonamide carbonyl and amidine linkages;
• Q', Q", Q"', Q"" may additionally independently represent a valence bond;
• said aliphatic hydrocarbons having from 1 to 12 linear carbon atoms;
• said aromatic hydrocarbons having from 6 to 12 carbon atoms;
• n, p, q, r, s, and t each may be either 0 or 1;
• X and X.sub.1 may be the same or different and represent O, S, C(CH.sub.3).sub.2 or Se;
• R.sub.8 is independently selected from the group consisting of H, CE.sub.3, CH.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 CH.sub.3 and CH(CH.sub.3).sub.2 ;
• y may be from 0 to 3;
• Z represents a substituent selected from the group consisting of H, alkyl, OH, --O--alkyl, COOH, CONH.sub.2, SO.sub.3 H, SO.sub.2 NH.sub.2, SH, S-alkyl, CONH-alkyl, CON-(alkyl).sub.2, NH-acyl, NH-alkyl, N(alkyl).sub.2, NO.sub.2, halogen, Si(alkyl).sub.3, O-Si(alkyl).sub.3, Sn(alkyl).sub.3 and --Hg--halogen, the alkyl groups comprising said Z substituent having from 1 to 4 carbon and
• A represents a pharmaceutically acceptable anion.