Patent ID: 8338140

Claim:
A method of preparing a modified dendrimer comprising: (a) obtaining a dendrimer molecule comprising surface carboxylic acid groups; (b) reacting one or more of the carboxylic acid groups with a carbodiimide and (i) an amine-containing acetylene molecule, or (ii) an amine-containing azide molecule to form an acetylene-derivatized or azide-derivatized dendrimer molecule; (c) reacting other carboxylic acid groups of the acetylene-derivatized or azide-derivatized dendrimer molecule with a carbodiimide and a maleimido amine to form a maleimide-appended, acetylene- or azide-derivatized dendrimer molecule; (d) reacting (i) the maleimide-appended, acetylene-derivatized dendrimer molecule with an azide-derivatized drug or (ii) the maleimide-appended, azide-derivatized dendrimer molecule with an acetylene-derivatized drug to form a maleimide-appended, drug modified dendrimer molecule; and (e) forming a covalent bond between the maleimide-appended, drug modified dendrimer molecule and a thiol-containing compound comprising a recognition moiety to form a recognition moiety-appended, drug-modified dendrimer molecule, wherein the recognition moiety is selected from the group consisting of (i) somatostatin, (ii) folic acid, (iii) biotin, (iv) an antibody that binds to a hapten HSG or In-DTPA and (v) an antibody or antigen binding fragment thereof wherein the antibody is hR1 (anti-IGFR), RS7 (anti-EGP-1), LL1 (anti-CD74), LL2 (anti-CD22), RFB4 (anti-CD22), A20 (anti-CD20), A19 (anti-CD19), IMMU31 (anti-AFP), PAM4 (anti-MUC-1), KC4 (anti-MUC-1), MN-3 (anti-CEA), MN-14 (anti-CEA), MN-15 (anti-CEA), Mu-9 (anti-colon-specific antigen-p), Immun 31 (anti-alpha-fetoprotein), CC49 (anti-TAG-72), J591 (anti-prostate specific membrane antigen), G250 (anti-carbonic anhydrase IX) and L243 (anti-HLA-DR).