Patent ID: 7771727

Claim:
A compound represented by the following formula: wherein: X is camptothecin, homocamptothecin, colchicine, thiocolchicine, combretastatin, dolastatin, doxorubicin, methotrexate, podophyllotoxin, rhizoxin, rhizoxin D, a taxol, paclitaxel, CC1065, or a maytansinoid; n is an integer from 0 to 6, wherein (CH 2 ) n is an alkyl or a cyclic group; R is N(R 1 R 2 ), OR 1 , or SR 1 , wherein R 1 and R 2 are, independently, hydrogen or a straight or branched chain lower alkyl group having fewer than 11 carbon atoms, and wherein R 3 is a NH(CH 2 ) m SH group and m=2 to 6, D or L cysteine, a benzophenone, an OH group, or is NH-Y-Z-Q wherein: Y is a hydrophilic spacer sequence selected from the group consisting of a peptide that increases the hydrophilic biodistribution of said compound and a hydrophilic polymer, or is omitted, wherein: said peptide that increases the hydrophilic biodistribution of said compound has the formula U(V-V)n, wherein U is D-Pro, L-Pro, D-4-OH-Pro, L-4-OH-Pro, Sarcosine, Lys, Ore, Dab, Dap, 4-NH 2 -Phe, or (NH 2 —(CH 2 ) m —COOH), where m=2-10, inclusive, or is deleted; each V is independently selected from the group consisting of: D-Ser, L-Ser, D-Thr, L-Thr, D-Gln, L-Gln, D-Asn, L-Asn, D-4-OH-Pro, and L-4 hydroxy-Pro; and n=1-50, inclusive, and said hydrophilic polymer is selected from the group consisting of polyethylene glycol, polyvinyl acetate, polyvinyl alcohol, HPMA (N-(2-hydroxypropyl) methacrylamide) or HPMA copolymers, α, β-poly(N-hydroxyethyl)-DL-aspartamide (PHEA), and α, β-poly(N-hydroxypropyl)-DL-aspartamide; Z is a linking peptide that is bonded to Q at the N-terminus or at a compatible side-chain amino group of Q or is omitted, wherein Z has the formula: A-B-C-E-F, wherein: A is D-Lys, D-Tyr, D-Ser, or L-Ser, or is deleted; B is D-Lys or D-Tyr, or is deleted; C is Lys, Ser, hSer, Thr, Nle, Abu, Nva, (2, 3, or 4) 3-pyridyl-Ala (Pal), Orn, Dab, Dap, 4-NH 2 -Phe, D-4-OH-Pro, or L-4-OH-Pro, or is deleted; E is D-Lys, D-Tyr, D-Ser, D-4-OH-Pro, L-4-OH-Pro, 3-iodo-D-Tyr, 3-5 diiodo-D-Tyr, 3-astatine-D-Tyr, 3-5 astatine-D-Tyr, 3-bromo-D-Tyr, 3-5 dibromo-D-Tyr, D-Asn, L-Asn, D-Asp, L-Asp, D-Glu, L-Glu, D-Gln, or L-Gln; and F is D-Lys, D-Tyr, D-Ser, L-Ser, D-4-OH-Pro, L-4-OH-Pro, 3-iodo-D-Tyr, 3-5 diiodo-D-Tyr, 3-astatine-D-Tyr, 3-5 astatine-D-Tyr, 3-bromo-D-Tyr, 3-5 dibromo-D-Tyr, D-Asn, L-Asn, D-Asp, L-Asp, D-Glu, L-Glu, D-Gln, or L-Gln; provided that when A, B, C, and E are Tyr, Tyr, Lys, and Tyr, respectively, F is not Lys; and when A, B, C, and E are Lys, Tyr, Lys, and Tyr, respectively, F is not Tyr or Lys; and when A and B are deleted, and C and E are Lys and Tyr, respectively, F is not Tyr or Lys; and Q is a targeting moiety selected from a somatostatin peptide, a bombesin peptide, or a vasoactive intestinal peptide (VIP).