| 主权项 |
1. A method of treating prostate cancer in a patient in need thereof comprising administering to said patient an effective amount of a compound according to the chemical structure: wherein A is an antibody binding moiety according to the chemical formula: Y′ is H or NO2; X is O, CH2, NR1, S(O), S(O)2, —S(O)2O, —OS(O)2, or OS(O)2O; R1 is H, a C1-C3 alkyl group, or a —C(O)(C1-C3) group; X′ is CH2, O, N—R1′ or S; R1′ is H or C1-C3 alkyl; Z is a bond, a monosaccharide, disaccharide, oligosaccharide, glycoprotein or glycolipid; Xb is a bond, O, CH2, NR1 or S; X″ is O, CH2, NR1; R1 is H, a C1-C3 alkyl group or a —C(O)(C1-C3) group; n is 1 or 2; n1 is 1; B is a cell binding moiety according to the chemical formula: Where X1 and X2 are each independently CH2, O, NH or S; X3 is O, CH2, NR1, S(O), S(O)2, —S(O)2O, —OS(O)2, or OS(O)2O; R1 is H, a C1-C3 alkyl group, or a —C(O)(C1-C3) group; k is an integer from 0 to 20; L is a linker according to the chemical formula: Or a polypropylene glycol or polypropylene-co-polyethylene glycol linker having between 1 and 100 glycol units; Where Ra is H, C1-C3 alkyl or alkanol or forms a proline side chain with R3; R3 forms a proline side chain with Ra or is a side chain derived from an amino acid wherein said amino acid is selected from the group consisting of alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, serine, threonine, tryptophan, tyrosine and valine; and m is an integer from 1 to 45, or L is a linker according to the chemical formula: Where Z and Z′ are each independently a bond, —(CH2)i—O, —(CH2)i—S, —(CH2)i—N—R, wherein said —(CH2)i group, if present in Z or Z′, is bonded to [CON] if present, antibody binding terminus (ABT) or cell binding terminus (CBT); Each R is independently H, or a C1-C3 alkyl or alkanol group; Each R2 is independently H or a C1-C3 alkyl group; Each Y is independently a bond, O, S or N—R; Each i is independently 0 to 100; D isor a bond,
with the proviso that Z, Z′ and D are not each simultaneously bonds; j is 1 to 100; m′ is 1 to 100; n′ is 1 to 100; and X1 is O, S or N—R, R is as defined above; and
[CON] is a bond or a moiety according to the chemical structure: Where X2 is O, S, NR4, S(O), S(O)2, —S(O)2O, —OS(O)2, or OS(O)2O; X3 is NR4, O or S; and R4 is H, a C1-C3 alkyl or alkanol group, or a —C(O)(C1-C3) group; or a pharmaceutically acceptable salt thereof. |
