Targeted therapeutics

A binding moiety-drug conjugate (SDC-TRAP) comprising a binding moiety and an effector moiety, wherein the binding moiety is an Hsp90 binding moiety and comprises compounds of the following general formula V

• wherein:
• R1 is H, or CONR4R5;
• R5 is H, (C1-C6)-alkyl, or (C3-C10)-cycloalkyl, each being optionally substituted once or more with OH, OMe, Cl, or F;
• R4 is H, (C1-C4)-alkyl, or CH(R11)COR12;
• or
• R4 and R5, taken together with the nitrogen atom to which they are attached, form a three- to seven-membered heterocycle optionally containing a further heteroatom selected from the group consisting of N, O and S;
• and wherein the heterocycle is optionally substituted once or more by OH, OMe, (C1-C4)-alkyl, optionally substituted phenyl, or benzyl;
• R11 is a side chain of a natural α-amino acid;
• R12 is OH, amino, alkylamino or dialkylamino;
• R2 is a bond, —NH(CO)—, —N(R7)— or —N(R7)CH2—;
• R7 is H, (C1-C4)-alkyl or CO2R8;
• R8 is (C1-C4)-alkyl or benzyl;
• the endocyclic symbols are, for each single compound, all double bonds or all single bonds;
• m is an integer comprised between 0 and 3;
• R9 and R10 are, independently from each other, (C1-C4)-alkyl optionally substituted with OH, cycloalkyl, heterocycloalkyl, OMe, amino, (C1-C6)-alkylamino or (C1-C10)-dialkylamino;
• heterocycloalkyl optionally substituted once or more by alkyl, amino, (C1-C6)-alkylamino or (C1-C6)-dialkylamino;
• cycloalkyl;
• or
• R9 and R10, taken together with the nitrogen atom to which they are attached, form a heterocycle ring chosen from the group consisting of piperidyl, pyrrolidinyl, piperazinyl and morpholinyl, each of them being optionally substituted once or more by F, Cl, Br, OH, OMe, amino, (C1-C6)-alkylamino, (C1-C6)-dialkylamino, (C1-C4)-alkyl, hydroxyalkyl, optionally substituted phenyl, or benzyl;
• or an imidazole unsaturated heterocycle;
• R3 is Cl, Et or i-Pr;
• their tautomers, their geometrical isomers, their optically active forms such as enantiomers, diastereomers and their racemate forms, as well as their pharmaceutically acceptable salts thereof.