Patent ID: 8410045
Filing Date: 2013-04-02
Classification: A61K,A61P

Abstract:
1. A conjugate comprising at least one camptothecin, wherein said conjugate has the following formula (VI): wherein X represents a cell penetrating peptide (CPP), which is attached to the remainder of the conjugate by a thioether bond, wherein the cell penetrating peptide comprises an amino acid sequence selected from the group consisting of: DPV3 (SEQ ID NO: 1): Arg Lys Lys Arg Arg Arg Glu Ser Arg Lys Lys Arg Arg Arg Glu Ser DPV6 (SEQ ID NO: 2): Gly Arg Pro Arg Glu Ser Gly Lys Lys Arg Lys Arg Lys Arg Leu Lys Pro DPV7 (SEQ ID NO: 3): Gly Lys Arg Lys Lys Lys Gly Lys Leu Gly Lys Lys Arg Asp Pro DPV7b (SEQ ID NO: 4): Gly Lys Arg Lys Lys Lys Gly Lys Leu GIy Lys Lys Arg Pro Arg Ser Arg DPV10 (SEQ ID NO: 5): Ser Arg Arg Ala Arg Arg Ser Pro Arg His Leu Gly Ser Gly DPV3/10 (SEQ ID NO: 6): Arg Lys Lys Arg Arg Arg Glu Ser Arg Arg Ala Arg Arg Ser Pro Arg His Leu DPV10/6 (SEQ ID NO: 7): Ser Arg Arg Ala Arg Arg Ser Pro Arg Glu Ser Gly Lys Lys Arg Lys Arg Lys Arg DPV1047 (SEQ ID NO: 8): Val Lys Arg Gly Leu Lys Leu Arg His Val Arg Pro Arg Val Thr Arg Met Asp Val DPV1048 (SEQ ID NO: 9): Val Lys Arg Gly Leu Lys Leu Arg His Val Arg Pro Arg Val Thr Arg Asp Val DPV15 (SEQ ID NO: 10): Leu Arg Arg Glu Arg Gln Ser Arg Leu Arg Arg Glu Arg Gln Ser Arg and DPV15b (SEQ ID NO: 11): Gly Ala Tyr Asp Leu Arg Arg Arg Glu Arg Gln Ser Arg Leu Arg Arg Arg Glu Arg Gln Ser Arg; Y represents the camptothecin and is represented by: wherein t is 0, 1 or 2 and Z is a —COO—group or a substituted or unsubstituted divalent alkyl group; Y is attached to the remainder of the conjugate by an ester bond, a carbonyl-disulfide bond or a carboxy-thioester bond; B is a cyclo(C R and R