Patent ID: 6759509
Filing Date: 2004-07-06
Classification: A61K,C07K

Abstract:
A compound of the following formula II: whereinA is a thiol acceptor; W is a bridging moiety; c is an integer of 0 to 1; a is an integer of 2 to 12; Q is O, NH, or N-lower alkyl; p is an integer of 0 or 1; d is an integer of 0 or 1; E is a polyvalent atom; each b is an integer of 1 to 10; each X is of the formula â€”COâ€”Yâ€”Zmâ€”GnD whereinY is two amino acid residues in the L form; Z is one or two amino acid residues; m is an integer of 0 or 1; G is a self-immolative spacer; n is a integer of 0 or 1; provided that when n is 0 then â€”Yâ€”Zmâ€” an amino acid sequence of SEQ ID NO:1 or SEQ ID NO:2; and D is a Drug moiety having a backbone and at least one chemically reactive functional group pendant thereto chemically reacted to the self-immolative spacer or terminal amino acid residue to form a covalent bond, said functional group selected from the group consisting of a primary amine or secondary amine, hydroxyl, sulfhydryl, carboxyl, aldehyde therefore ketone; or each X is of the formula wherein each X1 is of the formula â€”COâ€”Yâ€”Zmâ€”Gnâ€”D; wherein Y, Z, G, D, Q, E, m, d, p and n are as defined above; or each X1 is of the formula wherein each X2 is of the formula â€”COâ€”Yâ€”Zmâ€”Gnâ€”D; and wherein Y, Z, G, D, Q, E, m, d, p, a, b and n are as defined above; or each X2 is of the formula wherein each X3 is of the formula â€”COâ€”Yâ€”Zmâ€”Gnâ€”D; and whereinr Z, G, D, Q, E, m, d, p, a, b and n are as defined above; or each X3 is of the formula â€ƒand wherein each X4 is of the formula â€”COâ€”Yâ€”Zmâ€”Gnâ€”D; â€ƒand wherein Y, Z, G, D, Q, E, m, d, p, a, b and n are as defined above.