Patent ID: 6844318

Claim:
A compound of Formula (I): E cp -A (I) or a pharmaceutically acceptable salt form thereof, wherein; E cp is an enzyme cleavable peptide conjugated to A and selected from: Cap-Paa-Xa2-Gly-Xp1-Laa-; Cap-Xa2-Gly-Xp1-Laa-; Cap-Paa-Xa2-Gly-Xp1-Xp2-Laa-; Cap-Xa2-Gly-Xp1-Xp2-Laa-; Cap-Gly-Xp1-Xp2-Laa-; Cap-Paa-Xa2-Gly-Xp1-Xp2-Xp3-Laa-; Cap-Xa2-Gly-Xp1-Xp2-Xp3-Laa-; Cap-Gly-Xp1-Xp2-Xp3-Laa-; Cap-Paa-Xa2-Sar-Xp1-Laa-; Cap-Xa2-Sar-Xp1-Laa-; Cap-Paa-Xa2-Sar-Xp1-Xp2-Laa-; Cap-Xa2-Sar-Xp1-Xp2-Laa-; Cap-Sar-Xp1-Xp2-Laa-; Cap-Paa-Xa2-Sar-Xp1-Xp2-Xp3-Laa-; Cap-Xa2-Sar-Xp1-Xp2-Xp3-Laa-; and Cap-Sar-Xp1-Xp2-Xp3-Laa-; Paa is a Pro, Hyp, Aze, homo-Pro, Chg, Fph, Npa, Tzc, or proline mimetic; Xa2 is a natural amino acid; Xp1 is an amino acid wherein -Gly-Xp1- or -Sar-Xp1- form a bond cleavable by a matrixin; Xp2 is an amino acid; Xp3 is an amino acid; Laa is an amino acid selected from Leu, Ile, Nle, β-homo-Leu, Hol, Hos, Ala, β-Ala, Cha, Cba, Cta, 4-pyridyl-Ala, 3-pyridyl-Ala, 2-pyridyl-Ala, Gly, Abu, Aib, Iva, Nva, Ahx, Aph, Amh, Phe, Bip, Glu, Arg, Trp, Tyr, O—(C 1 -C 4 alkyl)-Tyr, O-(phenyl(C 1 -C 4 alkyl)-)-Tyr, (C 3 -C 8 alkyl)-Gly, and aminoalkyl carboxylic acid; Cap is an N-terminus group selected from R—; Xa4-; and R-Xa4-; Xa4- is an amino acid; R is an amino capping group; and A is an antineoplastic agent; with the following provisos: a) Cap is not hydrogen; b) Cap is not a polyhydroxyalkanoyl; c) Cap is not a non-natural amino acid or succinyl; d) Cap is not benzyloxycarbonyl (Cbz); e) E cp does not comprise a dipeptide linkage selected from-Tyr-Ser-; -Tyr-Thr-; -Phe-Ser-; -Gln-Ser-; -Gln-Thr-, and -Asn-Ser; and f) E cp is not -Gly-Gly-Arg-Leu-(SEQ ID NO: 225), E cp is not -Gly-Val-Phe-Arg-(SEQ ID NO: 226), E cp is not -Ala-Pro-Gly-Leu-(SEQ ID NO: 227), E cp is not 2-thienylalanine-Gly-Ala-Leu-, E cp is not 2-naphthylalanine -Gly-Ala-Leu-, or E cp is not -Gly-Leu-Gly-Leu-(SEQ ID NO: 230).