Patent ID: 6613879
Filing Date: 2003-09-02
Classification: A61K,A61P,B82Y,C07H,C07K

Abstract:
A compound of formula (I) or a pharmaceutically acceptable salt thereof, whereinR1 represents a residue of formula Cgâ€”A, Cgâ€”Bâ€”A or Cgâ€”(D)mâ€”Bâ€”A, in which Cg represents a capping group selected from the group consisting of R5â€”CO, R5â€”Oâ€”COâ€”, R5â€”NHâ€”COâ€”, R5â€”SO2â€” or R5â€”, wherein R5 is an optionally substituted C3-C8-cycloalkyl, aryl, aralkyl or heteroaryl group; A is an amino carboxylic acid moiety selected from L-proline, glycine, L-norleucine, L-cyclohexylglycine, L-5-hydroxynorleucine, L-6-hydroxynorleucine, L-5-hydroxylysine, L-arginine, and L-lysine; and B and D each independently represent an amino carboxylic moiety of the formula â€”[NR6â€”(X)pâ€”CO]â€” wherein X represents CR7R8 and wherein R6, R7 and R8 each independently represent a hydrogen atom, an optionally substituted C1-C6-alkyl, C3-C8-cycloalkyl, aryl or heteroaryl group, and p is 1, 2, 3, 4 or 5; or B and D each independently represent moieties derived from cyclic amino carboxylic acids of formula â€ƒwherein R9 represents C1-C6-alkyl, OH, or NH2, m is an integer from 1 to 10; q is 0, 1 or 2; and r is 0, 1 or 2; Ra and Rb together with the interjacent Nâ€”C group form an optionally substituted, optionally benzo- or cyclohexano-condensed 3- to 7-membered saturated or unsaturated heterocyclic ring, in which one or two CH2 groups may also be replaced by NH, O or S, and â€”NHâ€”Cytâ€² represents a cytotoxic compound or cytostatic compound, less a hydrogen atom.