Patent ID: 6214969
Filing Date: 2001-04-10
Classification: A61K,C07K,Y10S

Abstract:
A peptide selected from the group of peptides having the formula:X-R.sup.1 -R.sup.2 -R.sup.3 -Ser-R.sup.5 -R.sup.6 (Q)-Leu-Arg-Pro-R.sup.10 -NH.sub.2whereinR.sup.1 is pGlu or D-Nal(2),R.sup.2 is His or D-Phe(4Cl),R.sup.3 is Trp, D-Trp or D-Pal(3),R.sup.5 is Tyr or Arg,R.sup.6 is D-Lys or D-Orn,R.sup.10 is Gly or D-Ala,X is hydrogen or a lower alkanoyl group of 2-5 carbon atoms,Q is a cytotoxic moiety having the formula--Q.sup.4 or --A(Q.sup.3) or --B(Q.sup.1).sub.2 or --B(AQ.sup.2).sub.2whereinA is --NH--(CH.sub.2).sub.n --CO-- or --OC--(CH.sub.2).sub.n --CO--where n is 2-6,B is --HN--CH.sub.2 --(CH.sub.2).sub.m --CH(NH)--(CH.sub.2).sub.n --CO--wherem is 0 or 1,n is 0 or 1,the --CO moiety of A-- and of B-- being bonded to the epsilon or delta amino group of R.sup.6 when R.sup.6 is Lys or Orn respectively, and in the group B(AQ.sup.2).sub.2, the --CO moiety of A being bonded to an amino group on B,Q.sup.1 is D or L-melphalanyl, cyclopropanecarbonyl, aziridine-2-carbonyl, epoxyalkyl or 1,4-naphthoquinone-5-oxycarbonyl-ethyl,Q.sup.2 is Q.sup.1, 2-anthraquinonyl-methylenoxy or doxorubicinyl,Q.sup.3 is Q.sup.2, mitomicinyl, esperamycinyl or methotrexoyl,Q.sup.4 is Q.sup.1 or methotrexoyl,and pharmaceutically acceptable salts thereof.