Appeal No. 1996-2431
Application 08/008,186
Claims 1, 2, 5, 13 and 14 are representative of the subject matter on appeal and
read as follows:
1. A peptide selected from the group of peptides having the formula:
1 2 3 5 6 10
X-R -R -R -Ser-R -R (Q)-Leu-Arg-Pro-R -NH
2
wherein
1
R is pGlu or D-Nal(2),
2
R is His or D-Phe(4Cl),
3
R is Trp, D-Trp or D-PAl(3),
5
R is Tyr or Arg
6
R is D-Lys or D-Orn
10
R is Gly or D-Ala,
X is a hydrogen or a lower alkanoyl group of 2-5 carbon atoms,
Q is a cytotoxic moiety having the formula
4 3 1 2
-Q or -A(Q ) or -B(Q ) or -B(AQ )2 2
wherein
A is -NH-(CH ) -CO- or -OH-(CH ) -CO-2 n 2 n
where n is 2-6,
B is -HN-CH -(CH ) -CH(NH)-(CH ) -CO-
2 2 m 2 n
where
m 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 when R is Lys or Orn respectively, and in the group -B(AQ ) , the -CO moiety6 6 2 2
of A being bonded to an amino group on B,
1
Q is D or L-melphalanyl, cyclopropanecarbonyl, aziridine-2-carbonyl, epoxyalkyl or
1,4-naphthoquinone-5-oxycarbonyl-ethyl,
2 1,
Q is Q 2-anthraquinonyl-methylenoxy or doxorubicinyl,
3 2
Q is Q , mitomicinyl, esperamycinyl or methotrexoyl,
4 1
Q is Q or methotrexoyl,
and pharmaceutically acceptable salts thereof.
2
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