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US 2006/0135434 A1Published application
New peptides
OwnerMari Kulsethinventor
Life of this patent
Estimating the term…
Abstract
The present invention relates to new peptides for targeting to vascular endothelial growth factor receptor 2, VEGFR-2. The invention further relates to their use in therapeutically effective treatment as well as for diagnostic imaging techniques.
Claims11
A targetable therapeutically active and/or diagnostic agent of formula (III)
- V-L-Z (III)
- wherein the vector V is a peptide comprising the amino acid sequence of formula (I)
- Z1-Arg-X2-X3-Ile-X5-X6-X7-X8-X9-Z2-Y1 (I)
- or formula (II)
- Z1-Arg-Val(Arg/Lys)Ile-Asp-Gly-X7-Pro-X9-Z2-Y1 (II)
- wherein
- X2 is an amino acid selected from the group Val, Leu, Ile and Tyr
- X3 is an amino acid selected from the group Arg, Lys, Ile and Asn
- X5 is an amino acid selected from the group A sp and Asn
- X6 is an amino acid selected from the group Gly, Asn and Gln
- X7 is an amino acid selected from the group Ala, Met, Gln, Arg, Glu and Val,
- X8 is an amino acid selected from the group Pro, Gly, Ser and Arg
- X9 is an amino acid selected from the group Ala, Met, Gln, Arg, Gly and Val
- Z1 represent an amino acid residue capable of forming a disulphide bond, preferably a cysteine or a homocysteine residue, or a residue capable of forming a thioether preferably the residue is Q-C(═O) wherein Q represents —(CH2)n or —(CH2)n—C6H4 where n represents a positive integer 1 to 10 or is absent and
- Z2 represent an amino acid residue capable of forming a disulphide bond, preferably a cysteine or a homocysteine residue or is absent
- Y1 represents 1-10 amino acids or is absent
- L represents a bond, a spacer or a linker and
- Z represents an antineoplastic agent, a reporter or a group that optionally can carry an imaging moiety M.
15 more elements
A peptide comprising the amino acid sequence of formula (II)
- Z1-Arg-Val(Arg/Lys)Ile-Asp-Gly-X7-Pro-X9-Z2-Y1 (II)
- wherein
- X7 is an amino acid selected from the group Ala, Met, Gln, Arg, Glu and Val,
- X9 is an amino acid selected from the group Ala, Met, Gln, Arg, Gly and Val
- Z1 represent an amino acid residue capable of forming a disulphide bond, preferably a cysteine or a homocysteine residue, or a residue capable of forming a thioether preferably the residue is Q-C(═O) wherein Q represents —(CH2)n or —(CH2)n—C6H4 where n represents a positive integer 1 to 10 or is absent and
- Z2 represent an amino acid residue capable of forming a disulphide bond, preferably a cysteine or a homocysteine residue or is absent
- Y1 represents 1-10 amino acids or is absent
- or pharmaceutically acceptable salts thereof.
5 more elements
A peptide comprising the amino acid sequence
- Cys-Arg-Val-Arg-Ile-Asp-Gly-Ala-Pro-
- (SEQ ID NO 1)
- Ala-Cys,,
- Cys-Arg-Val-Arg-Ile-Asp-Asn-Met-Pro-
- (SEQ ID NO 2)
- Met-Cys,,
- Cys-Arg-Val-Arg-Ile-Asn-Gly-Gln-Pro-
- (SEQ ID NO 3)
- Gln-Cys,,
- Cys-Arg-Val-Lys-Ile-Asp-Gly-Arg-Pro-
- (SEQ ID NO 4)
- Met-Cys,,
- Cys-Arg-Leu-Lys-Ile-Asp-Gly-Met-Pro-
- (SEQ ID NO 5)
- Arg-Cys,,
- Cys-Arg-Ile-Lys-Ile-Asp-Gly-Glu-Gly-
- (SEQ ID NO 6)
- Gln-Cys,,
- Cys-Arg-Val-Tyr-Ile-Asp-Gly-Val-Ser-
- (SEQ ID NO 7)
- Val-Cys,,
- Cys-Arg-Val-Ile-Ile-Asp-Gly-Arg-Arg-
- (SEQ ID NO 8)
- Met-Cys,,
- Cys-Arg-Tyr-Asn-Ile-Asp-Gly-Arg-Pro-
- (SEQ ID NO 9)
- Gln-Cys,
- or
- Cys-Arg-Ile-Arg-Ile-Asp-Gln-Arg-Pro-
- (SEQ ID NO 10)
- Ala-Cys,.
28 more elements
A pharmaceutical composition comprising an effective amount of a compound of general Formula (III) or a salt thereof, together with one or more pharmaceutically acceptable adjuvants, excipients or diluents.
Dependencies are inferred from the claim text.