PEPTIDES HAVING PHARMACOLOGICAL ACTIVITY FOR TREATING DISORDERS ASSOCIATED WITH ALTERED CELL MIGRATION, SUCH AS CANCER
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Abstract
Peptides and their functionally equivalent derivatives, in salified or non-salified form, with the general formula L1-X1—X2—X3—X4, wherein:
L1 is H, or acyl, or any natural or non-natural amino acid, optionally N-acylated, N-alkylated and/or Cα-alkylated;
X1 and X3, which are equal or different, are any natural or non-natural basic amino acid, optionally N-alkylated and/or Cα-alkylated;
X2 is any natural or non-natural amino acid, optionally N-alkylated and/or Cα-alkylated, with the proviso that it is not glycine and amino acids mono-substituted on the α carbon atom with a linear or cyclic alkyl group, from 1 to 10 carbon atoms, and amino acids mono-substituted on the α carbon atom with a linear or cyclic alkyl group containing 4 to 10 carbon atoms, or amino acids mono-substituted on the α carbon atom with an alkyl group containing 1 to 8 carbon atoms, optionally substituted with a carbamoyl, hydroxyl or aromatic group;
X4 is any natural or non-natural hydrophobic amino acid, optionally Cα-alkylated and/or amidated at the C-terminal end, or any hydrophobic amino alcohol, or a hydrophobic gem-diamine, optionally N′-alkylated or N′-acylated.
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Citations
28 Claims
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1-16. -16. (canceled)
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17. Peptides and their functionally equivalent derivatives, in salified or non-salified form, with the general formula L1-X1—
- X2—
X3—
X4, wherein;L1 is H, or acyl, Glu, Gln, optionally N-acylated or N-alkylated and/or Cα
-alkylated, Pro, hydroxy-Pro, Azt, Pip, pGlu, optionally N-acylated and/or Cα
-alkylated, Aib, Ac3c, Ac4c, Ac5c or Ac6c, optionally N-acylated or N-alkylated;X1 and X3, which are equal or different, optionally N-alkylated and/or Cα
-alkylated, are selected from Arg, Orn and Lys, optionally guanidinylated, and phenylalanine substituted in the meta or para positions with an amine or guanidine group;X2 is chosen from among Glu, Lys, optionally N-alkylated and/or Cα
-alkylated, Aib, Ac3c, Ac4c, Ac5c and Ac6c, optionally N-alkylated;X4 is chosen from among Phe, h-Phe, Tyr, Trp, 1-NaI, 2-NaI, h-1-NaI, h-2-NaI, Cha, Chg and Phg, optionally amidated and/or Cα
-alkylated. - View Dependent Claims (18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28)
- X2—
Specification