RU-2024133179-A - New short peptides, analogues of kisspeptin 54, and pharmaceutical compositions based on them for the treatment of male hypogonadism

Inventors

• Байрамов Алекбер Азизович
• Шабанов Петр Дмитриевич

Assignees

• федеральное государственное бюджетное учреждение "Национальный медицинский исследовательский центр имени В.А. Алмазова" Министерства здравоохранения Российской Федерации

Dates

Publication Date

20260505

Application Date

20241105

Claims (20)

1. 1. A new short peptide Kiss1-6X, an analogue of the Kisspeptin 54 protein, with affinity for the Kiss1R receptors, with the general formula
2. 1. NH2–Phe–Arg–Leu–Gly–Phe–Ser
3. 2. NH2–Phe–Arg–Leu–Gly–Phe–Ser–pGlu,
4. characterized by the amino acid sequence A1-A2-A3-A4-A5-X6, or a pharmaceutically acceptable salt thereof,
5. Where
6. X6 - amino acid D-serine (D-Ser); acetyl-D-serine (Ac-D-Ser);
7. A1 - aromatic a-amino acid phenylalanine, L- or D-phenylalanine;
8. A2 - α-amino acids L-Arginine (Arg), α-amino acids D-Arginine;
9. A3 - amino acid leucine (Leu), L- or D-leucine;
10. A4 - amino acid L- or D-glycine (Gly);
11. A5 - aromatic α-amino acid phenylalanine, L- or D-phenylalanine (Phe);
12. 2. A new short peptide Kiss1-6X according to claim 1, characterized in that pyroglutamic acid (pGlu); D-pyroglutamic acid (D-pGlu) or a pharmaceutically acceptable salt thereof is attached to the amino acid X6 - serine (Ser); D-serine (D-Ser); acetyl-D-serine (Ac-D-Ser).
13. 3. A pharmaceutical composition having Kisspeptin 54 agonist activity, containing an effective amount of peptides as the active agent of the composition from the formula of claims 1 and 2, and their pharmaceutically acceptable carrier.
14. 4. A pharmaceutical composition according to claim 3, intended for parenteral, oral or intranasal administration.
15. 5. A new short peptide Kiss1-8X, an analogue of the Kisspeptin 54 protein, with affinity for the Kiss1R receptors, with the general formula
16. 1. NH2–Phe–Arg–Leu–Gly–Phe–Ser–Asn–Trp
17. 2. NH2–Phe–Arg–Leu–Gly–Phe–Ser–Asn– pGlu
18. 3. NH2–Phe–Arg–Leu–Gly–Phe–Ser–Asp– pGlu,
19. characterized by the amino acid sequence A1-A2-A3-A4-A5-A6-A7-X8, or a pharmaceutically acceptable salt thereof,
20. where X8 is the amino acid L- or D-tryptophan (Trp);