Analogs of human growth hormone-releasing hormone, their...

Details Analogs of human growth hormone-releasing hormone, their... Analogs of human growth hormone-releasing hormone, their...

2011-04-19

2011-04-19

Bradley, Christina (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

Reexamination Certificate

active

07928063

ABSTRACT:
Growth hormone-releasing hormone analogs having the amino acid sequence of the formula: Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser-Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2(I), wherein R11is hArg, Gab or Gap; R12is hArg, Orn, Gab or Gap; R20is hArg, hArg, Gab or Gap; R21is hArg, Orn, Gab or Gap; R29is D-Arg, hArg, Gab or Gap; and their pharmaceutically acceptable salts. Said peptides are potent and selective stimulators of GH release and they are highly resistant to enzymatic degradation. Said peptides are prepared using the solid phase synthesis method, by introducing suitable derivatives of lysine, 2,4-diaminobutyric acid or 2,3-diaminopropionic acid at appropriate positions in the peptide chain attached to a polymeric support, deprotecting side-chain amino groups and reacting free amino groups with a guanidinating agent, removing all remaining t-butyloxycarbonyl protective groups, and cleaving the synthesized peptide from the support, followed by purification and optionally, converting the peptide into a pharmaceutically acceptable salt.

REFERENCES:
patent: 5416073 (1995-05-01), Coy et al.
patent: 5792747 (1998-08-01), Schally et al.
patent: 6380358 (2002-04-01), Goodman et al.
Schwegler (“Influence on the Trypsin Activity by the Side Chain of Arginine Homologues,” Cellular and Molecular Life Sciences, 1976, 32, 1380-1).
Frohman et al. (“Dipeptidylpeptidase IV and Trypsin-like Enzymatic Degradation of Human Growth Hormone-releasing Hormone in Plasma,” J. Clin. Invest., 1989, 83, 1533-1540).
Campbell et al. (“Rational Design, Synthesis, and Biological Evaluation of Novel Growth Hormone Releasing Factor Analogues,” Biopolymers, 1995, 37, 67-88).
Izdebski et al. “New Potent hGH-RH Analogues with Increased Resistance to Enzymatic Degradation.” J. Peptide Science, 2002, 8, 289-296.
Witkowska et al. (“Tryptic Hydrolysis of hGH-RH(1-29)-NH2 Analogues Containing Lys or Orn in Positions 12 and 21,” J. Peptide Sci., 2001, 7, 166-172).

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