Diazaspiro, azepino and azabicyclo therapeutic peptides

Details Diazaspiro, azepino and azabicyclo therapeutic peptides Diazaspiro, azepino and azabicyclo therapeutic peptides

1998-06-03

2000-02-15

Woodward, Michael P.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

4 to 5 amino acid residues in defined sequence

530329, 514 17, 540484, C07K 700

Patent

active

060254718

ABSTRACT:
The present invention relates a number of novel peptide sequences which include a spirolactam, bicyclic or tricyclic peptidomimetic unit. The peptides disclosed herein exhibit binding to cardiac tissue and normalize cardiac pressure after administration, as well as diagnostic and therapeutic properties for certain neoplastic tissues. Importantly, these peptides do not release pituitary hormones such as corticotropin (ACTH) and growth hormone (GH), and are therefore devoid of certain unwanted side-effects. These peptides preferably have at least one lysine unit and at least one D-2-alkyl-trptophan unit.

REFERENCES:
C. Bowers, "Xenobiotic Growth Hormone Secretagogues: Growth Hormone Releasing Peptides" in Bercu BB, Walker RF editors, Growth Hormone Secretagogues, New York: Springer-Verlag, pp. 9-28 (1996).
V. De Gennaro Colonna, "Cardiac ischemia and impairment of vascular endothelium function in hearts from growth hormone-deficient rats: Protection by hexarelin", European Journal of Pharmacology, 334:201-207 (1997).
R. Deghenghi, "Small Peptides as Potent Releasers of Growth Hormone", Journal of Pediatric Endocrinology & Metabolism, 8:311-313 (1995).
R. Deghenghi, "The development of `impervious peptides` as growth hormone secretagogues", Acta Paediatr. Suppl., 423:85-7 (1997).

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