GRF analogs VII

Details GRF analogs VII GRF analogs VII

1987-05-22

1991-03-26

Doll, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530324, 530345, A61K 3743, C07K 710

Patent

active

050029312

ABSTRACT:
The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which have the sequence: (B)R.sub.1 -R.sub.2 -R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-(Q.sub.1)R.sub.10 - Arg-R.sub.12. (Q.sub.2)R.sub.13 -Leu-R.sub.15 -Gln-Leu-Ser-(Q.sub.3)Ala-Arg. R.sub.21 -(Q.sub.4)R.sub.22 -Leu-Gln-Asp-Ile-R.sub.27 -R.sub.28 -Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-R.sub.42 -R.sub.43 -R.sub.44 wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His; B is H, C.sup.a Me, N.sup.a Me, desamino, Ac or For; R.sub.2 is Ala, D-Ala, NMA or D-NMA; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, Lys, Arg, Asp or Gln; R.sub.10 is Tyr, D-Tyr or Phe; R.sub.12 is Arg or Lys; R.sub.13 is Ile, Val, Leu or Ala; R.sub.15 is Gly or Ala; R.sub.21 is Lys, D-Lys or D-Arg; R.sub.22 is Leu, Ile, Ala or Val; R.sub.27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn or Ser; R.sub.42 is Phe, Ala or Val; R.sub.43 is Asn or Arg; R.sub.44 is a natural amino acid; Q.sub.1 -Q.sub.4 are either H or C.sup.a Me, provided however that any or all of the residues between R.sub.30 and R.sub.44, inclusive, may be deleted.
These peptides as well as their nontoxic salts may also be used diagnostically.

REFERENCES:
patent: 4518586 (1985-05-01), Rivier et al.
patent: 4528190 (1985-07-01), Vale, Jr. et al.
patent: 4595676 (1986-06-01), Spiess et al.
patent: 4689318 (1987-08-01), Kaiser et al.
patent: 4784987 (1988-11-01), Rivier et al.
patent: 4801456 (1989-01-01), Drengler
Heiman et al., Endocrinology, vol. 116, No. 1, pp. 410-415 (1985).

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