Merck + Co., Inc.

Michael Rosenblatt

Michael Chorev

Ruth F Nutt

Eliahu Roubini

Lynn H Caporale

Le T Duong

Michael P Caulfield

Jay J Levy

Roberta L McKee

The present invention relates to the use of peptide analogues as inhibitors of their respective naturally occurring peptides. The structure of the peptide analogues is exemplified by an internal region of the N-terminus of humoral hypercalcemic factor hHCF, and truncations thereof: hHCF(14-34)NH.sub.2, hHCF(13-34)NH.sub.2, hHCF(12-34)NH.sub.2, hHCF(11-23)NH.sub.2, hHCF(10-34)NH.sub.2, hHCF(9-34)NH.sub.2, hHCF(8-34)NH.sub.2 and various amino acid substitutions.

Humoral hypercalcemic factor antagonists

The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone (PTH), wherein Lys.sup.13 is substituted to increase the biological activity of the PTH analogues. Thus, there are disclosed peptides having the formulae:

Antagonists with position 13 modification

The present invention relates to the use of peptide analogues as inhibitors of their respective naturally occurring peptides. The structure of the peptide hormone analogues is exemplified by human humoral hypercalcemic factor (hHCF), wherein Lys.sup.13 or Lys.sup.11 is modified on the epsilon-amino group by biotin so as to produce HCF analogues which can inhibit the action of HCF.

Humoral hypercalcemic factor antagonists modified at position 13 by

The present invention relates to the use of peptide analogues as inhibitors of their respective naturally occurring peptides. The structure of the peptide hormone analogues is exemplified by human humoral hypercalcemic factor (hHCF), wherein Lys.sup.13 is modified so as to produce HCF analogues which can inhibit the action of HCF.

Humoral hypercalcemic factor antagonists with modification at position

The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone wherein Phe.sup.7 is substituted by NMePhe, D-Phe, desamino Phe, or Met.sup.8 is substituted by NMeMet.

Parathyroid hormone antagonists with enhanced metabolic properties

The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone wherein Gly.sup.12 is substituted by D-Trp, L-Trp, L- or D- alpha- or beta-naphthylalanine, or D- or L- alpha-MeTrp.

Parathyroid hormone antagonists

The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone and methods of synthesis of such analogues. The structure of the peptide hormone analogues is exemplified by parathyroid hormone wherein Trp.sup.23 is substituted by L-Phe or other hydrophobic amino acids such as Leu, Nle, Val, Tyr, beta-napthylalanine and alpha-napthylalanine.

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Ardmore, PA, United States of America

Michael Rosenblatt