Parathyroid hormone derivatives

Details Parathyroid hormone derivatives Parathyroid hormone derivatives

1993-03-16

1995-07-18

Schain, Howard E.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

25 or more amino acid residues in defined sequence

C07K 1400, C07K 400, A61K 3823

Patent

active

054342465

ABSTRACT:
Parathyroid hormone (PTH) derivatives represented by the general formula: ##STR1## or a salt thereof, wherein R.sub.1 represents Ser or a D-.alpha.-amino acid residue of 4 or less carbon atoms;
R.sub.2 represents a tetrapeptide chain which contains at least one water-soluble .alpha.-amino acid residue;
R.sub.3 represents a tripeptide chain which contains at least one water-soluble .alpha.-amino acid residue; and
R.sub.4 represents an aromatic amino acid residue or an amide thereof,
except that R.sub.1 is Ser when R.sub.2 is His-Leu-Asn-Ser, R.sub.3 is E-F-G
wherein E is Arg or His, F is Lys or His, G is Lys, Leu or Gln, are disclosed.
The parathyroid hormone derivatives of the present invention are stable and have high biological activity, therefore they are useful as drugs for bone diseases and the like.

REFERENCES:
patent: 4086196 (1978-04-01), Tregear
patent: 4086198 (1978-04-01), Tregear
patent: 4656250 (1987-04-01), Morita et al.
patent: 4968669 (1990-11-01), Rosenblatt
Reeve et al., British Medical J., 7 Jun. pp. 1340-1344 (1980).
Lehninger, "Principles of Biochemistry", Worth Pub. pp. 100-101 (1982).
Biochemistry, 17(16):3188-3191 (1978).
F. Cohen et al., The Journal of Biological Chemistry, 266(3):1997-2004 (1991).

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