US 5,393,869 AGranted

Parathyroid hormone derivatives

AssigneeTakeda Chemical Industries, Ltd.

InventorsShizue Nakagawa, Tsunehiko Fukuda, Masahiro Kawase, Iwao Yamazaki

Life of this patent

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Abstract

Disclosed are peptides and salts thereof represented by general formul ##STR1## wherein R.sub.1 represents Ser or Aib; R.sub.2 represents Met or a naturally occurring hydrophobic amino acid; R.sub.3 represents Leu, Ser, Lys or an aromatic amino acid; R.sub.4 represents Gly or a D-.alpha.-amino acid; R.sub.5 represents Lys or Leu; R.sub.6 represents Met or a naturally occurring hydrophobic amino acid; R.sub.7 represents Glu or a basic amino acid; R.sub.8 represents Val or basic amino acid; R.sub.9 represents Trp or 2-(1,3-dithiolane-2-yl)Trp; R.sub.10 represents Arg or His; R.sub.11 represents Lys or His; R.sub.12 represents Lys, Gln or Leu; and R.sub.13 represents Phe or Phe-NH.sub.2 ; except that simultaneously R.sub.1 consists of Ser, R.sub.2 consists of Met, R.sub.3 consists of Leu, R.sub.4 consists of Gly, D-Ala or D-Pro, R.sub.5 consists of Lys, R.sub.6 consists of Met, R.sub.7 consists of Glu, R.sub.8 consists of Val, R.sub.9 consists of Trp, R.sub.10 consists of Arg, R.sub.11 consists of Lys and R.sub.12 consists of Lys. The parathyroid hormone (1-34) analogs are useful in hormone therapy.

Claims12

Dependent claims

(twice amended) A peptide or salts thereof having the formula ##STR4## wherein R.sub.1 represents Ser or Aib;

R.sub.2 represents Met or a naturally occurring hydrophobic amino acid;
R.sub.3 represents Leu, Ser, Lys or an aromatic amino acid;
R.sub.4 represents Gly or a D-.alpha.-amino acid;
R.sub.5 represents Lys or Leu;
R.sub.6 represents Met or a naturally occurring hydrophobic amino acid;
R.sub.7 represents Glu or a basic amino acid;
R.sub.8 represents Val or a basic amino acid;
R.sub.9 represents Trp or 2-(1,3-dithiolane-2-yl)Trp;
R.sub.10 represents Arg or His;
R.sub.11 represents Lys or His;
R.sub.12 represents Lys, Gln or Leu;
and R.sub.13 represents Phe or Phe-NH.sub.2 ;
with the exclusion of:
(1) the peptide or salt thereof wherein R.sub.1 is Ser, R.sub.2 is Met, R.sub.3 is Leu, R.sub.4 is Gly, R.sub.5 is Lys, R.sub.6 is Met, R.sub.7 is Glu, R.sub.8 is Val, R.sub.9 is Trp, R.sub.10 is Arg, R.sub.11 is Lys and R.sub.12 is Lys;
(2) the peptide or salt thereof wherein R.sub.1 is Ser, R.sub.2 is Met, R.sub.3 is Leu, R.sub.4 is D-Ala, R.sub.5 is Lys, R.sub.6 is Met, R.sub.7 is GlU, R.sub.8 is Val, R.sub.9 is Trp, R.sub.10 is Arg, R.sub.11 is Lys and R.sub.12 is Lys;
and
(3) the peptide or salt thereof wherein R.sub.1 is Ser, R.sub.2 is Met. R.sub.4 is D-Pro, R.sub.5 is Lys, R.sub.6 is Met, R.sub.7 is Glu, R.sub.8 is Val, R.sub.9 is Trp, R.sub.10 is Arg, R.sub.11 is Lys and R.sub.12 is Lys.

14 more elements

Dependencies are inferred from the claim text.

Facts

Application: 07/765,373Filed 25 Sep 1991
Priority: JP 2-25749028 Sep 1990
Granted: 28 Feb 1995
Term ends: Not estimatedThe source records don’t support an estimate.

Classification12 codes

C07K 14/635
Hormones: parathyroid hormone, i.e. parathormone; Parathyroid hormone-related peptides
A61P 3/02
Drugs for disorders of the metabolism: nutrients, e.g. vitamins, minerals
A61P 5/12
Of the posterior pituitary hormones, e.g. oxytocin, ADH: for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
A61P 9/12
Drugs for disorders of the cardiovascular system: antihypertensives