Sandoz Gmbh

Francois Cardinaux

Janos Pless

Wilfried Bauer

Rene Huguenin

Edmond Sandrin

Rainer Albert

Monika Mergler

Walter Prikoszovich

Robert H Buck

The present invention provides a sugar derivative of a biologically active peptide, which derivative has a prolonged duration of action when compared to the non-sugar modified peptide, and contains at least on one of the amino acid units a sugar residue which is attached to an amino group thereof by a coupling other than a direct N-glycosidic bond, and additionally, when it is a condensation product of a carboxyl group containing sugar and a peptide with less than 8 amino acid units, by a coupling other than a direct amide bond.

Peptide derivatives

A compound of formula I ##STR1## wherein R is H or R'CO wherein R'CO is an acyl radical of a carboxylic acid,

Calcitonin derivatives

The invention provides polypeptides of formula I,

Organic compounds

Pentapeptides of formula I, ##STR1## wherein Z.sup.1 =H, CH.sub.3 or amidino; R.sub.1 =H or alkyl and R.sub.2 =H or R.sub.1 +R.sub.2 =--CH.sub.2 --CH.sub.2 --; R.sub.3 =m- or p--OH or -alkoxy; B=residue of a (D)-.alpha.-amino acid; R.sub.4 =H or alkyl; Z.sup.2 =optionally substituted phenyl; and E=.beta.-amino alcohol residue (whereby when Z.sup.1 =H or CH.sub.3, R.sub.4 =C.sub.3-4 -alkyl) as well as their esters and the acid addition salts and complexes of such peptides and esters. Compounds according to the invention have valuable pharmacological, in particular LH-secretion inhibiting activity.

Growing community of inventors

Reinach, Switzerland

Francois Cardinaux