Sandoz Gmbh

Novartis Ag

Janos Pless

Wilfried Bauer

Rainer Albert

Francois Cardinaux

Edmond Sandrin

Rene Huguenin

Eric Paul Krenning

Steven W Lamberts

Monika Mergler

Francedillaois Cardinaux

Walter Prikoszovich

Jean H Feyen

Robert H Buck

Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.

Chelated somatostatin peptides and complexes thereof, pharmaceutical

Use of certain complexed somatostatin peptides for the invivo imaging of

A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.

Polypeptide derivatives

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

Peptide derivatives selected from (i) a calcitonin peptide and a LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, and (ii) a calcitonin peptide modified by at least one formyl and/or at least C.sub.3-5 alkyl attached to an amino group other than a N-terminal amino group, and (iii) a calcitonin peptide modified by a combination of said substituents, with the provisos that

Calcitonin derivatives

Somatostatin analogues and derivatives in free form or in pharmaceutically acceptable salt or complex form are useful for treating degenerative and inflammatory processes in bone or catilage, e.g. arthritic conditions or diseases.

Treatment of arthritis

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

Somatostatine derivatives of the general formula ##STR1## wherein either (a)

Somatostatine derivatives

Straight-chain or mono-cyclicpolypeptides comprising a heptapeptide moiety, said moiety having in the 1-position (N-terminal) an .alpha.-N-phenylalkylated, optionally ring-substituted phenylalanine residue, in the 2-position a cysteine residue, in the 3-position an optionally ring-substituted phenylalanine residue, in the 4-position an optionally benzene-ring-substituted tryptophan residue, in the 5-position an optionally .epsilon.-N-alkylated lysine residue and in the 7-position (C-terminal) a cysteine or cysteinol residue the S-atoms of the cysteine residue at the 2-position and the cysteine or cysteinol residue at the 7-position being linked together in the case of the mono-cyclic polypeptides to form an -S-S-bridge, whereby the residues at the 1-, 2-, 4-, 6-, and 7-positions of said heptapeptide moiety may each be in the (L)- or (D)-configuration and the residues at the 4-, 5- and 6-positions of said heptapeptide moiety may each be optionally .alpha.-N-alkylated, said polypeptides being in free or protected form, as well as salt forms and complexes thereof. Subject compounds are useful as pharmaceuticals, e.g. as GH-secretion inhibitors.

Polypeptides, processes for their production, pharmaceutical

The invention provides polypeptides of formula I,

Organic compounds

N-Acyl-polypeptides comprising the basic sequence ##STR1## wherein 'Acyl' is the acyl residue of an organic or inorganic acid; A is H or alkyl; &gt;N--CH(Z)--CO-- and E are the residues of natural .alpha.-amino acids or corresponding (D)-amino acids; C is --Trp-- or --(D)Trp--; F is a terminal grouping; and Y.sub.1 and Y.sub.2 are each H or together are a direct bond; as well as their salt forms and complexes.

N-Acyl-polypeptides and processes for the production thereof

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.

Novel pentapeptides, processes for their production, pharmaceutical

Straight-chain and mono-cyclic polypeptides containing the basic sequence ##STR1## wherein X is an amino acid residue, the residues in the 1- and 6-positions being linked by an --S--S-- bridge when the polypeptide is monocyclic, have pharmacological, in particular GH--, gastric- and pancreatic-secretion inhibiting activity.

The invention provides polypeptides of the formula,

Growing community of inventors

Basel, Switzerland

Janos Pless