The present invention provides prodrugs of somatostatin peptide and peptide analogs that are tissue permeable and oral bioavailable and enable activity of the somatostatin analog at the circulation or target tissue after cleavage of charge-masking lipophilic moieties. Pharmaceutical compositions comprising these prodrugs and their use in therapy and diagnosis are also provided.

[Problem] To provide a glycosylated polypeptide having affinity to somatostatin receptors and, compared to somatostatins, having improved in-blood stability. [Solution] The glycosylated polypeptide is characterized by at least two amino acids in a somatostatin or an analog thereof being replaced by glycosylated amino acids.

The present invention provides prodrugs of somatostatin peptide and peptide analogs that are tissue permeable and oral bioavailable and enable activity of the somatostatin analog at the circulation or target tissue after cleavage of charge-masking lipophilic moieties. Pharmaceutical compositions comprising these prodrugs and their use in therapy and diagnosis are also provided.

Novel backbone-cyclized peptidomimetics of the general formula
cyclo[-P.sup.1-P.sup.2-P.sup.3-P.sup.4-P.sup.5-P.sup.6-P.sup.7-P.sup.8-T.sup.1-T.sup.2-] (I)
wherein the single elements T or P are -amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes. These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solidand solution phase synthetic strategy.

Disclosed are compositions and methods related to improving pharmacological properties of bioactive compounds targeting nervous system.

[Problem] To provide a glycosylated polypeptide having an affinity to somatostatin receptors, and, compared to somatostatins, having improved in-blood stability. [Solution] The glycosylated polypeptide is characterized by at least one amino acid in a somatostatin or an analog thereof being replaced with a glycosylated amino acid.

Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.

Novel backbone-cyclized peptidomimetics of the general formula

cyclo[-P.sup.1-P.sup.2-P.sup.3-P.sup.4-P.sup.5-P.sup.6-P.sup.7-P.sup.8-T.sup.1-T.sup.2-] (I)

wherein the single elements T or P are -amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes.

These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solidand solution phase synthetic strategy.

[Problem] To provide a glycosylated polypeptide having an affinity to somatostatin receptors, and, compared to somatostatins, having improved in-blood stability. [Solution] The glycosylated polypeptide is characterized by at least one amino acid in a somatostatin or an analogue thereof being replaced with a glycosylated amino acid.

Disclosed are compositions and methods related to improving pharmacological properties of bioactive compounds targeting nervous system.