Somatostatin prodrugs
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorsAmnon Hoffman, Chaim Gilon, Adi Klinger, Johnny Naoum
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Abstract
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.
Claims19
A somatostatin prodrug comprising a lipophilic carbamate derivative of a somatostatin peptide or peptide analog, wherein the lipophilic carbamate is having a formula selected from the group consisting of:
- wherein R1 is a primary alkyl having the formula n-CnH2n+1, wherein n is in the range of 3 to 15.
A method of increasing the permeability and bioavailability of a somatostatin peptide or peptide analog, comprising masking at least one terminal amine or side-chain nitrogen atom of the somatostatin peptide or analog to form a lipophilic carbamate somatostatin prodrug, wherein the lipophilic carbamate is having a formula selected from the group consisting of:
- wherein R1 is a primary alkyl having the formula n-CnH2n+1 wherein n is in the range of 3 to 15.
Dependencies are inferred from the claim text.