Patent application number | Description | Published |
20120329711 | GLP-1 RECEPTOR AGONIST COMPOUNDS WITH A MODIFIED N-TERMINUS - The invention relates to GLP-1 receptor agonist compounds with a modified N-terminus. The compounds are of the formula Chem. 1: Y—Z—P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y—Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-1 A (1-37). The invention also relates to derivatives of these compounds, in particular compounds with one or more albumin binding side chains capable of protracting the duration of action in vivo of these compounds. The peptides and derivatives of the invention have a good potency, a protracted pharmacokinetic profile, are stable against degradation by gastro intestinal enzymes, and/or have a high oral bioavailability. These properties are of importance in the development of GLP-1 receptor agonist compounds for subcutaneous, intravenous, and/or in particular oral administration. The invention also relates to intermediate products for use in the preparation of the GLP-1 receptor agonist compounds of the invention. | 12-27-2012 |
20130059781 | Long-Acting Gastrin Derivatives - The present invention relates to gastrin derivatives comprising gastrin or an analogue or fragment thereof and a derivatisation group and therapeutic use thereof. | 03-07-2013 |
20130288960 | Double-Acylated GLP-1 Derivatives - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1 (7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: Chem.: HOOC—(CH | 10-31-2013 |
20140018290 | LEPTIN DERIVATIVES - The invention relates to Leptin derivatives, compositions and therapeutic use there-of. | 01-16-2014 |
20150148521 | INSULINS WITH AN ACYL MOIETY COMPRISING REPEATING UNITS OF ALKYLENE GLYCOL CONTAINING AMINO ACIDS - Acylated insulins wherein an acyl moiety is attached to the parent insulin and wherein said acyl moiety comprises repeating units of alkylene glycol containing amino acids and wherein there is only one lysine residue (K & Lys) in the parent insulin have satisfactory properties when administered pulmonary. | 05-28-2015 |
20150210747 | PROTEASE STABILIZED ACYLATED INSULIN ANALOGUES - Novel acylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. | 07-30-2015 |
20150210748 | PROTEASE STABILIZED ACYLATED INSULIN ANALOGUES - Novel acylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. | 07-30-2015 |
20150344540 | NOVEL GLP-1 RECEPTOR AGONISTS WITH CHOLESTEROL EFFLUX ACTIVITY - The present invention provides novel glucagon-like protein-1 (GLP-1) receptor agonist compounds that promote cholesterol efflux. The ABCA1-mediated cholesterol efflux present invention also provides compositions comprising the novel glucagon-like protein-1(GLP-1) receptor agonist compounds, and relates to the use of said compounds in therapy, to methods of treatment comprising administration of said compounds to patients, and to the use of said compounds in the manufacture of medicaments. | 12-03-2015 |