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US 6,555,521 B2Granted
Glucagon-like peptide-1 crystals
AssigneeEli Lilly and Company
InventorsRonald Norbert Hermeling, James Arthur Hoffmann, Chakravarthy Narasimhan
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Abstract
The invention provides individual tetragonal flat rod shaped or plate-like crystals of glucagon-like peptide-1 related molecules, processes for their preparation, compositions and methods of use. The crystal preparations exhibit extended time action in vivo and are useful for treating diabetes, obesity and related conditions.
Claims6
Crystals comprising zinc, and a GLP-1 analog wherein the crystals have a tetragonal flat rod shaped or plate-like morphology and the GLP-1 analog is a peptide of the formula:
- R1-X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Y-Gly-Gln-Ala-Ala-Lys-Z-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-R2 SEQ ID NO:2
- wherein:
- R1 is selected from the group consisting of L-histidine, D-histidine, desamino-histidine, 2-amino-histidine, beta-hydroxy-histidine, homohistidine, alpha-fluoromethyl-histidine, and alpha-methyl-histidine;
- X is selected from the group consisting of Ala, Gly, Val, Thr, Met, Ile, and alpha-methyl-Ala;
- Y is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly;
- Z is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly;
- and R2 is selected from the group consisting of NH2, and Gly-OH.
4 more elements
Dependencies are inferred from the claim text.