http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CY-1120117-T1

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filingDate 2018-04-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5deead4c8a935970e0588b21d02f6f9f
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publicationDate 2018-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CY-1120117-T1
titleOfInvention GASTRINI'S MINI ANALOG, MORE SPECIFIED FOR USE IN DIAGNOSIS AND / OR CCK2 TUMOR TREATMENT TREATMENT
abstract It is an object of the present invention to provide a gastrin analogue which exhibits high uptake in CCK-2 positive receptor tumors with a very low concentration in the kidneys. This objective is accomplished according to the present invention by a PP-F11 mini-gastrin analogue having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y -Asp-Phe-NH2, where Y denotes an amino acid that replaces methionine and X denotes a peptide-bound group for the purpose of diagnosing and / or treating CCK-2 receptor-related diseases . In particular, very suitable compounds with respect to a high ratio of tumor to kidney are the mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine that can be readily oxidized which is a disadvantage for clinical application under GMP due to the forms that may occur. Consequently, the elimination of methionine at a lower affinity for oxidation which generally favors the ratio of tumor to kidney. In a preferred embodiment of the present invention methionine is replaced by norleucine. This so-called mini-gastrin PP-F11N currently has the best tumor-kidney ratio and is therefore the most promising candidate for clinical applications.
priorityDate 2013-11-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 37.