http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-2820038-A1
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3120ae9cab5bb4831f0cc16288966367 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K14-575 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K14-605 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-642 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-605 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-26 |
filingDate | 2013-02-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_089d2f61d632a03a19d5ca3c8580e4fe |
publicationDate | 2015-01-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | EP-2820038-A1 |
titleOfInvention | Glp-1 prodrugs |
abstract | The invention relates to a GLP-1 prodrug of the general formula I: R1-(NHXaa1)- Xaa2-(OHis)-(GLP-1peptide) (Formula I), wherein GLP-1 peptide is GLP-1(8-37) (SEQ ID NO: 1) or an analogue thereof having a maximum of nineamino acid changes as compared to GLP-1(8-37), R1 is lower alkyl, (NHXaa1) is an amino acid, Xaa2 is an amino acid, and (OHis) is a radical of imidazole-lactic acid; or a pharmaceutically acceptable salt, amide, or ester of the prodrug. The invention also relates to specific GLP-1 parent drugs of the general formula II: (HOHis)-(GLP-1peptide) (Formula II), as well as specific intermediate products. The invention furthermore relates to a method of achieving release in vivo of an active and stabilised GLP-1 parent drug of the general formula II: (HOHis)-(GLP-1 peptide), by administering a GLP-1 prodrug; as well as to such GLP-1 prodrug, and such GLP-1 parent drug, respectively, for use as a medicament, in particular for use in the treatment and/or prevention of all forms of diabetes and related diseases. The prodrug may be used to alter the PK and/or absorption profile of the drug, for example to a desirable bell-shaped curve. The parent drug has a good biological activity, and is stabilised against degradation by DPP- IV. |
priorityDate | 2012-03-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 335.