http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-2820038-A1

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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
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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

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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID127796630
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID1983
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128492838
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128185245
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID791
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID95194
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID11025495
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID342
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128006268
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID87275422
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226394385
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID8761
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID716901
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226443756
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID2756092
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID736301
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID243
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID127894603
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226745129
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226736319
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226393819
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID6274
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128926318
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226517761
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID27282473
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID2723939
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID13529
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID7184
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID135943241
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128121089
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226570840
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID18611905
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID57365414
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128833854

Total number of triples: 335.