http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2017114116-A1
Outgoing Links
Predicate | Object |
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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/C07K14-605 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C237-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C235-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-08 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C235-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-605 |
filingDate | 2015-04-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4821342d612e35406478646ac0b71d56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_daa66cc56588f122bf03e732f213e97b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_64b6310b715a10c7152b4c34e157d25e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e98777c090fe0572b11cb3dd471b802c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fb9e3b74e5b3c1b7852a226bf9493347 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a1d4af99aa5432aa5c4be8802be55a03 |
publicationDate | 2017-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | US-2017114116-A1 |
titleOfInvention | Double-Acylated GLP-1 Compounds |
abstract | The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO:1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from: Chem. 1: HOOC—C 6 H 4 -0-(CH 2 ) y —CO—*, and Chem. 2: HOOC—(CH 2 ) x —CO—*, wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of: Chem. 3: *—NH—CH(COOH)—(CH 2 ) 2 —CO—*, Chem. 4: *—NH—CH((CH 2 ) 2 —COOH)—CO—*, and/or Chem. 5: *—NH—(CH 2 ) 2 -[0-(CH 2 ) 2 ] k -0-[CH 2 ] n —CO—*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no other Lys residues, and the GLP-1(9-37) fragments thereof. The invention furthermore relates to an intermediate product comprising 3-carboxyphenoxy-nonanoic acid with a protection group at the carboxy group of the nonanoic acid, optionally via a linker. The derivatives have a very good potency and a long half-life which makes them potentially useful for, e.g., oral administration. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2023175037-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11604193-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-3783014-A4 |
priorityDate | 2014-04-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 1341.