JP2016512213A5 - - Google Patents

Info

Publication number

JP2016512213A5

JP2016512213A5 JP2015562166A JP2015562166A JP2016512213A5 JP 2016512213 A5 JP2016512213 A5 JP 2016512213A5 JP 2015562166 A JP2015562166 A JP 2015562166A JP 2015562166 A JP2015562166 A JP 2015562166A JP 2016512213 A5 JP2016512213 A5 JP 2016512213A5

Authority

JP

Japan

Prior art keywords

less

peptide

peg

receptor

glp

Prior art date

2014-03-13

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Pending

Links

• Espacenet
• Global Dossier
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• 108090000765 processed proteins & peptides Proteins 0.000 claims 50
• 238000000034 method Methods 0.000 claims 14
• KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 7
• 239000004472 Lysine Substances 0.000 claims 7
• 230000000694 effects Effects 0.000 claims 7
• FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 6
• 108010063919 Glucagon Receptors Proteins 0.000 claims 6
• 102100040890 Glucagon receptor Human genes 0.000 claims 6
• 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 6
• 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 claims 6
• DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 5
• 150000001413 amino acids Chemical group 0.000 claims 5
• 102100040918 Pro-glucagon Human genes 0.000 claims 4
• 239000000203 mixture Substances 0.000 claims 4
• 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 3
• 102000051325 Glucagon Human genes 0.000 claims 3
• 108060003199 Glucagon Proteins 0.000 claims 3
• 102000008100 Human Serum Albumin Human genes 0.000 claims 3
• 108091006905 Human Serum Albumin Proteins 0.000 claims 3
• 239000000556 agonist Substances 0.000 claims 3
• MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 3
• 229960004666 glucagon Drugs 0.000 claims 3
• 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 3
• 102000004196 processed proteins & peptides Human genes 0.000 claims 3
• YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims 2
• 101001040075 Homo sapiens Glucagon receptor Proteins 0.000 claims 2
• 101001015516 Homo sapiens Glucagon-like peptide 1 receptor Proteins 0.000 claims 2
• 238000013262 cAMP assay Methods 0.000 claims 2
• 201000010099 disease Diseases 0.000 claims 2
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
• 238000002347 injection Methods 0.000 claims 2
• 239000007924 injection Substances 0.000 claims 2
• 239000003446 ligand Substances 0.000 claims 2
• 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
• 229920001184 polypeptide Polymers 0.000 claims 2
• GUOSQNAUYHMCRU-UHFFFAOYSA-N 11-Aminoundecanoic acid Chemical group NCCCCCCCCCCC(O)=O GUOSQNAUYHMCRU-UHFFFAOYSA-N 0.000 claims 1
• KXSKAZFMTGADIV-UHFFFAOYSA-N 2-[3-(2-hydroxyethoxy)propoxy]ethanol Chemical compound OCCOCCCOCCO KXSKAZFMTGADIV-UHFFFAOYSA-N 0.000 claims 1
• SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical group NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims 1
• 102000009027 Albumins Human genes 0.000 claims 1
• 108010088751 Albumins Proteins 0.000 claims 1
• 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
• 102000004127 Cytokines Human genes 0.000 claims 1
• 108090000695 Cytokines Proteins 0.000 claims 1
• 102000004190 Enzymes Human genes 0.000 claims 1
• 108090000790 Enzymes Proteins 0.000 claims 1
• 108091016366 Histone-lysine N-methyltransferase EHMT1 Proteins 0.000 claims 1
• 101000693243 Homo sapiens Paternally-expressed gene 3 protein Proteins 0.000 claims 1
• 102100026120 IgG receptor FcRn large subunit p51 Human genes 0.000 claims 1
• 101710177940 IgG receptor FcRn large subunit p51 Proteins 0.000 claims 1
• 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 1
• 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 1
• 101001040082 Mus musculus Glucagon receptor Proteins 0.000 claims 1
• 101001015515 Mus musculus Glucagon-like peptide 1 receptor Proteins 0.000 claims 1
• 208000008589 Obesity Diseases 0.000 claims 1
• 206010033307 Overweight Diseases 0.000 claims 1
• 102100025757 Paternally-expressed gene 3 protein Human genes 0.000 claims 1
• 239000002202 Polyethylene glycol Substances 0.000 claims 1
• 229960002684 aminocaproic acid Drugs 0.000 claims 1
• 229960002685 biotin Drugs 0.000 claims 1
• 235000020958 biotin Nutrition 0.000 claims 1
• 239000011616 biotin Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 229920000592 inorganic polymer Polymers 0.000 claims 1
• 235000020824 obesity Nutrition 0.000 claims 1
• 229920000620 organic polymer Polymers 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 229920001223 polyethylene glycol Polymers 0.000 claims 1
• 229920000642 polymer Polymers 0.000 claims 1
• 108020001580 protein domains Proteins 0.000 claims 1
• 102000004169 proteins and genes Human genes 0.000 claims 1
• 108090000623 proteins and genes Proteins 0.000 claims 1
• 102000005962 receptors Human genes 0.000 claims 1
• 108020003175 receptors Proteins 0.000 claims 1
• 210000002966 serum Anatomy 0.000 claims 1
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1