JP2018515088A5 - - Google Patents

Info

Publication number

JP2018515088A5

JP2018515088A5 JP2017557346A JP2017557346A JP2018515088A5 JP 2018515088 A5 JP2018515088 A5 JP 2018515088A5 JP 2017557346 A JP2017557346 A JP 2017557346A JP 2017557346 A JP2017557346 A JP 2017557346A JP 2018515088 A5 JP2018515088 A5 JP 2018515088A5

Authority

JP

Japan

Prior art keywords

fusion protein

seq

amino acid

insulin

acid sequence

Prior art date

2016-04-28

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 102000037865 fusion proteins Human genes 0.000 claims 21
• 108020001507 fusion proteins Proteins 0.000 claims 21
• 150000001413 amino acids Chemical group 0.000 claims 17
• 239000008194 pharmaceutical composition Substances 0.000 claims 10
• 108090000765 processed proteins & peptides Proteins 0.000 claims 9
• 102000004877 Insulin Human genes 0.000 claims 8
• 108090001061 Insulin Proteins 0.000 claims 8
• 239000000710 homodimer Substances 0.000 claims 4
• 229910052739 hydrogen Inorganic materials 0.000 claims 4
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 3
• 229940079288 Insulin receptor agonist Drugs 0.000 claims 3
• 239000004480 active ingredient Substances 0.000 claims 3
• KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
• 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 2
• 229940089838 Glucagon-like peptide 1 receptor agonist Drugs 0.000 claims 2
• 239000003814 drug Substances 0.000 claims 2
• MGXWVYUBJRZYPE-YUGYIWNOSA-N incretin Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(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](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(O)=O)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=1C=CC(O)=CC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=C(O)C=C1 MGXWVYUBJRZYPE-YUGYIWNOSA-N 0.000 claims 2
• 239000000859 incretin Substances 0.000 claims 2
• 230000004048 modification Effects 0.000 claims 2
• 238000012986 modification Methods 0.000 claims 2
• GNZCSGYHILBXLL-UHFFFAOYSA-N n-tert-butyl-6,7-dichloro-3-methylsulfonylquinoxalin-2-amine Chemical group ClC1=C(Cl)C=C2N=C(S(C)(=O)=O)C(NC(C)(C)C)=NC2=C1 GNZCSGYHILBXLL-UHFFFAOYSA-N 0.000 claims 2
• 229910052757 nitrogen Inorganic materials 0.000 claims 2
• 229910052698 phosphorus Inorganic materials 0.000 claims 2
• 229940124597 therapeutic agent Drugs 0.000 claims 2
• KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
• 101000976075 Homo sapiens Insulin Proteins 0.000 claims 1
• 101500025353 Homo sapiens Insulin A chain Proteins 0.000 claims 1
• 101500025354 Homo sapiens Insulin B chain Proteins 0.000 claims 1
• 229930195725 Mannitol Natural products 0.000 claims 1
• 125000000729 N-terminal amino-acid group Chemical group 0.000 claims 1
• 239000006172 buffering agent Substances 0.000 claims 1
• 235000015165 citric acid Nutrition 0.000 claims 1
• 206010012601 diabetes mellitus Diseases 0.000 claims 1
• PBGKTOXHQIOBKM-FHFVDXKLSA-N insulin (human) Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 PBGKTOXHQIOBKM-FHFVDXKLSA-N 0.000 claims 1
• 239000007951 isotonicity adjuster Substances 0.000 claims 1
• 239000000594 mannitol Substances 0.000 claims 1
• 235000010355 mannitol Nutrition 0.000 claims 1
• 239000000203 mixture Substances 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 102000040430 polynucleotide Human genes 0.000 claims 1
• 108091033319 polynucleotide Proteins 0.000 claims 1
• 239000002157 polynucleotide Substances 0.000 claims 1
• 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
• 229920000053 polysorbate 80 Polymers 0.000 claims 1
• 229940068968 polysorbate 80 Drugs 0.000 claims 1
• 239000004094 surface-active agent Substances 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1