JP2022025114A5 - - Google Patents

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Publication number

JP2022025114A5

JP2022025114A5 JP2021178501A JP2021178501A JP2022025114A5 JP 2022025114 A5 JP2022025114 A5 JP 2022025114A5 JP 2021178501 A JP2021178501 A JP 2021178501A JP 2021178501 A JP2021178501 A JP 2021178501A JP 2022025114 A5 JP2022025114 A5 JP 2022025114A5

Authority

JP

Japan

Prior art keywords

group

pharmaceutical composition

composition according

region

exendin

Prior art date

2021-11-01

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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• 239000008194 pharmaceutical composition Substances 0.000 claims 15
• NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 14
• JUFFVKRROAPVBI-PVOYSMBESA-N chembl1210015 Chemical class C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=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](CCCCN)C(=O)N[C@@H](CC(=O)N[C@H]1[C@@H]([C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@]3(O[C@@H](C[C@H](O)[C@H](O)CO)[C@H](NC(C)=O)[C@@H](O)C3)C(O)=O)O2)O)[C@@H](CO)O1)NC(C)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)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)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 JUFFVKRROAPVBI-PVOYSMBESA-N 0.000 claims 10
• 108060003951 Immunoglobulin Proteins 0.000 claims 9
• 102000018358 immunoglobulin Human genes 0.000 claims 9
• 229920000642 polymer Polymers 0.000 claims 8
• 102000004877 Insulin Human genes 0.000 claims 7
• 108090001061 Insulin Proteins 0.000 claims 7
• 229940125396 insulin Drugs 0.000 claims 7
• 125000001151 peptidyl group Chemical group 0.000 claims 7
• 108090000765 processed proteins & peptides Proteins 0.000 claims 7
• 230000003248 secreting effect Effects 0.000 claims 7
• 108010011459 Exenatide Proteins 0.000 claims 6
• 229960001519 exenatide Drugs 0.000 claims 6
• 125000003277 amino group Chemical group 0.000 claims 5
• 208000010706 fatty liver disease Diseases 0.000 claims 5
• 229940079593 drug Drugs 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 3
• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
• 239000002202 Polyethylene glycol Substances 0.000 claims 2
• 102100021538 Protein kinase C zeta type Human genes 0.000 claims 2
• 125000003172 aldehyde group Chemical group 0.000 claims 2
• 229910052799 carbon Inorganic materials 0.000 claims 2
• 208000019425 cirrhosis of liver Diseases 0.000 claims 2
• 230000000694 effects Effects 0.000 claims 2
• 230000004130 lipolysis Effects 0.000 claims 2
• 229920001223 polyethylene glycol Polymers 0.000 claims 2
• 108010050991 protein kinase C zeta Proteins 0.000 claims 2
• KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical class O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims 2
• ZJIFDEVVTPEXDL-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) hydrogen carbonate Chemical compound OC(=O)ON1C(=O)CCC1=O ZJIFDEVVTPEXDL-UHFFFAOYSA-N 0.000 claims 1
• KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 1
• ZTQSAGDEMFDKMZ-UHFFFAOYSA-N Butyraldehyde Chemical group CCCC=O ZTQSAGDEMFDKMZ-UHFFFAOYSA-N 0.000 claims 1
• 229920002101 Chitin Polymers 0.000 claims 1
• 229920002307 Dextran Polymers 0.000 claims 1
• 102000004190 Enzymes Human genes 0.000 claims 1
• 108090000790 Enzymes Proteins 0.000 claims 1
• 102000018711 Facilitative Glucose Transport Proteins Human genes 0.000 claims 1
• 108010027279 Facilitative Glucose Transport Proteins Proteins 0.000 claims 1
• NQTADLQHYWFPDB-UHFFFAOYSA-N N-Hydroxysuccinimide Chemical compound ON1C(=O)CCC1=O NQTADLQHYWFPDB-UHFFFAOYSA-N 0.000 claims 1
• 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
• NBBJYMSMWIIQGU-UHFFFAOYSA-N Propionic aldehyde Chemical group CCC=O NBBJYMSMWIIQGU-UHFFFAOYSA-N 0.000 claims 1
• 101150116689 Slc2a2 gene Proteins 0.000 claims 1
• 239000004480 active ingredient Substances 0.000 claims 1
• 229920002988 biodegradable polymer Polymers 0.000 claims 1
• 239000004621 biodegradable polymer Substances 0.000 claims 1
• 230000007882 cirrhosis Effects 0.000 claims 1
• 229920001577 copolymer Polymers 0.000 claims 1
• 206010012601 diabetes mellitus Diseases 0.000 claims 1
• 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 150000004676 glycans Chemical class 0.000 claims 1
• 125000000487 histidyl group Chemical group [H]N([H])C(C(=O)O*)C([H])([H])C1=C([H])N([H])C([H])=N1 0.000 claims 1
• 235000003642 hunger Nutrition 0.000 claims 1
• 229920002674 hyaluronan Polymers 0.000 claims 1
• 229960003160 hyaluronic acid Drugs 0.000 claims 1
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
• FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 claims 1
• 150000002632 lipids Chemical class 0.000 claims 1
• 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 1
• 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
• 229920001583 poly(oxyethylated polyols) Polymers 0.000 claims 1
• 229920001451 polypropylene glycol Polymers 0.000 claims 1
• 229920001282 polysaccharide Polymers 0.000 claims 1
• 239000005017 polysaccharide Substances 0.000 claims 1
• 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
• 230000002265 prevention Effects 0.000 claims 1
• XANRGTLFBAJYDA-UHFFFAOYSA-N propanoic acid;pyrrolidine-2,5-dione Chemical compound CCC(O)=O.O=C1CCC(=O)N1 XANRGTLFBAJYDA-UHFFFAOYSA-N 0.000 claims 1
• 230000037351 starvation Effects 0.000 claims 1
• 230000007863 steatosis Effects 0.000 claims 1
• 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
• -1 succinimidyl carboxylmethyl Chemical group 0.000 claims 1
• 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
• 229920002554 vinyl polymer Polymers 0.000 claims 1