JP2015503554A5 - - Google Patents

Info

Publication number

JP2015503554A5

JP2015503554A5 JP2014550024A JP2014550024A JP2015503554A5 JP 2015503554 A5 JP2015503554 A5 JP 2015503554A5 JP 2014550024 A JP2014550024 A JP 2014550024A JP 2014550024 A JP2014550024 A JP 2014550024A JP 2015503554 A5 JP2015503554 A5 JP 2015503554A5

Authority

JP

Japan

Prior art keywords

glp

group

derivative

immunoglobulin

fragment

Prior art date

2012-12-28

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

• TWSALRJGPBVBQU-PKQQPRCHSA-N glucagon-like peptide 2 Chemical compound C([C@@H](C(=O)N[C@H](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]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O)[C@@H](C)CC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=CC=C1 TWSALRJGPBVBQU-PKQQPRCHSA-N 0.000 claims 43
• 101800000221 Glucagon-like peptide 2 Proteins 0.000 claims 39
• 102100040918 Pro-glucagon Human genes 0.000 claims 38
• 102000018071 Immunoglobulin Fc Fragments Human genes 0.000 claims 14
• 108010091135 Immunoglobulin Fc Fragments Proteins 0.000 claims 14
• 229920000642 polymer Polymers 0.000 claims 14
• 108090000765 processed proteins & peptides Proteins 0.000 claims 13
• 125000003277 amino group Chemical group 0.000 claims 9
• 125000003396 thiol group Chemical group [H]S* 0.000 claims 8
• 108060003951 Immunoglobulin Proteins 0.000 claims 3
• 102000018358 immunoglobulin Human genes 0.000 claims 3
• 238000000034 method Methods 0.000 claims 3
• KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical class O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims 3
• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
• 125000003172 aldehyde group Chemical group 0.000 claims 2
• 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims 2
• 239000011541 reaction mixture Substances 0.000 claims 2
• -1 succinimidyl carboxymethyl Chemical group 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
• AASBXERNXVFUEJ-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) propanoate Chemical compound CCC(=O)ON1C(=O)CCC1=O AASBXERNXVFUEJ-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
• 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
• 102000015626 Glucagon-Like Peptide-2 Receptor Human genes 0.000 claims 1
• 108010024044 Glucagon-Like Peptide-2 Receptor Proteins 0.000 claims 1
• PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
• 239000002202 Polyethylene glycol Substances 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
• 239000004480 active ingredient Substances 0.000 claims 1
• 150000001299 aldehydes Chemical class 0.000 claims 1
• 150000001412 amines Chemical class 0.000 claims 1
• 235000001014 amino acid Nutrition 0.000 claims 1
• 125000000539 amino acid group Chemical group 0.000 claims 1
• 150000001413 amino acids Chemical class 0.000 claims 1
• 229940053198 antiepileptics succinimide derivative Drugs 0.000 claims 1
• 229920002988 biodegradable polymer Polymers 0.000 claims 1
• 239000004621 biodegradable polymer Substances 0.000 claims 1
• 210000004899 c-terminal region Anatomy 0.000 claims 1
• 229910052799 carbon Inorganic materials 0.000 claims 1
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
• 229920001577 copolymer Polymers 0.000 claims 1
• 230000008878 coupling Effects 0.000 claims 1
• 238000010168 coupling process Methods 0.000 claims 1
• 238000005859 coupling reaction Methods 0.000 claims 1
• 235000018417 cysteine Nutrition 0.000 claims 1
• XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
• 239000000539 dimer Substances 0.000 claims 1
• 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 150000004676 glycans Chemical class 0.000 claims 1
• HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 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
• 229940072221 immunoglobulins Drugs 0.000 claims 1
• 208000028774 intestinal disease Diseases 0.000 claims 1
• 230000000968 intestinal effect Effects 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
• 238000004519 manufacturing process Methods 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 230000004048 modification Effects 0.000 claims 1
• 238000012986 modification Methods 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 229920001583 poly(oxyethylated polyols) Polymers 0.000 claims 1
• 229920001223 polyethylene glycol 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
• 238000006467 substitution reaction Methods 0.000 claims 1
• 229920002554 vinyl polymer Polymers 0.000 claims 1