JP2015524419A5 - - Google Patents

Info

Publication number

JP2015524419A5

JP2015524419A5 JP2015523532A JP2015523532A JP2015524419A5 JP 2015524419 A5 JP2015524419 A5 JP 2015524419A5 JP 2015523532 A JP2015523532 A JP 2015523532A JP 2015523532 A JP2015523532 A JP 2015523532A JP 2015524419 A5 JP2015524419 A5 JP 2015524419A5

Authority

JP

Japan

Prior art keywords

aib

seq

hypoglycemia

glu

ser

Prior art date

2013-07-23

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

• 208000013016 Hypoglycemia Diseases 0.000 claims 40
• 230000002218 hypoglycaemic effect Effects 0.000 claims 34
• 150000001875 compounds Chemical class 0.000 claims 17
• 150000003839 salts Chemical class 0.000 claims 15
• 239000012453 solvate Substances 0.000 claims 15
• 125000003295 alanine group Chemical group N[C@@H](C)C(=O)* 0.000 claims 10
• 241000024188 Andala Species 0.000 claims 9
• 125000003275 alpha amino acid group Chemical group 0.000 claims 9
• 230000001154 acute effect Effects 0.000 claims 6
• 206010012601 diabetes mellitus Diseases 0.000 claims 6
• 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 6
• 239000008194 pharmaceutical composition Substances 0.000 claims 6
• 125000000174 L-prolyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(*)=O 0.000 claims 5
• 238000012217 deletion Methods 0.000 claims 5
• 230000037430 deletion Effects 0.000 claims 5
• 238000006467 substitution reaction Methods 0.000 claims 5
• 125000000030 D-alanine group Chemical group [H]N([H])[C@](C([H])([H])[H])(C(=O)[*])[H] 0.000 claims 4
• 239000003814 drug Substances 0.000 claims 4
• AXDLCFOOGCNDST-VIFPVBQESA-N (2s)-3-(4-hydroxyphenyl)-2-(methylamino)propanoic acid Chemical compound CN[C@H](C(O)=O)CC1=CC=C(O)C=C1 AXDLCFOOGCNDST-VIFPVBQESA-N 0.000 claims 3
• 201000001320 Atherosclerosis Diseases 0.000 claims 3
• 208000032928 Dyslipidaemia Diseases 0.000 claims 3
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
• 208000002705 Glucose Intolerance Diseases 0.000 claims 3
• 206010018464 Glycogen storage disease type I Diseases 0.000 claims 3
• 206010020772 Hypertension Diseases 0.000 claims 3
• 102000004877 Insulin Human genes 0.000 claims 3
• 108090001061 Insulin Proteins 0.000 claims 3
• 208000017170 Lipid metabolism disease Diseases 0.000 claims 3
• 208000008589 Obesity Diseases 0.000 claims 3
• 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 3
• 239000002876 beta blocker Substances 0.000 claims 3
• 229940097320 beta blocking agent Drugs 0.000 claims 3
• 230000001684 chronic effect Effects 0.000 claims 3
• 208000029078 coronary artery disease Diseases 0.000 claims 3
• 201000010099 disease Diseases 0.000 claims 3
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
• 229940079593 drug Drugs 0.000 claims 3
• 230000002496 gastric effect Effects 0.000 claims 3
• 201000004541 glycogen storage disease I Diseases 0.000 claims 3
• 229940125396 insulin Drugs 0.000 claims 3
• 206010022498 insulinoma Diseases 0.000 claims 3
• 108020004707 nucleic acids Proteins 0.000 claims 3
• 150000007523 nucleic acids Chemical class 0.000 claims 3
• 102000039446 nucleic acids Human genes 0.000 claims 3
• 235000020824 obesity Nutrition 0.000 claims 3
• 208000021255 pancreatic insulinoma Diseases 0.000 claims 3
• 201000009104 prediabetes syndrome Diseases 0.000 claims 3
• 230000035935 pregnancy Effects 0.000 claims 3
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
• 125000000180 D-prolyl group Chemical group N1[C@@H](C(=O)*)CCC1 0.000 claims 2
• 125000003625 D-valyl group Chemical group N[C@@H](C(=O)*)C(C)C 0.000 claims 2
• 208000004930 Fatty Liver Diseases 0.000 claims 2
• 102000051325 Glucagon Human genes 0.000 claims 2
• 108060003199 Glucagon Proteins 0.000 claims 2
• 206010019708 Hepatic steatosis Diseases 0.000 claims 2
• 101500028775 Homo sapiens Glucagon Proteins 0.000 claims 2
• ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims 2
• 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
• 239000000556 agonist Substances 0.000 claims 2
• 125000000217 alkyl group Chemical group 0.000 claims 2
• 150000001413 amino acids Chemical class 0.000 claims 2
• 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 2
• 230000000694 effects Effects 0.000 claims 2
• 239000013604 expression vector Substances 0.000 claims 2
• 208000010706 fatty liver disease Diseases 0.000 claims 2
• 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 2
• 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 2
• 229960004666 glucagon Drugs 0.000 claims 2
• 229910052739 hydrogen Inorganic materials 0.000 claims 2
• 239000001257 hydrogen Substances 0.000 claims 2
• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
• 231100000572 poisoning Toxicity 0.000 claims 2
• 230000000607 poisoning effect Effects 0.000 claims 2
• 108090000765 processed proteins & peptides Proteins 0.000 claims 2
• 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
• 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 2
• 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 1
• 206010012335 Dependence Diseases 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 210000004185 liver Anatomy 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1