JP2014500244A5 - - Google Patents

Info

Publication number

JP2014500244A5

JP2014500244A5 JP2013535439A JP2013535439A JP2014500244A5 JP 2014500244 A5 JP2014500244 A5 JP 2014500244A5 JP 2013535439 A JP2013535439 A JP 2013535439A JP 2013535439 A JP2013535439 A JP 2013535439A JP 2014500244 A5 JP2014500244 A5 JP 2014500244A5

Authority

JP

Japan

Prior art keywords

insulin

chain

cooh

des

amino acid

Prior art date

2011-10-27

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

• 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 66
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 28
• 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 25
• 239000004026 insulin derivative Substances 0.000 claims 24
• VEVRNHHLCPGNDU-MUGJNUQGSA-O desmosine Chemical compound OC(=O)[C@@H](N)CCCC[N+]1=CC(CC[C@H](N)C(O)=O)=C(CCC[C@H](N)C(O)=O)C(CC[C@H](N)C(O)=O)=C1 VEVRNHHLCPGNDU-MUGJNUQGSA-O 0.000 claims 21
• 102000004877 Insulin Human genes 0.000 claims 20
• 108090001061 Insulin Proteins 0.000 claims 20
• 229940125396 insulin Drugs 0.000 claims 20
• 125000000539 amino acid group Chemical group 0.000 claims 18
• 125000002843 carboxylic acid group Chemical group 0.000 claims 8
• 125000003275 alpha amino acid group Chemical group 0.000 claims 6
• 125000001183 hydrocarbyl group Chemical group 0.000 claims 6
• 101000976075 Homo sapiens Insulin Proteins 0.000 claims 5
• VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical compound [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims 4
• 230000007774 longterm Effects 0.000 claims 4
• 201000010099 disease Diseases 0.000 claims 3
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
• 125000000729 N-terminal amino-acid group Chemical group 0.000 claims 2
• 125000003368 amide group Chemical group 0.000 claims 2
• 125000003277 amino group Chemical group 0.000 claims 2
• 230000009286 beneficial effect Effects 0.000 claims 2
• 125000004432 carbon atom Chemical group C* 0.000 claims 2
• -1 carboxyethyl Chemical group 0.000 claims 2
• 230000007935 neutral effect Effects 0.000 claims 2
• 201000009104 prediabetes syndrome Diseases 0.000 claims 2
• 206010006895 Cachexia Diseases 0.000 claims 1
• 208000002705 Glucose Intolerance Diseases 0.000 claims 1
• 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
• 206010061218 Inflammation Diseases 0.000 claims 1
• 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
• 208000008589 Obesity Diseases 0.000 claims 1
• 208000001280 Prediabetic State Diseases 0.000 claims 1
• 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
• 208000022531 anorexia Diseases 0.000 claims 1
• 229940127003 anti-diabetic drug Drugs 0.000 claims 1
• 239000003472 antidiabetic agent Substances 0.000 claims 1
• 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims 1
• 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
• 230000030833 cell death Effects 0.000 claims 1
• 230000006727 cell loss Effects 0.000 claims 1
• 206010061428 decreased appetite Diseases 0.000 claims 1
• 206010012601 diabetes mellitus Diseases 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 230000001747 exhibiting effect Effects 0.000 claims 1
• 201000001421 hyperglycemia Diseases 0.000 claims 1
• 238000001727 in vivo Methods 0.000 claims 1
• 230000004054 inflammatory process Effects 0.000 claims 1
• 235000020824 obesity Nutrition 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 239000003981 vehicle Substances 0.000 claims 1