JPWO2020039051A5 - - Google Patents

Info

Publication number

JPWO2020039051A5

JPWO2020039051A5 JP2021509906A JP2021509906A JPWO2020039051A5 JP WO2020039051 A5 JPWO2020039051 A5 JP WO2020039051A5 JP 2021509906 A JP2021509906 A JP 2021509906A JP 2021509906 A JP2021509906 A JP 2021509906A JP WO2020039051 A5 JPWO2020039051 A5 JP WO2020039051A5

Authority

JP

Japan

Prior art keywords

calcitonin mimetic

amino acid

linking group

calcitonin

accsnlstcmlgk

Prior art date

2024-03-13

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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• 102000055006 Calcitonin Human genes 0.000 claims 59
• 108060001064 Calcitonin Proteins 0.000 claims 59
• BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims 59
• 229960004015 calcitonin Drugs 0.000 claims 59
• 235000014113 dietary fatty acids Nutrition 0.000 claims 34
• 229930195729 fatty acid Natural products 0.000 claims 34
• 239000000194 fatty acid Substances 0.000 claims 34
• 150000004665 fatty acids Chemical class 0.000 claims 34
• FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 32
• 125000000539 amino acid group Chemical group 0.000 claims 22
• 125000005647 linker group Chemical group 0.000 claims 20
• KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 10
• 235000001014 amino acid Nutrition 0.000 claims 10
• 229910052757 nitrogen Inorganic materials 0.000 claims 10
• 108090000765 processed proteins & peptides Proteins 0.000 claims 10
• 125000002252 acyl group Chemical group 0.000 claims 8
• 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 7
• KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 6
• 230000008482 dysregulation Effects 0.000 claims 6
• 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 6
• 230000002378 acidificating effect Effects 0.000 claims 5
• 150000001413 amino acids Chemical class 0.000 claims 5
• 206010033307 Overweight Diseases 0.000 claims 4
• 239000003814 drug Substances 0.000 claims 4
• 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 claims 4
• 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 4
• 229940079593 drug Drugs 0.000 claims 3
• LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
• WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 2
• 206010020710 Hyperphagia Diseases 0.000 claims 2
• 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
• 208000001132 Osteoporosis Diseases 0.000 claims 2
• 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
• 208000026594 alcoholic fatty liver disease Diseases 0.000 claims 2
• 239000008280 blood Substances 0.000 claims 2
• 210000004369 blood Anatomy 0.000 claims 2
• 206010012601 diabetes mellitus Diseases 0.000 claims 2
• 230000037406 food intake Effects 0.000 claims 2
• 235000012631 food intake Nutrition 0.000 claims 2
• 238000007446 glucose tolerance test Methods 0.000 claims 2
• 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 2
• 201000008482 osteoarthritis Diseases 0.000 claims 2
• 239000002245 particle Substances 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 229910052698 phosphorus Inorganic materials 0.000 claims 2
• 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
• 238000006467 substitution reaction Methods 0.000 claims 2
• 230000004580 weight loss Effects 0.000 claims 2
• XRTHAPZDZPADIL-UHFFFAOYSA-N 8-[(5-chloro-2-hydroxybenzoyl)amino]octanoic acid Chemical compound OC(=O)CCCCCCCNC(=O)C1=CC(Cl)=CC=C1O XRTHAPZDZPADIL-UHFFFAOYSA-N 0.000 claims 1
• 102000004877 Insulin Human genes 0.000 claims 1
• 108090001061 Insulin Proteins 0.000 claims 1
• 229940122355 Insulin sensitizer Drugs 0.000 claims 1
• 208000008589 Obesity Diseases 0.000 claims 1
• 210000004899 c-terminal region Anatomy 0.000 claims 1
• 229940000425 combination drug Drugs 0.000 claims 1
• WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 1
• 238000002347 injection Methods 0.000 claims 1
• 239000007924 injection Substances 0.000 claims 1
• 229940125396 insulin Drugs 0.000 claims 1
• XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 1
• 229960003105 metformin Drugs 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 230000003278 mimic effect Effects 0.000 claims 1
• 235000020824 obesity Nutrition 0.000 claims 1
• 238000007911 parenteral administration Methods 0.000 claims 1
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
• 230000001235 sensitizing effect Effects 0.000 claims 1
• XUHVCHNJCBBXMP-UHFFFAOYSA-M sodium;10-[(2-hydroxybenzoyl)amino]decanoate Chemical compound [Na+].OC1=CC=CC=C1C(=O)NCCCCCCCCCC([O-])=O XUHVCHNJCBBXMP-UHFFFAOYSA-M 0.000 claims 1
• UOENJXXSKABLJL-UHFFFAOYSA-M sodium;8-[(2-hydroxybenzoyl)amino]octanoate Chemical compound [Na+].OC1=CC=CC=C1C(=O)NCCCCCCCC([O-])=O UOENJXXSKABLJL-UHFFFAOYSA-M 0.000 claims 1