HRP20201732T1 - A22k, desb27, b29r, dez b30, na položaju epsilon u lizinu 22 aciliranog analoga ljudskog inzulina - Google Patents
A22k, desb27, b29r, dez b30, na položaju epsilon u lizinu 22 aciliranog analoga ljudskog inzulina Download PDFInfo
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- HRP20201732T1 HRP20201732T1 HRP20201732TT HRP20201732T HRP20201732T1 HR P20201732 T1 HRP20201732 T1 HR P20201732T1 HR P20201732T T HRP20201732T T HR P20201732TT HR P20201732 T HRP20201732 T HR P20201732T HR P20201732 T1 HRP20201732 T1 HR P20201732T1
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- Croatia
- Prior art keywords
- dezb30
- dezb27
- eps
- human insulin
- gglu
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- PBGKTOXHQIOBKM-FHFVDXKLSA-N insulin (human) Chemical class 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 title claims 52
- 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 title claims 5
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 title 1
- 239000004472 Lysine Substances 0.000 title 1
- 101150019032 B29R gene Proteins 0.000 claims 56
- 101000976075 Homo sapiens Insulin Proteins 0.000 claims 50
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical class 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 28
- 239000004026 insulin derivative Substances 0.000 claims 26
- 125000002252 acyl group Chemical group 0.000 claims 6
- 238000006467 substitution reaction Methods 0.000 claims 6
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 239000011701 zinc Substances 0.000 claims 5
- 229910052725 zinc Inorganic materials 0.000 claims 5
- 239000002253 acid Substances 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 4
- HQHCYKULIHKCEB-UHFFFAOYSA-N tetradecanedioic acid Chemical compound OC(=O)CCCCCCCCCCCCC(O)=O HQHCYKULIHKCEB-UHFFFAOYSA-N 0.000 claims 4
- 150000007513 acids Chemical class 0.000 claims 3
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims 2
- BTZVDPWKGXMQFW-UHFFFAOYSA-N Pentadecanedioic acid Chemical compound OC(=O)CCCCCCCCCCCCCC(O)=O BTZVDPWKGXMQFW-UHFFFAOYSA-N 0.000 claims 2
- PTFCDOFLOPIGGS-UHFFFAOYSA-N Zinc dication Chemical compound [Zn+2] PTFCDOFLOPIGGS-UHFFFAOYSA-N 0.000 claims 2
- -1 Zn2+ ions Chemical class 0.000 claims 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- QQHJDPROMQRDLA-UHFFFAOYSA-N hexadecanedioic acid Chemical compound OC(=O)CCCCCCCCCCCCCCC(O)=O QQHJDPROMQRDLA-UHFFFAOYSA-N 0.000 claims 2
- RUVRGYVESPRHSZ-UHFFFAOYSA-N 2-[2-(2-azaniumylethoxy)ethoxy]acetate Chemical compound NCCOCCOCC(O)=O RUVRGYVESPRHSZ-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 208000031773 Insulin resistance syndrome Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical group OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000008469 Peptic Ulcer Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 201000010390 abdominal obesity-metabolic syndrome 1 Diseases 0.000 claims 1
- 230000010933 acylation Effects 0.000 claims 1
- 238000005917 acylation reaction Methods 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 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
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 208000011661 metabolic syndrome X Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 229960003966 nicotinamide Drugs 0.000 claims 1
- 235000005152 nicotinamide Nutrition 0.000 claims 1
- 239000011570 nicotinamide Substances 0.000 claims 1
- 229960002715 nicotine Drugs 0.000 claims 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- BNJOQKFENDDGSC-UHFFFAOYSA-N octadecanedioic acid Natural products OC(=O)CCCCCCCCCCCCCCCCC(O)=O BNJOQKFENDDGSC-UHFFFAOYSA-N 0.000 claims 1
- 208000011906 peptic ulcer disease Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/62—Insulins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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Claims (26)
1. Derivat inzulina, naznačen time što je derivat inzulina acilirani analog ljudskog inzulina, gdje je navedeni analog
[A22K, dezB27, B29R, dezB30] u odnosu na ljudski inzulin;
te što navedeni je analog inzulina je deriviran aciliranjem epsilon amino skupineu lizinskom ostatku na položaju A22 skupinom Formule II
[acil]-[spojnica]-
gdje je spojna skupina aminokiselinski lanac koji se sastoji od 1 do 10 aminokiselinskih ostataka koje se bira između -gGlu- i -OEG-; gdje
gGlu predstavlja ostatak gama-glutaminske kiseline;
OEG predstavlja ostatak 8-amino-3,6-dioksaoktanske kiseline (tj. skupina formule -NH-(CH2)2-O-(CH2)2-O-CH2-CO-);
gdje navedeni aminokiselinski ostaci mogu biti prisutni u bilo kojem redoslijedu; i
gdje navedeni aminokiselinski lanac sadrži najmanje jedan gGlu ostatak; i
gdje je acilna skupina ostatak α,ω-dikarboksilne kiseline kojeg se bira između
1,14-tetradekanske dikiseline;
1,15-pentadekanske dikiseline; i
1,16-heksadekanske dikiseline;
gdje acilirani analog može dodatno sadržavati zamjene A14E i/ili B3E, ili B3Q.
2. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što acilirani analog dodatno sadrži zamjenu B3E ili B3Q.
3. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što acilirani analog dodatno sadrži zamjenu A14E.
4. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što acilirani analog dodatno sadrži zamjene A14E i B3E.
5. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što acilirani analog dodatno sadrži B3E zamjena.
6. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što acilirani analog dodatno sadrži zamjenu B3Q.
7. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što je analog [A14E, A22K, B3E, dezB27, B29R, dezB30]; [A14E, A22K, dezB27, B29R, dezB30]; [A22K, B3E, dezB27, B29R, dezB30]; [A22K, B3Q, dezB27, B29R, dezB30]; ili [A22K, dezB27, B29R, dezB30]; u odnosu na ljudski inzulin; te što je analog inzulina aciliran na epsilon amino skupini u lizinskom ostatku na položaju A22.
8. Derivat inzulina u skladu s patentnim zahtjevom 7, naznačen time što je analog [A14E, A22K, dezB27, B29R, dezB30]; [A22K, B3E, dezB27, B29R, dezB30]; [A22K, B3Q, dezB27, B29R, dezB30]; ili [A22K, dezB27, B29R, dezB30]; u odnosu na ljudski inzulin; te što je analog inzulina aciliran na epsilon amino skupini u lizinskom ostatku na položaju A22.
9. Derivat inzulina u skladu s patentnim zahtjevom 7, naznačen time što je analog [A22K, B3E, dezB27, B29R, dezB30]; u odnosu na ljudski inzulin; te što je analog inzulina aciliran na epsilon amino skupini u lizinskom ostatku na položaju A22.
10. Derivat inzulina u skladu s bilo kojim od patentnih zahtjeva 1-9, naznačen time što se spojnu skupinu bira između -gGlu-; -2xgGlu-; -3xgGlu-; -4xgGlu-; -gGlu-2xOEG-; -gGlu-3x(OEG-gGlu)-; -4xgGlu-2xOEG-; -2xOEG-; i -2xOEG-gGlu-.
11. Derivat inzulina u skladu s patentnim zahtjevom 10, naznačen time što se spojnu skupinu bira između -gGlu-; -2xgGlu-; -4xgGlu-; -gGlu-2xOEG-; -gGlu-3x(OEG-gGlu)-; -2xOEG-; i -2xOEG-gGlu-.
12. Derivat inzulina u skladu s patentnim zahtjevom 10, naznačen time što je spojna skupina - 4xgGlu-.
13. Derivat inzulina u skladu s bilo kojim od patentnih zahtjeva 1-12, naznačen time što je acilna skupina di-kiselina skupina izvedena iz 1,14-tetradekandiojska kiseline; 1,15-pentadekandiojska kiselina; ili 1,16-heksadekandiojska kiselina.
14. Derivat inzulina u skladu s patentnim zahtjevom 13, naznačen time što je acilna skupina 1,14-tetradekandiojska kiselina.
15. Derivat inzulina u skladu s bilo kojim od patentnih zahtjeva 1-14, naznačen time što je skupina u Formuli II (tj. [acil]-[spojnica]-) tetradekandioil-gGlu-; tetradekandioil-2xgGlu-; tetradekandioil-3xgGlu-; tetradekandioil-4xgGlu-; tetradekandioil-gGlu-2xOEG-; tetradekandioil-4xgGlu-2xOEG-; tetradekandioil-2xOEG-; pentadekandioil-4xgGlu-; heksadekandioil-4xgGlu-; heksadekandioil-gGlu-2xOEG-; ili heksadekandioil-3x(gGlu-OEG)-gGlu-.
16. Derivat inzulina u skladu s patentnim zahtjevom 15, naznačen time što je skupina u Formuli II (tj. [acil]-[spojnica]-) tetradekandioil-4xgGlu-.
17. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što je
A22K(N(eps)-tetradekandioil-4xgGlu), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A14E, A22K(N(eps)-tetradekandioil-4xgGlu), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-gGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-3x(gGlu-OEG)-gGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-4xgGlu), B3Q, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-gGlu-2xOEG), B3Q, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-3x(gGlu-OEG)-gGlu), B3Q, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-2xgGlu), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-4xgGlu), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-gGlu-2xOEG), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-3x(gGlu-OEG)-gGlu), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-gGlu), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-gGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-gGlu-2xOEG), B3Q, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-2xOEG), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-heksadekandioil-4xgGlu), B3Q, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-pentadekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-4xgGlu-2xOEG), dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-4xgGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A14E, A22K(N(eps)-tetradekandioil-gGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A14E, A22K(N(eps)-tetradekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-2xgGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin;
A22K(N(eps)-tetradekandioil-gGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin; ili
A22K(N(eps)-tetradekandioil-3xgGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin.
18. Derivat inzulina u skladu s patentnim zahtjevom 1, naznačen time što je
A22K(N(eps)-tetradekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudski inzulin.
19. Farmaceutski pripravak, naznačen time što sadrži derivat inzulina u skladu s bilo kojim od patentnih zahtjeva 1-18, kao i jedan ili više farmaceutski prihvatljivih nosača ili razrjeđivača.
20. Farmaceutski pripravak u skladu s patentnim zahtjevom 19, naznačen time što je formuliran kao pripravak s niskim sadržajem cinka, bez dodanih cinkovih iona.
21. Farmaceutski pripravak u skladu s patentnim zahtjevom 19, naznačen time što je formuliran kao pripravak s niskim sadržajem cinka, bez dodanih cinkovih iona, te što sadrži acilirani analog ljudskog inzulina kojeg se bira između:
A22K(N(eps)-tetradekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-heksadekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-heksadekandioil-gGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-heksadekandioil-3x(gGlu-OEG)-gGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-tetradekandioil-gGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-pentadekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-tetradekandioil-4xgGlu), B3Q, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-heksadekandioil-gGlu-2xOEG), B3Q, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-heksadekandioil-3x(gGlu-OEG)-gGlu), B3Q, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-tetradekandioil-gGlu-2xOEG), B3Q, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-heksadekandioil-4xgGlu), B3Q, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-tetradekandioil-4xgGlu-2xOEG), dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-tetradekandioil-4xgGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A14E, A22K(N(eps)-tetradekandioil-gGlu-2xOEG), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A14E, A22K(N(eps)-tetradekandioil-4xgGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-tetradekandioil-2xgGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina;
A22K(N(eps)-tetradekandioil-gGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina; i
A22K(N(eps)-tetradekandioil-3xgGlu), B3E, dezB27, B29R, dezB30 ljudskog inzulina.
22. Farmaceutski pripravak u skladu s nilo kojim od patentnih zahtjeva 20-21, naznačen time što je formuliran kao pripravak s niskim sadržajem cinka, koji sadrži manje od 0,2 iona Zn2+ na 6 molekula inzulina.
23. Farmaceutski pripravak s niskim sadržajem cinka u skladu s bilo kojim od patentnih zahtjeva 20-21, naznačen time što nije dodan tenzid.
24. Farmaceutski pripravak s niskim sadržajem cinka u skladu s bilo kojim od patentnih zahtjeva 20-21, naznačen time što sadrži nikotinski spoj, a osobito nikotinamid.
25. Derivat inzulina u skladu s bilo kojim od patentnih zahtjeva 1-18, naznačen time što je namijenjen upotrebi kao medikament.
26. Derivat inzulina u skladu s bilo kojim od patentnih zahtjeva 1-18, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju dijabetesa, dijabetesa tip 1, dijabetesa tip 2, smanjene tolerancije glukoze, hiperglikemije, dislipidemije, pretilosti, metaboličkog sindroma (metaboličkog sindroma X, sindroma otpornosti na inzulin), hipertenzije, poremećaja kognitivnih funkcija, ateroskleroze, infarkta miokarda, inzulta, kardiovaskularnih poremećaja, koronarne bolesti srca, sindroma crijevne upale, dispepsije ili želučanog vrijeda.
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EP15707102.8A EP3110840B1 (en) | 2014-02-28 | 2015-02-26 | An a22k, desb27, b29r, des b30, at epsilon position of lysine 22 acylated human insulin analogue |
PCT/EP2015/053989 WO2015128403A2 (en) | 2014-02-28 | 2015-02-26 | Novel insulin derivatives and the medical uses hereof |
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2015
- 2015-02-25 AR ARP150100559A patent/AR099569A1/es unknown
- 2015-02-26 TW TW104106145A patent/TWI686403B/zh not_active IP Right Cessation
- 2015-02-26 RU RU2016135543A patent/RU2684456C2/ru active
- 2015-02-26 PT PT157071028T patent/PT3110840T/pt unknown
- 2015-02-26 MX MX2016010899A patent/MX368387B/es active IP Right Grant
- 2015-02-26 HU HUE15707102A patent/HUE051355T2/hu unknown
- 2015-02-26 AU AU2015222135A patent/AU2015222135B2/en not_active Ceased
- 2015-02-26 CA CA2941103A patent/CA2941103A1/en not_active Withdrawn
- 2015-02-26 CN CN201580010746.3A patent/CN106459171B/zh active Active
- 2015-02-26 ES ES15707102T patent/ES2831848T3/es active Active
- 2015-02-26 KR KR1020167024826A patent/KR20160125988A/ko not_active Application Discontinuation
- 2015-02-26 BR BR112016017193A patent/BR112016017193A2/pt not_active Application Discontinuation
- 2015-02-26 US US15/121,206 patent/US10040839B2/en active Active
- 2015-02-26 DK DK15707102.8T patent/DK3110840T3/da active
- 2015-02-26 SI SI201531416T patent/SI3110840T1/sl unknown
- 2015-02-26 EP EP15707102.8A patent/EP3110840B1/en active Active
- 2015-02-26 JP JP2016554498A patent/JP6580583B2/ja active Active
- 2015-02-26 WO PCT/EP2015/053989 patent/WO2015128403A2/en active Application Filing
- 2015-02-26 RS RS20201399A patent/RS61137B1/sr unknown
- 2015-02-26 PL PL15707102T patent/PL3110840T3/pl unknown
-
2016
- 2016-07-13 IL IL246757A patent/IL246757B/en active IP Right Grant
- 2016-08-21 SA SA516371705A patent/SA516371705B1/ar unknown
-
2020
- 2020-10-27 HR HRP20201732TT patent/HRP20201732T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
CN106459171A (zh) | 2017-02-22 |
TW201620930A (zh) | 2016-06-16 |
EP3110840B1 (en) | 2020-10-21 |
US10040839B2 (en) | 2018-08-07 |
KR20160125988A (ko) | 2016-11-01 |
CN106459171B (zh) | 2020-12-15 |
AR099569A1 (es) | 2016-08-03 |
US20170008945A1 (en) | 2017-01-12 |
RU2016135543A3 (hr) | 2018-08-30 |
RU2016135543A (ru) | 2018-03-30 |
WO2015128403A2 (en) | 2015-09-03 |
BR112016017193A2 (pt) | 2017-10-03 |
MX368387B (es) | 2019-10-01 |
SA516371705B1 (ar) | 2019-10-08 |
TWI686403B (zh) | 2020-03-01 |
MX2016010899A (es) | 2016-11-18 |
RS61137B1 (sr) | 2020-12-31 |
IL246757B (en) | 2020-04-30 |
DK3110840T3 (da) | 2020-11-02 |
AU2015222135A1 (en) | 2016-07-28 |
ES2831848T3 (es) | 2021-06-09 |
CA2941103A1 (en) | 2015-09-03 |
RU2684456C2 (ru) | 2019-04-09 |
PL3110840T3 (pl) | 2021-04-06 |
HUE051355T2 (hu) | 2021-03-01 |
PT3110840T (pt) | 2020-11-26 |
WO2015128403A3 (en) | 2015-12-10 |
IL246757A0 (en) | 2016-08-31 |
AU2015222135B2 (en) | 2018-12-20 |
JP2017508741A (ja) | 2017-03-30 |
EP3110840A2 (en) | 2017-01-04 |
JP6580583B2 (ja) | 2019-09-25 |
SI3110840T1 (sl) | 2020-12-31 |
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