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 PDF

Info

Publication number
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
Authority
HR
Croatia
Prior art keywords
dezb30
dezb27
eps
human insulin
gglu
Prior art date
Application number
HRP20201732TT
Other languages
English (en)
Inventor
Peter Madsen
Susanne HOSTRUP
Martin Münzel
Thomas Børglum KJELDSEN
Claudia Ulrich HJØRRINGGAARD
Christian Fledelius
Original Assignee
Novo Nordisk A/S
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novo Nordisk A/S filed Critical Novo Nordisk A/S
Publication of HRP20201732T1 publication Critical patent/HRP20201732T1/hr

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)

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.
HRP20201732TT 2014-02-28 2015-02-26 A22k, desb27, b29r, dez b30, na položaju epsilon u lizinu 22 aciliranog analoga ljudskog inzulina HRP20201732T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14157215 2014-02-28
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

Publications (1)

Publication Number Publication Date
HRP20201732T1 true HRP20201732T1 (hr) 2020-12-25

Family

ID=50184804

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20201732TT HRP20201732T1 (hr) 2014-02-28 2015-02-26 A22k, desb27, b29r, dez b30, na položaju epsilon u lizinu 22 aciliranog analoga ljudskog inzulina

Country Status (23)

Country Link
US (1) US10040839B2 (hr)
EP (1) EP3110840B1 (hr)
JP (1) JP6580583B2 (hr)
KR (1) KR20160125988A (hr)
CN (1) CN106459171B (hr)
AR (1) AR099569A1 (hr)
AU (1) AU2015222135B2 (hr)
BR (1) BR112016017193A2 (hr)
CA (1) CA2941103A1 (hr)
DK (1) DK3110840T3 (hr)
ES (1) ES2831848T3 (hr)
HR (1) HRP20201732T1 (hr)
HU (1) HUE051355T2 (hr)
IL (1) IL246757B (hr)
MX (1) MX368387B (hr)
PL (1) PL3110840T3 (hr)
PT (1) PT3110840T (hr)
RS (1) RS61137B1 (hr)
RU (1) RU2684456C2 (hr)
SA (1) SA516371705B1 (hr)
SI (1) SI3110840T1 (hr)
TW (1) TWI686403B (hr)
WO (1) WO2015128403A2 (hr)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170028031A1 (en) * 2014-03-07 2017-02-02 Klavs Holger Jørgensen Novel fast acting insulin preparations
ES2908373T3 (es) 2015-08-25 2022-04-28 Novo Nordisk As Nuevos derivados de insulina y los usos médicos de los mismos
CA3294636A1 (en) * 2016-11-21 2026-02-10 Case Western Reserve University Rapid-acting insulin analogues of enhanced stability
KR101909052B1 (ko) * 2017-02-09 2018-10-17 강원대학교산학협력단 인슐린의 a 사슬로부터 유래된 펩타이드 단편 및 이를 포함하는 당뇨병 또는 당뇨병성 창상의 예방 또는 치료용 약학 조성물
JP2020513019A (ja) * 2017-04-05 2020-04-30 ノヴォ ノルディスク アー／エス オリゴマー伸長インスリン−Ｆｃコンジュゲート
JOP20190273A1 (ar) * 2017-05-26 2019-11-24 Lilly Co Eli مركب إنسولين معالج بأسيل
US10919949B2 (en) * 2017-08-17 2021-02-16 Novo Nordisk A/S Acylated insulin analogues and uses thereof
WO2019079710A1 (en) 2017-10-19 2019-04-25 Buice Mona E TOPIC COMPOSITION FOR ENHANCED WOUND WOUND HEALING
RU2020128624A (ru) 2018-02-27 2022-03-28 Зп Спв 3 К/С Аналоги компстатина и их медицинское применение
TWI829687B (zh) * 2018-05-07 2024-01-21 丹麥商諾佛 儂迪克股份有限公司 包含glp-1促效劑與n-(8-(2-羥基苯甲醯基)胺基)辛酸之鹽的固體組成物
KR20210102347A (ko) 2018-12-11 2021-08-19 사노피 인슐린 수용체 결합 친화성이 감소된 인슐린 유사체
JP7432531B2 (ja) 2019-02-13 2024-02-16 住友ファーマ株式会社 システイン残基を有するヘミアスタリン誘導体
WO2020166592A1 (ja) * 2019-02-13 2020-08-20 大日本住友製薬株式会社 ヘミアスタリン誘導体とその抗体薬物複合体
BR112022003760A2 (pt) * 2019-08-27 2022-05-31 Zp Spv 3 K/S Análogos de compstatina e seus usos médicos
DK4073097T3 (da) 2019-12-11 2024-08-19 Novo Nordisk As Nye insulinanaloger og anvendelser heraf
CN118754967A (zh) * 2019-12-30 2024-10-11 甘李药业股份有限公司 胰岛素衍生物
CN115385843A (zh) * 2021-05-24 2022-11-25 广东东阳光药业有限公司 一种新型的酰化胰岛素类似物

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3528960A (en) 1968-10-07 1970-09-15 Lilly Co Eli N-carboxyaroyl insulins
US3869437A (en) 1970-05-08 1975-03-04 Nat Res Dev Mono-, di, and N{HD A1{B , N{HU B1{B , N{HU B29{B -tri-acylated insulin
GB1381274A (en) 1971-01-28 1975-01-22 Nat Res Dev Insulin derivatives
US3864325A (en) 1971-11-18 1975-02-04 Nat Res Dev (N{HU Al{b , N{HU Bl{b , N{HU B29{B , carbamoyl)-(O{HU A14{B , O{HU B16{B , O{HU B26{B aryl) insulin derivatives
JPH01254699A (ja) 1988-04-05 1989-10-11 Kodama Kk インスリン誘導体及びその用途
HUT56857A (en) * 1988-12-23 1991-10-28 Novo Nordisk As Human insulin analogues
JP3122128B2 (ja) * 1989-12-21 2001-01-09 ノボ ノルディスク アクティーゼルスカブ ペプチド製剤
US6011007A (en) 1993-09-17 2000-01-04 Novo Nordisk A/S Acylated insulin
US6869930B1 (en) 1993-09-17 2005-03-22 Novo Nordisk A/S Acylated insulin
EP1132404A3 (en) 1993-09-17 2002-03-27 Novo Nordisk A/S Acylated insulin
US6703017B1 (en) * 1994-04-28 2004-03-09 Ixion Biotechnology, Inc. Reversal of insulin-dependent diabetes by islet-producing stem cells, islet progenitor cells and islet-like structures
US5461031A (en) 1994-06-16 1995-10-24 Eli Lilly And Company Monomeric insulin analog formulations
US5646242A (en) 1994-11-17 1997-07-08 Eli Lilly And Company Selective acylation of epsilon-amino groups
US5693609A (en) 1994-11-17 1997-12-02 Eli Lilly And Company Acylated insulin analogs
US6251856B1 (en) 1995-03-17 2001-06-26 Novo Nordisk A/S Insulin derivatives
CZ289343B6 (cs) 1995-03-17 2002-01-16 Novo Nordisk A/S Inzulinový derivát a farmaceutický prostředek pro léčení diabetes
US6451970B1 (en) 1996-02-21 2002-09-17 Novo Nordisk A/S Peptide derivatives
US5905140A (en) 1996-07-11 1999-05-18 Novo Nordisk A/S, Novo Alle Selective acylation method
US5898067A (en) 1997-02-07 1999-04-27 Novo Nordisk A/S Crystallization of proteins
EP1005490B1 (en) 1997-03-20 2006-03-29 Novo Nordisk A/S Zinc free insulin crystals for use in pulmonary compositions
RU2218349C2 (ru) 1997-10-24 2003-12-10 Ново Нордиск А/С Агрегаты производных инсулина человека
US6444641B1 (en) 1997-10-24 2002-09-03 Eli Lilly Company Fatty acid-acylated insulin analogs
JP2001521006A (ja) 1997-10-24 2001-11-06 イーライ・リリー・アンド・カンパニー 不溶性インシュリン組成物
US6451762B1 (en) 1997-10-24 2002-09-17 Novo Nordisk A/S Aggregates of human insulin derivatives
ZA989744B (en) 1997-10-31 2000-04-26 Lilly Co Eli Method for administering acylated insulin.
US6531448B1 (en) 1997-12-23 2003-03-11 Eli Lilly And Company Insoluble compositions for controlling blood glucose
WO1999034821A1 (en) 1998-01-09 1999-07-15 Novo Nordisk A/S Stabilised insulin compositions
AU8029798A (en) 1998-06-12 2000-01-05 Deutsches Wollforschungsinstitut Insulin analogue
AU5454200A (en) 1999-06-29 2001-01-31 Eli Lilly And Company Protamine-free insoluble acylated insulin compositions
AU2001264789A1 (en) 2000-06-08 2001-12-17 Eli Lilly And Company Protein powder for pulmonary delivery
DE10114178A1 (de) 2001-03-23 2002-10-10 Aventis Pharma Gmbh Zinkfreie und zinkarme Insulinzubereitungen mit verbesserter Stabilität
EP1453860A2 (en) 2001-12-02 2004-09-08 Novo Nordisk A/S Novel glucose-dependant insulins
CZ2004710A3 (cs) 2001-12-20 2005-02-16 Eli Lilly And Company Inzulínová sloučenina s protrahovaným účinkem
AU2003208316A1 (en) 2002-03-13 2003-09-22 Novo Nordisk A/S Minimising body weight gain in insulin treatment
US20040138099A1 (en) 2002-11-29 2004-07-15 Draeger Eberhard Kurt Insulin administration regimens for the treatment of subjects with diabetes
EP1620465A2 (en) 2003-04-29 2006-02-01 Eli Lilly And Company Insulin analogs having protracted time action
US20060183667A1 (en) 2003-07-11 2006-08-17 Novo Nordisk A/S Stabilised insulin compositions
WO2005005477A2 (en) 2003-07-11 2005-01-20 Novo Nordisk A/S Stabilised insulin compositions
CA2531988C (en) 2003-08-05 2016-06-28 Novo Nordisk A/S Novel insulin derivatives
AU2004264958B2 (en) 2003-08-13 2010-04-15 Biocon, Ltd Micro-particle fatty acid salt solid dosage formulations for therapeutic agents
EP1687428A1 (en) 2003-11-14 2006-08-09 Novo Nordisk A/S Processes for making acylated insulin
EP1692168B1 (en) 2003-12-03 2011-07-20 Novo Nordisk A/S Single-chain insulin
WO2006008238A1 (en) 2004-07-16 2006-01-26 Novo Nordisk A/S Method for selective acylation
RU2527893C2 (ru) 2004-07-19 2014-09-10 Биокон Лимитед Инсулин-олигомерные конъюгаты, их препараты и применения
EP2256130B1 (en) 2005-02-02 2013-09-25 Novo Nordisk A/S Novel insulin derivatives
US20080171695A1 (en) 2005-02-02 2008-07-17 Novo Nordisk A/S Insulin Derivatives
JP2008533100A (ja) 2005-03-18 2008-08-21 ノボ ノルディスク アクティーゼルスカブ Ｐｅｇ化された単鎖インスリン
ES2371361T3 (es) 2005-12-28 2011-12-30 Novo Nordisk A/S Composiciones que comprenden una insulina acilada y zinc y método de producción de dichas composiciones.
DE602007009496D1 (de) 2006-02-27 2010-11-11 Novo Nordisk As Insulinderivate
WO2007128815A1 (en) 2006-05-09 2007-11-15 Novo Nordisk A/S Insulin derivative
EP2015770B1 (en) 2006-05-09 2012-09-26 Novo Nordisk A/S Insulin derivative
JP2009544716A (ja) 2006-07-27 2009-12-17 ノバルティス アクチエンゲゼルシャフト 肺送達のためのインスリン含有エアロゾル化可能製剤
CN101573133B (zh) 2006-07-31 2014-08-27 诺沃-诺迪斯克有限公司 Peg化延长的胰岛素
RU2524150C2 (ru) * 2006-09-22 2014-07-27 Ново Нордиск А/С Аналоги инсулина, устойчивые к протеазам
WO2008145721A2 (en) 2007-06-01 2008-12-04 Novo Nordisk A/S N-terminal modification of polypeptides for protection against degradation by aminopeptidases
JP5552046B2 (ja) 2007-06-13 2014-07-16 ノボ・ノルデイスク・エー／エス インスリン誘導体を含有する薬学的製剤
WO2009015456A1 (en) 2007-07-30 2009-02-05 Generex Pharmaceuticals Inc. Pharmaceutical formulation in mixed micellar form and dispenser for oral delivery of agents as a spray
US9150633B2 (en) 2007-08-15 2015-10-06 Novo Nordisk A/S Insulin analogues with an acyl and alkylene glycol moiety
EP2217621B1 (en) 2007-11-08 2015-04-22 Novo Nordisk A/S Insulin derivative
BRPI0820535B8 (pt) 2007-11-16 2021-05-25 Novo Nordisk As composições farmacêuticas contendo insulina e um peptídeo insulinotrópico
MX2010005317A (es) 2007-11-20 2010-06-02 Ambrx Inc Polipeptidos de insulina modificados y sus usos.
WO2009112583A2 (en) 2008-03-14 2009-09-17 Novo Nordisk A/S Protease-stabilized insulin analogues
HUE032284T2 (en) * 2008-03-18 2017-09-28 Novo Nordisk As Protease-stabilized, acylated insulin analogues
ES2561208T3 (es) 2008-09-12 2016-02-25 Novo Nordisk A/S Método de acilación de un péptido o una proteína
JP4959005B2 (ja) 2008-10-30 2012-06-20 ノボ・ノルデイスク・エー／エス 毎日の注射頻度より少ないインスリン注射での真性糖尿病の治療
AU2009335715B2 (en) 2008-12-19 2016-09-15 Indiana University Research And Technology Corporation Amide-based insulin prodrugs
EP2448962B1 (en) 2009-06-30 2016-10-19 Novo Nordisk A/S Insulin derivatives
NZ597964A (en) * 2009-07-31 2014-04-30 Sanofi Aventis Deutschland Long acting insulin composition
MX2012012943A (es) 2010-05-10 2012-11-29 Novo Nordisk As Proceso para preparacion de complejos de insulina-cinc.
JP5973427B2 (ja) 2010-06-23 2016-08-23 ノヴォ ノルディスク アー／エス 追加のジスルフィド結合を含有するインスリン類似体
KR20130036290A (ko) * 2010-06-23 2013-04-11 노보 노르디스크 에이/에스 추가 이황화 결합을 함유하는 인슐린 유도체
CN103415300B (zh) 2010-07-20 2018-02-23 诺沃—诺迪斯克有限公司 N‑末端修饰的fgf21化合物
CN103596584B (zh) * 2011-06-15 2016-12-14 诺沃—诺迪斯克有限公司 多取代的胰岛素
KR20150021011A (ko) 2011-10-27 2015-02-27 케이스 웨스턴 리저브 유니버시티 초고도 농축된, 속효성 인슐린 유사체 제형

Also Published As

Publication number Publication date
KR20160125988A (ko) 2016-11-01
PT3110840T (pt) 2020-11-26
JP2017508741A (ja) 2017-03-30
CN106459171B (zh) 2020-12-15
WO2015128403A3 (en) 2015-12-10
BR112016017193A2 (pt) 2017-10-03
TWI686403B (zh) 2020-03-01
US10040839B2 (en) 2018-08-07
RU2016135543A (ru) 2018-03-30
AU2015222135B2 (en) 2018-12-20
IL246757B (en) 2020-04-30
HUE051355T2 (hu) 2021-03-01
US20170008945A1 (en) 2017-01-12
EP3110840A2 (en) 2017-01-04
EP3110840B1 (en) 2020-10-21
RS61137B1 (sr) 2020-12-31
CA2941103A1 (en) 2015-09-03
IL246757A0 (en) 2016-08-31
PL3110840T3 (pl) 2021-04-06
DK3110840T3 (da) 2020-11-02
MX368387B (es) 2019-10-01
ES2831848T3 (es) 2021-06-09
AR099569A1 (es) 2016-08-03
MX2016010899A (es) 2016-11-18
CN106459171A (zh) 2017-02-22
TW201620930A (zh) 2016-06-16
SA516371705B1 (ar) 2019-10-08
SI3110840T1 (sl) 2020-12-31
AU2015222135A1 (en) 2016-07-28
RU2016135543A3 (hr) 2018-08-30
WO2015128403A2 (en) 2015-09-03
JP6580583B2 (ja) 2019-09-25
RU2684456C2 (ru) 2019-04-09

Similar Documents

Publication Publication Date Title
HRP20201732T1 (hr) A22k, desb27, b29r, dez b30, na položaju epsilon u lizinu 22 aciliranog analoga ljudskog inzulina
JP2017508741A5 (hr)
RU2018107727A (ru) Новые производные инсулина и их медицинские применения
JP2013533227A5 (hr)
UA114700C2 (uk) Тверда фармацевтична форма для перорального застосування та процес її виготовлення
RU2017121277A (ru) Фармацевтические композиции, содержащие epa и сердечно-сосудистое средство, и способы их применения
RU2013131913A (ru) Твердые композиции, содержащие агонист glp и соль n-(2-гидроксибензоил)амино)каприловой кислоты
CO6410287A2 (es) Composición farmacéutica, forma farmacéutica, procedimiento para su preparación, métodos de tratamiento y usos de la misma
JP2012506402A5 (hr)
ME02182B (me) TERAPEUTSKA KOMBINACIJA KOJA SADRŽI DOLUTEGRAVIR, ABAKAVIR l LAMIVUDIN
MY189770A (en) Biaryl derivative as gpr120 agonists
BRPI0416444B8 (pt) composto de ácido borônico heterocíclico, composição farmacêutica, e, combinação farmacêutica compreendendo o mesmo
BR112012012947B8 (pt) sal de hemitartarato e composição farmacêutica compreendendo o mesmo
ATE557030T1 (de) Kondensiertes heterocyclisches derivat, dieses enthaltende medizinische zusammensetzung und deren medizinische verwendung
MA32175B1 (fr) Oxadiazoanthracènes pour le traitement du diabète
JP2013530974A5 (hr)
HRP20240173T1 (hr) Fluorofenil beta-hidroksietilamini i njihova upotreba u liječenju hiperglikemije
MX2017004614A (es) Preparacion compuesta, que contiene derivado novedoso de acido 3-(4-(benciloxi)fenil)hex-4-inoico y otro ingrediente activo, para prevenir o tratar enfermedades metabolicas.
JP2015513544A5 (hr)
SI2945620T1 (en) Nitroxyl donors with improved therapeutic index
JP2014520163A5 (hr)
RU2019118696A (ru) Фармацевтические композиции, содержащие инсулин
NZ594244A (en) Thiadiazole and oxadiazole derivatives, preparation thereof, and therapeutic use thereof
RU2020108281A (ru) Новые ацилированные аналоги инсулина и варианты их применения
JP2007238598A5 (hr)