HRP20240135T1 - Fgf21 mutanti i njihove upotrebe - Google Patents

Fgf21 mutanti i njihove upotrebe Download PDF

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Publication number
HRP20240135T1
HRP20240135T1 HRP20240135TT HRP20240135T HRP20240135T1 HR P20240135 T1 HRP20240135 T1 HR P20240135T1 HR P20240135T T HRP20240135T T HR P20240135TT HR P20240135 T HRP20240135 T HR P20240135T HR P20240135 T1 HRP20240135 T1 HR P20240135T1
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Croatia
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polypeptide
seq
amino acid
substituted
residue
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HRP20240135TT
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English (en)
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Edward John Belouski
Murielle Marie Ellison
Agnes Eva Hamburger
Randy Ira Hecht
Yue-Sheng Li
Mark Leo Michaels
Jeonghoon Sun
Jing Xu
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Amgen Inc.
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Application filed by Amgen Inc. filed Critical Amgen Inc.
Publication of HRP20240135T1 publication Critical patent/HRP20240135T1/hr

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    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/475Growth factors; Growth regulators
    • C07K14/50Fibroblast growth factor [FGF]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
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    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
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    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2319/00Fusion polypeptide
    • C07K2319/30Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto

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Claims (15)

1. Polipeptid koji sadrži aminokiselinsku sekvencu SEQ ID NO: 4, gdje: (a) aminokiselinski ostatak na položaju 180 u SEQ ID NO:4 je supstituiran s aminokiselinom odabranom iz skupine koju čine glicin, prolin, serin i glutaminska kiselina; i (b) aminokiselinski ostatak na položaju 98 u SEQ ID NO: 4 je supstituiran s argininom ili je aminokiselinski ostatak na položaju 171 u SEQ ID NO: 4 glicin, i pri čemu je polipeptid sposoban sniziti razinu glukoze u krvi kod sisavaca.
2. Polipeptid sukladno patentnom zahtjevu 1, naznačen time, da nadalje sadrži slijed linkera koji sadrži SEQ ID NO:31
3. Polipeptid sukladno patentnom zahtjevu 1 ili patentnom zahtjevu 2, naznačen time, da nadalje sadrži Fc domenu koja sadrži SEQ ID NO:11.
4. Polipeptid sukladno bilo kojem od zahtjeva 1-3, naznačen time, da (i) polipeptid SEQ ID NO: 4 sadrži: (a) skraćivanje amino-kraja ne više od 8 aminokiselinskih ostataka, pri čemu je polipeptid sposoban za snižavanje glukoze u krvi kod sisavaca; (b) skraćivanje karboksi kraja ne više od 12 aminokiselinskih ostataka, pri čemu je polipeptid sposoban sniziti glukozu u krvi kod sisavaca; ili (c) skraćivanje amino-kraja od najviše 8 aminokiselinskih ostataka, i skraćivanje karboksi-terminusa od najviše 12 aminokiselinskih ostataka, pri čemu je polipeptid sposoban sniziti glukozu u krvi kod sisavaca, ili (ii) polipeptid je kovalentno vezan za jedan ili više polimera, po izboru polimer je PEG.
5. Farmaceutski pripravak koji sadrži polipeptid prema bilo kojem od zahtjeva 1-3, i farmaceutski prihvatljivo sredstvo za formuliranje.
6. Farmaceutski pripravak sukladno zahtjevu 5, naznačen time, da je farmaceutski prihvatljivo sredstvo za formuliranje hidrogel.
7. Farmaceutski pripravak sukladno patentnom zahtjevu 5 ili 6, za upotrebu u liječenju metaboličkog poremećaja.
8. Farmaceutski pripravak za upotrebu sukladno zahtjevu 7, naznačen time, da je metabolički poremećaj dijabetes tipa 2 ili pretilost.
9. Farmaceutski pripravak za upotrebu sukladno zahtjevu 7, naznačen time, da je metabolički poremećaj nealkoholni steatohepatitis (NASH).
10. Farmaceutski pripravak za upotrebu sukladno zahtjevu 9, naznačen time, da polipeptid sadrži aminokiselinsku sekvencu SEQ ID NO: 4 koja nadalje uključuje supstituciju argininskog ostatka s leucinskim ostatkom na položaju 98, glicinskog ostatka s prolinskim ostatkom na poziciji 171 i glutaminsku kiselinu s alaninom na poziciji 180.
11. Nukleinska kiselina koja kodira polipeptid sukladno bilo kojem od patentnih zahtjeva 1-3.
12. Vektor koji sadrži molekulu nukleinske kiseline sukladno zahtjevu 10.
13. Stanica domaćin koja sadrži molekulu nukleinske kiseline sukladno zahtjevu 10.
14. Multimer koji sadrži dva ili više od polipeptida sukladno patentnom zahtjevu 3.
15. Multimer sukladno patentnom zahtjevu 14, koji sadrži prvi i drugi lanac, pri čemu prvi lanac sadrži: (a.1) polipeptid SEQ ID NO: 4, gdje je (i) leucin na položaju 98 supstituiran s argininom; (ii) prolin na položaju 171 je supstituiran s glicinom; i (iii) alanin na položaju 180 je supstituiran s glutaminskom kiselinom; (b.1) linker sekvenca koja sadrži SEQ ID NO:31; i (c.1) Fc domena koja sadrži SEQ ID NO: 11; i drugi lanac koji sadrži: (a.2) polipeptid SEQ ID NO: 4, gdje je (i) leucin na položaju 98 supstituiran s argininom; (ii) prolin na položaju 171 je supstituiran s glicinom; i (iii) alanin na položaju 180 je supstituiran s glutaminskom kiselinom; (b.2) linker sekvenca koja sadrži SEQ ID NO:31; i (c.2) Fc domena koja sadrži SEQ ID NO:11.
HRP20240135TT 2009-05-05 2010-05-04 Fgf21 mutanti i njihove upotrebe HRP20240135T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17573609P 2009-05-05 2009-05-05
US28511809P 2009-12-09 2009-12-09
EP17167682.8A EP3248610B1 (en) 2009-05-05 2010-05-04 Fgf21 mutants and uses thereof

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HRP20240135T1 true HRP20240135T1 (hr) 2024-04-12

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US (4) US8188040B2 (hr)
EP (3) EP3248610B1 (hr)
JP (1) JP5823954B2 (hr)
KR (2) KR101860572B1 (hr)
CN (2) CN107188950B (hr)
AR (1) AR076541A1 (hr)
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BR (1) BRPI1011404B1 (hr)
CA (1) CA2760196C (hr)
CL (1) CL2011002768A1 (hr)
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ES (2) ES2632742T3 (hr)
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