HRP20100663T1 - POBOLJSANI sgp 130Fc DIMERI - Google Patents

POBOLJSANI sgp 130Fc DIMERI Download PDF

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Publication number
HRP20100663T1
HRP20100663T1 HR20100663T HRP20100663T HRP20100663T1 HR P20100663 T1 HRP20100663 T1 HR P20100663T1 HR 20100663 T HR20100663 T HR 20100663T HR P20100663 T HRP20100663 T HR P20100663T HR P20100663 T1 HRP20100663 T1 HR P20100663T1
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polypeptide dimer
amino acid
dimer according
polypeptide
domain
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HR20100663T
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English (en)
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W�tzig Georg
Seegert Dirk
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Conaris Research Institute Ag
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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
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/715Receptors; Cell surface antigens; Cell surface determinants for cytokines; for lymphokines; for interferons
    • C07K14/7155Receptors; Cell surface antigens; Cell surface determinants for cytokines; for lymphokines; for interferons for interleukins [IL]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K19/00Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/20Interleukins [IL]
    • A61K38/204IL-6
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • 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
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants
    • CCHEMISTRY; METALLURGY
    • 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
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/715Receptors; Cell surface antigens; Cell surface determinants for cytokines; for lymphokines; for interferons
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/24Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
    • C07K16/244Interleukins [IL]
    • C07K16/248IL-6
    • CCHEMISTRY; METALLURGY
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
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  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
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  • Diabetes (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
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  • Peptides Or Proteins (AREA)
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Abstract

Polipeptidni dimer koji moze inhibirati aktivnost agonistickog kompleksa IL-6/sIL-6R i sadrzi dva monomera, gdje svaki od spomenutih monomera sadrzi (a) vanstanicni dio gp130 molekule ili (b) varijantu ili fragment spomenutog vanstanicnog dijela koji moze inhibirati aktivnost agonistickog kompleksa IL-6/sIL-6R, fuzioniran s Fc domenom IgG1 proteina i gdje je najmanje jedan aminokiselinski ostatak Leu235 zglobne regije Fc domene zamijenjen najmanje jednim hidrofilnim aminokiselinskim ostatkom. Patent sadrzi jos 16 patentnih zahtjeva.

Claims (17)

1. Polipeptidni dimer koji može inhibirati aktivnost agonističkog kompleksa IL-6/sIL-6R i sadrži dva monomera, gdje svaki od spomenutih monomera sadrži (a) vanstanični dio gp130 molekule ili (b) varijantu ili fragment spomenutog vanstaničnog dijela koji može inhibirati aktivnost agonističkog kompleksa IL-6/sIL-6R, fuzioniran s Fc domenom IgG1 proteina i gdje je najmanje jedan aminokiselinski ostatak Leu235 zglobne regije Fc domene zamijenjen najmanje jednim hidrofilnim aminokiselinskim ostatkom.
2. Polipeptidni dimer prema patentnom zahtjevu 1, naznačen time što je hidrofilni aminokiselinski ostatak Glu ili Asp.
3. Polipeptidni dimer prema patentnom zahtjevu 1 ili 2, naznačen time što je, dodatno, aminokiselinski ostatak Leu234 zglobne regije zamijenjen sa Phe ili Ala.
4. Polipeptidni dimer prema patentnom zahtjevu 3, naznačen time što su aminokiselinski ostaci Leu234 i/ili Gly237 zglobne regije zamijenjeni sa aminokiselinskim ostatkom Ala.
5. Polipeptidni dimer prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time što zglobna regija sadrži motiv aminokiselinske sekvence Ala234-Glu235-Gly236-Ala237 umjesto Leu234-Leu235-Gly236-Gly237.
6. Polipeptidni dimer prema patentnom zahtjevu 5, naznačen time što zglobna regija sadrži aminokiselinsku sekvencu Asp221-Lys222-Thr223-His224-Thr225-Cys226-Pr227-Pro228-Cys229-Pro230-Ala231-Pro232-Glu233-Ala234-Glu235-Gly236-Ala237-Pro238-Ser239-Val240.
7. Polipeptidni dimer prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time što je topljiva gp130 molekula ili njena varijanta direktno fuzionirana sa zglobnom regijom Fc domene IgG1 proteina ili preko fleksibilne polipeptidne poveznice.
8. Polipeptidni dimer prema patentnom zahtjevu 7, naznačen time što, poveznica je poveznica koja sadrži 2 do 50 aminokiselinskih ostataka nezavisno izabranih iz grupe koja se sastoji od glicina, serina, asparagina, treonina i alanina.
9. Polipeptidni dimer prema bilo kojem od patentnih zahtjeva 1 do 8, naznačen time što je jedno ili više N-glikolizacijskih mjesta umetnuto između topljive gp130 molekule ili njegove varijante ili fragmenta i Fc domene.
10. Polipeptidni dimer prema bilo kojem od patentnih zahtjeva 1 do 9, naznačen time što su monomeri međusobno vezani preko jednostavne kovalentne veze, fleksibilne peptidne poveznice ili jednog ili više disulfidnih mostova.
11. Polipeptidni dimer prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time što je najmanje jedan od monomera spomenutog dimera PEG-iliran.
12. Polinukleotid koji kodira monomer polipeptidnog dimera prema bilo kojem od patentnih zahtjeva 1 do 10.
13. Ekspresijski vektor koji sadrži polinukleotid prema patentnom zahtjevu 12.
14. Stanica domaćin koja sadrži ekspresijski vektor prema patentnom zahtjevu 13.
15. Postupak za proizvodnju polipeptidnog dimera prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time što obuhvaća kultiviranje stanice domaćina prema patentnom zahtjevu 14 i dobivanje monomera ili dimera iz spomenute stanice domaćina ili kulture.
16. Farmaceutska smjesa koja sadrži polipeptidni dimer kao što je definiran u bilo kojem od patentnih zahtjeva 1 do 11.
17. Uporaba polipeptidnog dimera kao što je definiran u bilo kojem od patentnih zahtjeva 1 do 11 za pripremu farmaceutskih smjesa za liječenje i/ili prevenciju resorpcije kostiju, hiperkalcemije, kaheksije, tumora ili druge vrste raka, autoimune bolesti, upalne ili atopične bolesti, infekcije, endokrinološkog poremećaja ili metaboličke ili kataboličke bolesti.
HR20100663T 2006-06-30 2010-12-01 POBOLJSANI sgp 130Fc DIMERI HRP20100663T1 (hr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06013668A EP1873166B1 (en) 2006-06-30 2006-06-30 Improved sgp 130Fc dimers

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HRP20100663T1 true HRP20100663T1 (hr) 2011-01-31

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US (3) US8895012B2 (hr)
EP (1) EP1873166B1 (hr)
JP (1) JP5417171B2 (hr)
KR (1) KR101474817B1 (hr)
CN (1) CN101484472B (hr)
AT (1) ATE480568T1 (hr)
AU (1) AU2007263939B2 (hr)
BR (1) BRPI0713063B8 (hr)
CA (1) CA2656440C (hr)
CY (1) CY1110973T1 (hr)
DE (1) DE602006016765D1 (hr)
DK (1) DK1873166T3 (hr)
EA (1) EA015620B1 (hr)
ES (1) ES2352561T3 (hr)
HR (1) HRP20100663T1 (hr)
PL (1) PL1873166T3 (hr)
PT (1) PT1873166E (hr)
RS (1) RS51544B (hr)
SI (1) SI1873166T1 (hr)
UA (1) UA95636C2 (hr)
WO (1) WO2008000516A2 (hr)

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Publication number Publication date
EP1873166B1 (en) 2010-09-08
ES2352561T3 (es) 2011-02-21
US20100028367A1 (en) 2010-02-04
US9573989B2 (en) 2017-02-21
UA95636C2 (en) 2011-08-25
CN101484472A (zh) 2009-07-15
WO2008000516A3 (en) 2008-03-27
WO2008000516B1 (en) 2008-05-08
AU2007263939B2 (en) 2011-11-24
JP2009540843A (ja) 2009-11-26
PL1873166T3 (pl) 2011-03-31
WO2008000516A2 (en) 2008-01-03
CY1110973T1 (el) 2015-06-11
AU2007263939A1 (en) 2008-01-03
CN101484472B (zh) 2013-07-24
CA2656440C (en) 2018-10-02
US9034817B2 (en) 2015-05-19
EA200802396A1 (ru) 2009-06-30
EP1873166A1 (en) 2008-01-02
US20140178378A1 (en) 2014-06-26
DK1873166T3 (da) 2010-12-20
KR101474817B1 (ko) 2014-12-22
BRPI0713063B1 (pt) 2019-10-08
SI1873166T1 (sl) 2011-01-31
US8895012B2 (en) 2014-11-25
PT1873166E (pt) 2010-12-09
RS51544B (en) 2011-06-30
EA015620B1 (ru) 2011-10-31
US20150361157A1 (en) 2015-12-17
KR20090037898A (ko) 2009-04-16
CA2656440A1 (en) 2008-01-03
DE602006016765D1 (de) 2010-10-21
BRPI0713063B8 (pt) 2021-05-25
JP5417171B2 (ja) 2014-02-12
BRPI0713063A2 (pt) 2012-04-17
ATE480568T1 (de) 2010-09-15

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