SI2068907T1 - Z glicerolom povezani pegilirani sladkorji in glikopeptidi - Google Patents

Z glicerolom povezani pegilirani sladkorji in glikopeptidi Download PDF

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SI2068907T1
SI2068907T1 SI200731992T SI200731992T SI2068907T1 SI 2068907 T1 SI2068907 T1 SI 2068907T1 SI 200731992 T SI200731992 T SI 200731992T SI 200731992 T SI200731992 T SI 200731992T SI 2068907 T1 SI2068907 T1 SI 2068907T1
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substituted
glycopeptides
independently selected
unsubstituted alkyl
sugars
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SI200731992T
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Shawn Defrees
Xiao Zeng
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Novo Nordisk A/S
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    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
    • A—HUMAN NECESSITIES
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    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/482—Serine endopeptidases (3.4.21)
    • A61K38/4846—Factor VII (3.4.21.21); Factor IX (3.4.21.22); Factor Xa (3.4.21.6); Factor XI (3.4.21.27); Factor XII (3.4.21.38)
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/59—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6437—Coagulation factor VIIa (3.4.21.21)
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    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21021—Coagulation factor VIIa (3.4.21.21)
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    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21022—Coagulation factor IXa (3.4.21.22)

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  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
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  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Claims (2)

  1. Z GLICEROLOM POVEZANI PEGILIRANI SLADKORJI IN GLIKOPEPTIDI EP 2 068 907 B1 PATENTNI ZAHTEVKI
    1. Peptidni konjugati, ki obsegajo: a) peptid, ki je Faktor IX, in ki je kovalentno vezan na delec, ki je izbran izmed:
    kjer sta navedena m in n celi števili, neodvisno izbrani od 100 do 4000, kjer je R2 izbran izmed H, CH2OR7, COOR7 in OR7, kjer je R7 izbran izmed H, substituiranega ali nesubstituiranega alkila in substituiranega ali nesubstituiranega heteroalkila ali kjer je omenjeni delec:
    kjer so m, n in R2, kot je definirano zgoraj, in kjer sta R3 in R4 člena, neodvisno izbrana izmed H, substituiranega ali nesubstituiranega alkila, OR8 in NHC(0)R9, in kjer sta R8 in R9 neodvisno izbrana izmed H, substituiranega ali nesubstituiranega alkila, substituiranega ali nesubstituiranega heteroalkila, sialne kisline in polisialne kisline.
  2. 2. Farmacevtska formulacija, ki obsega peptidni konjugat po zahtevku 1 in farmacevtsko sprejemljivo razredčilo.
SI200731992T 2006-10-04 2007-10-04 Z glicerolom povezani pegilirani sladkorji in glikopeptidi SI2068907T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US82820806P 2006-10-04 2006-10-04
PCT/US2007/080471 WO2008060780A2 (en) 2006-10-04 2007-10-04 Glycerol linked pegylated sugars and glycopeptides
EP07868373.7A EP2068907B1 (en) 2006-10-04 2007-10-04 Glycerol linked pegylated sugars and glycopeptides

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SI2068907T1 true SI2068907T1 (sl) 2018-01-31

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US (4) US20080146782A1 (sl)
EP (1) EP2068907B1 (sl)
JP (1) JP5457185B2 (sl)
KR (1) KR101556248B1 (sl)
CN (1) CN101600448B (sl)
AU (1) AU2007319657B9 (sl)
BR (1) BRPI0717505B8 (sl)
CA (1) CA2665480C (sl)
CY (2) CY1119943T1 (sl)
DK (1) DK2068907T3 (sl)
ES (1) ES2655734T3 (sl)
HU (2) HUE036502T2 (sl)
IL (1) IL197770A (sl)
LT (2) LT2068907T (sl)
LU (1) LUC00075I2 (sl)
MX (1) MX2009003470A (sl)
PL (1) PL2068907T3 (sl)
PT (1) PT2068907T (sl)
RU (1) RU2460543C2 (sl)
SI (1) SI2068907T1 (sl)
WO (1) WO2008060780A2 (sl)

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