DK2109457T3 - Terapeutisk anvendelse af serinprotease-hæmmere af kazal-type - Google Patents

Terapeutisk anvendelse af serinprotease-hæmmere af kazal-type Download PDF

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DK2109457T3
DK2109457T3 DK08707646.9T DK08707646T DK2109457T3 DK 2109457 T3 DK2109457 T3 DK 2109457T3 DK 08707646 T DK08707646 T DK 08707646T DK 2109457 T3 DK2109457 T3 DK 2109457T3
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DK08707646.9T
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Stefan Schulte
Ulrich Kronthaler
Stefan Schmidbauer
Thomas Weimer
Kay Hofmann
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Csl Behring Gmbh
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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
    • C07K14/81—Protease inhibitors
    • C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
    • C07K14/8135—Kazal type inhibitors, e.g. pancreatic secretory inhibitor, ovomucoid
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Biophysics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)

Claims (12)

1. Muterede Kazal-inhibitorer, der er afledt fra SPINK-1, hvor inhibitorerne udviser mere end 20 identiske aminosyrer med infestin-4 eller en konservativ substitution i stedet for identitet, dvs. en konservativ substitution i stedet for en identisk aminosyre, og som er egnet til forhindring af dannelse og/eller af stabilisering af tredimensionale arterielle eller venøse thromber, og hvor inhibitoren er udvalgt som tilhørende gruppen omfattende SPINK Kl, K2 og K3 (SEQ ID NO. 2, 3 og 4).
2. Muterede Kazal-inhibitorer ifølge krav 1, hvor inhibitorerne er sammenknyttet med polypeptider, der er forlængende halvlevetiden.
3. Inhibitorer ifølge krav 2, kendetegnet ved , at den halvlevetids-forlængende polypeptid er afledt fra et medlem af humant albumin-proteinfamilien, navnlig albumin, afamin, alpha-fetoprotein eller vitamin D bindende protein.
4. Inhibitorer ifølge krav 2 eller 3, kendetegnet ved , at det ved den halv-levetids-forlængende polypeptid drejer sig om humant albumin eller en variant eller et domæne eller en del deraf.
5. Inhibitorer ifølge krav 2, 3 eller 4, kendetegnet ved , at det ved den halvlevetids-forlængende polypeptid drejer sig om en immun globulin eller en del deraf.
6. Inhibitorer ifølge krav 5, kendetegnet ved, at det ved immun globulin-delen drejer sig om en igG-Fc-andel.
7. Inhibitorer ifølge krav 2, 3, 4, 5 eller 6, kendetegnet ved , at de halvlevetids-forlængende polypeptider er linket med Kasal-inhibitor-grupperingen via linkere, fortrinsvis kløvelige linkere.
8. Inhibitorer ifølge krav 7, kendetegnet ved , at linkeme er kløvelige ved koagulations-proteaser hørende til den intrinsiske koagulerings-forløbsvej.
9. Inhibitor ifølge krav 8, kendetegnet ved med FXIIa kløvelige linkere.
10. Pharmaceutisk produkt omfattende en inhibitor ifølge krav 1, 2, 3, 4, 5, 6, 7, 8 eller 9 eller omfattende en infestin eller et fragment deraf.
11. Inhibitor ifølge krav 1, 2, 3, 4, 5, 6, 7, 8 eller 9 og/eller infestin eller fragment deraf til anvendelse som et medikament.
12. Fremgangsmåde til fremstilling af en fra SPINK-1 afledt muteret Kazal-inhibitor ifølge et vilkårligt af kravene 1 til 9 ved hjælp af rekombination i eukaryotiske celler, bakterier, gær, plante- eller insekt-celler eller i transgenetiske dyr.
DK08707646.9T 2007-02-12 2008-02-11 Terapeutisk anvendelse af serinprotease-hæmmere af kazal-type DK2109457T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07002903 2007-02-12
PCT/EP2008/001009 WO2008098720A1 (en) 2007-02-12 2008-02-11 Therapeutic application of kazal-type serine protease inhibitors

Publications (1)

Publication Number Publication Date
DK2109457T3 true DK2109457T3 (da) 2016-04-11

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Application Number Title Priority Date Filing Date
DK08707646.9T DK2109457T3 (da) 2007-02-12 2008-02-11 Terapeutisk anvendelse af serinprotease-hæmmere af kazal-type
DK12175363.6T DK2526962T3 (da) 2007-02-12 2008-02-11 Therapeutic application of Kazal-type serine protease inhibitors

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DK12175363.6T DK2526962T3 (da) 2007-02-12 2008-02-11 Therapeutic application of Kazal-type serine protease inhibitors

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US (1) US8283319B2 (da)
EP (2) EP2526962B1 (da)
JP (1) JP2010518039A (da)
KR (1) KR101629702B1 (da)
CA (1) CA2678001C (da)
DK (2) DK2109457T3 (da)
ES (2) ES2566385T3 (da)
WO (1) WO2008098720A1 (da)

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Publication number Publication date
EP2526962A1 (en) 2012-11-28
US20100279923A1 (en) 2010-11-04
CA2678001C (en) 2017-07-11
JP2010518039A (ja) 2010-05-27
KR20090110936A (ko) 2009-10-23
EP2109457A1 (en) 2009-10-21
EP2526962B1 (en) 2019-08-14
AU2008214916A1 (en) 2008-08-21
US8283319B2 (en) 2012-10-09
WO2008098720A1 (en) 2008-08-21
CA2678001A1 (en) 2008-08-21
ES2566385T3 (es) 2016-04-12
DK2526962T3 (da) 2019-10-07
ES2753183T3 (es) 2020-04-07
EP2109457B1 (en) 2016-01-06
KR101629702B1 (ko) 2016-06-13

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