JP5833448B2 - セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用 - Google Patents

セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用 Download PDF

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JP5833448B2
JP5833448B2 JP2011541497A JP2011541497A JP5833448B2 JP 5833448 B2 JP5833448 B2 JP 5833448B2 JP 2011541497 A JP2011541497 A JP 2011541497A JP 2011541497 A JP2011541497 A JP 2011541497A JP 5833448 B2 JP5833448 B2 JP 5833448B2
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factor
seq
protein
amino acid
derivative
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JP2012512645A (ja
JP2012512645A5 (enExample
Inventor
クリストフ，オリヴィエ
ドゥニ，セシール
シュレル，ギスレーヌ
ゲゲン，ポール
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Institut National de la Sante et de la Recherche Medicale INSERM
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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
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745—Blood coagulation or fibrinolysis factors
    • 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
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • 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
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K19/00—Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
    • 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
    • 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)
    • C12N9/6429—Thrombin (3.4.21.5)
    • 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)
    • C12N9/6432—Coagulation factor Xa (3.4.21.6)
    • 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)
    • C12N9/6464—Protein C (3.4.21.69)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21005—Thrombin (3.4.21.5)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21006—Coagulation factor Xa (3.4.21.6)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21069—Protein C activated (3.4.21.69)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide

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  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Hematology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2011541497A 2008-12-19 2009-12-21 セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用 Expired - Fee Related JP5833448B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP08305990.7 2008-12-19
EP08305990A EP2199387A1 (en) 2008-12-19 2008-12-19 Serine protease derivatives and uses for the prevention and/or the treatment of blood coagulation disorders
EP09305349.4 2009-04-23
EP09305349 2009-04-23
US22296009P 2009-07-03 2009-07-03
US61/222960 2009-07-03
PCT/EP2009/067632 WO2010070137A1 (en) 2008-12-19 2009-12-21 Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders

Publications (3)

Publication Number Publication Date
JP2012512645A JP2012512645A (ja) 2012-06-07
JP2012512645A5 JP2012512645A5 (enExample) 2013-02-14
JP5833448B2 true JP5833448B2 (ja) 2015-12-16

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JP2011541497A Expired - Fee Related JP5833448B2 (ja) 2008-12-19 2009-12-21 セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用

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US (3) US8436144B2 (enExample)
EP (1) EP2358874B1 (enExample)
JP (1) JP5833448B2 (enExample)
KR (1) KR20110114587A (enExample)
CN (2) CN102325880B (enExample)
AU (1) AU2009329493B2 (enExample)
CA (1) CA2747065A1 (enExample)
ES (1) ES2629099T3 (enExample)
WO (1) WO2010070137A1 (enExample)

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* Cited by examiner, † Cited by third party
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MX2008006313A (es) * 2005-11-15 2008-11-06 Philadelphia Children Hospital Metodos y composiciones para modular la hemostasia.
PT3078743T (pt) 2007-09-28 2020-07-15 Portola Pharm Inc Antídotos para inibidores do fator xa e métodos de utilização dos mesmos
US8455439B2 (en) 2008-11-14 2013-06-04 Portola Pharmaceuticals, Inc. Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents
US8436144B2 (en) * 2008-12-19 2013-05-07 Institut National De La Sante Et De La Recherche Medicale (Inserm) Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders
EP3604510B1 (en) 2009-03-30 2025-03-26 Alexion Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
WO2011008885A1 (en) 2009-07-15 2011-01-20 Portola Pharmaceuticals, Inc. Unit dose formulation of antidotes for factor xa inhibitors and methods of using the same
EP2760887B1 (en) * 2011-09-30 2024-10-23 The Children's Hospital of Philadelphia Compositions and methods for modulating hemostasis
AU2013293573B2 (en) * 2012-07-25 2016-10-27 Catalyst Biosciences, Inc. Modified Factor X polypeptides and uses thereof
ES2761730T3 (es) 2013-01-31 2020-05-20 Pfizer Composiciones y procedimientos para contrarrestar la inhibición del factor Xa
FR3001729B1 (fr) * 2013-02-04 2015-03-06 Lab Francais Du Fractionnement Mutants du facteur x
JP2016510984A (ja) * 2013-03-12 2016-04-14 ノヴォ ノルディスク アー／エス トロンビン感受性凝固第ｘ因子分子
KR101988705B1 (ko) 2013-09-24 2019-06-12 화이자 인코포레이티드 재조합 인간 응고 인자 Xa 단백질의 이질적 집단을 포함하는 조성물
EP3242936A1 (en) * 2015-01-07 2017-11-15 INSERM (Institut National de la Santé et de la Recherche Médicale) Mutated factor x polypeptides and uses thereof for the treatment of haemophilia
EP3328998A1 (en) * 2015-07-27 2018-06-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Mutated factor x polypeptides and uses thereof for the treatment of haemophilia

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US4992373A (en) 1987-12-04 1991-02-12 Eli Lilly And Company Vectors and compounds for direct expression of activated human protein C
US5278056A (en) 1988-02-05 1994-01-11 The Trustees Of Columbia University In The City Of New York Retroviral packaging cell lines and process of using same
US4981952A (en) 1988-10-04 1991-01-01 Eli Lilly And Company Method for the purification of vitamin K-dependent proteins
US5670488A (en) 1992-12-03 1997-09-23 Genzyme Corporation Adenovirus vector for gene therapy
MY110664A (en) 1992-05-21 1999-01-30 Lilly Co Eli Protein c derivatives
AU6248994A (en) 1993-02-22 1994-09-14 Rockefeller University, The Production of high titer helper-free retroviruses by transient transfection
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IL116816A (en) 1995-01-20 2003-05-29 Rhone Poulenc Rorer Sa Cell for the production of a defective recombinant adenovirus or an adeno-associated virus and the various uses thereof
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FR2831170B1 (fr) * 2001-10-19 2004-03-19 Inst Nat Sante Rech Med Proteines c modifiees activables directement par la thrombine
FR2841904B1 (fr) 2002-07-03 2004-08-20 Inst Nat Sante Rech Med Analogues de facteurs x clivables par la thrombine
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JP2008509688A (ja) * 2004-08-17 2008-04-03 ツェー・エス・エル・ベーリング・ゲー・エム・ベー・ハー 改変ビタミンｋ依存性ポリペプチド
EP1820508A1 (en) * 2006-02-21 2007-08-22 CSL Behring GmbH Coagulation factor X polypeptides with modified activation properties
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Also Published As

Publication number Publication date
US20130261060A1 (en) 2013-10-03
US8436144B2 (en) 2013-05-07
AU2009329493B2 (en) 2014-09-18
CN104262479A (zh) 2015-01-07
US8518400B2 (en) 2013-08-27
EP2358874A1 (en) 2011-08-24
JP2012512645A (ja) 2012-06-07
US20110293597A1 (en) 2011-12-01
CN102325880B (zh) 2014-10-01
CN102325880A (zh) 2012-01-18
KR20110114587A (ko) 2011-10-19
EP2358874B1 (en) 2017-03-29
US8741286B2 (en) 2014-06-03
US20130101570A1 (en) 2013-04-25
WO2010070137A1 (en) 2010-06-24
AU2009329493A1 (en) 2011-07-21
ES2629099T3 (es) 2017-08-07
CA2747065A1 (en) 2010-06-24

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