CA2747065A1 - Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders - Google Patents

Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders Download PDF

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Publication number
CA2747065A1
CA2747065A1 CA2747065A CA2747065A CA2747065A1 CA 2747065 A1 CA2747065 A1 CA 2747065A1 CA 2747065 A CA2747065 A CA 2747065A CA 2747065 A CA2747065 A CA 2747065A CA 2747065 A1 CA2747065 A1 CA 2747065A1
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CA
Canada
Prior art keywords
seq
protein
factor
chimeric
derivative
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2747065A
Other languages
English (en)
French (fr)
Inventor
Olivier Christophe
Cecile Denis
Ghislaine Cherel
Paul Gueguen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Institut National de la Santé et de la Recherche Médicale
Original Assignee
Institut National de la Santé et de la Recherche Médicale
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from EP08305990A external-priority patent/EP2199387A1/en
Application filed by Institut National de la Santé et de la Recherche Médicale filed Critical Institut National de la Santé et de la Recherche Médicale
Publication of CA2747065A1 publication Critical patent/CA2747065A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • 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)
CA2747065A 2008-12-19 2009-12-21 Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders Abandoned CA2747065A1 (en)

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 (1)

Publication Number Publication Date
CA2747065A1 true CA2747065A1 (en) 2010-06-24

Family

ID=41718355

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2747065A Abandoned CA2747065A1 (en) 2008-12-19 2009-12-21 Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders

Country Status (9)

Country Link
US (3) US8436144B2 (enExample)
EP (1) EP2358874B1 (enExample)
JP (1) JP5833448B2 (enExample)
KR (1) KR20110114587A (enExample)
CN (2) CN104262479A (enExample)
AU (1) AU2009329493B2 (enExample)
CA (1) CA2747065A1 (enExample)
ES (1) ES2629099T3 (enExample)
WO (1) WO2010070137A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX336958B (es) * 2005-11-15 2016-02-05 Philadelphia Children Hospital Metodos y composiciones para modular la hemostasia.
KR102069498B1 (ko) 2007-09-28 2020-01-23 포톨라 파마슈티컬스, 인코포레이티드 인자 Ｘａ 저해제에 대한 안티도트 및 그것을 사용하는 방법
CA2743496C (en) 2008-11-14 2018-03-27 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
JP5833448B2 (ja) * 2008-12-19 2015-12-16 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 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
PL3604510T3 (pl) 2009-03-30 2025-07-28 Alexion Pharmaceuticals, Inc. Antidota na inhibitory czynnika xa i sposoby ich stosowania
EP2453910B1 (en) 2009-07-15 2016-08-31 Portola Pharmaceuticals, Inc. Unit dose formulation of antidote for factor xa inhibitors for use in preventing bleeding
JP6514893B2 (ja) * 2011-09-30 2019-05-15 ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィアＴｈｅ Ｃｈｉｌｄｒｅｎ’Ｓ Ｈｏｓｐｉｔａｌ Ｏｆ Ｐｈｉｌａｄｅｌｐｈｉａ 止血を調節するための組成物および方法
KR102049900B1 (ko) 2012-07-25 2019-11-28 카탈리스트 바이오사이언시즈, 인코포레이티드 변형 인자 x 폴리펩티드 및 이의 용도
HK1215196A1 (zh) 2013-01-31 2016-08-19 辉瑞公司 用於抵消因子xa抑制的组合物和方法
FR3001729B1 (fr) * 2013-02-04 2015-03-06 Lab Francais Du Fractionnement Mutants du facteur x
CN105008530A (zh) * 2013-03-12 2015-10-28 诺和诺德股份有限公司 凝血酶敏感性凝固因子x分子
CN112195169A (zh) 2013-09-24 2021-01-08 辉瑞大药厂 包含重组人凝血因子Xa蛋白的异质性群体的组合物
US10676730B2 (en) 2015-01-07 2020-06-09 Inserm (Institut National De La Sante Et De La Recherche Medicale) 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

Family Cites Families (18)

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Publication number Priority date Publication date Assignee Title
US4861719A (en) 1986-04-25 1989-08-29 Fred Hutchinson Cancer Research Center DNA constructs for retrovirus packaging cell lines
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
JP3866760B2 (ja) 1993-02-22 2007-01-10 ザ ロックフェラー ユニバーシティ 一過性トランスフェクションによる高力価のヘルパーフリーのレトロウイルスの生産
FR2712812B1 (fr) 1993-11-23 1996-02-09 Centre Nat Rech Scient Composition pour la production de produits thérapeutiques in vivo.
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
US6013516A (en) 1995-10-06 2000-01-11 The Salk Institute For Biological Studies Vector and method of use for nucleic acid delivery to non-dividing cells
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
EP1651252B1 (en) 2003-07-08 2014-11-26 The Scripps Research Institute Activated protein c variants with normal cytoprotective activity but reduced anticoagulant activity
EP1769092A4 (en) 2004-06-29 2008-08-06 Europ Nickel Plc IMPROVED LIXIVIATION OF BASE METALS
RU2396347C2 (ru) * 2004-08-17 2010-08-10 Ксл Бехринг Гмбх Модифицированные витамин к-зависимые полипептиды
EP1820508A1 (en) * 2006-02-21 2007-08-22 CSL Behring GmbH Coagulation factor X polypeptides with modified activation properties
CN101765560B (zh) 2007-08-01 2012-09-26 陶氏环球技术公司 制备层状剥离石墨烯的高效率方法
JP5833448B2 (ja) * 2008-12-19 2015-12-16 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 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

Also Published As

Publication number Publication date
AU2009329493B2 (en) 2014-09-18
CN102325880B (zh) 2014-10-01
EP2358874A1 (en) 2011-08-24
EP2358874B1 (en) 2017-03-29
US8518400B2 (en) 2013-08-27
ES2629099T3 (es) 2017-08-07
US20130261060A1 (en) 2013-10-03
AU2009329493A1 (en) 2011-07-21
JP5833448B2 (ja) 2015-12-16
US20110293597A1 (en) 2011-12-01
US20130101570A1 (en) 2013-04-25
US8741286B2 (en) 2014-06-03
US8436144B2 (en) 2013-05-07
CN102325880A (zh) 2012-01-18
JP2012512645A (ja) 2012-06-07
KR20110114587A (ko) 2011-10-19
CN104262479A (zh) 2015-01-07
WO2010070137A1 (en) 2010-06-24

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EEER Examination request

Effective date: 20141128

FZDE Discontinued

Effective date: 20170606