KR102373215B1 - 인자 Xa 유도체의 제조 - Google Patents

인자 Xa 유도체의 제조 Download PDF

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KR102373215B1
KR102373215B1 KR1020197000840A KR20197000840A KR102373215B1 KR 102373215 B1 KR102373215 B1 KR 102373215B1 KR 1020197000840 A KR1020197000840 A KR 1020197000840A KR 20197000840 A KR20197000840 A KR 20197000840A KR 102373215 B1 KR102373215 B1 KR 102373215B1
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acid sequence
amino acid
gly
glu
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KR20190019134A (ko
Inventor
마크 카바즈
파멜라 비 콘리
건민 루
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포톨라 파마슈티컬스, 인코포레이티드
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Application filed by 포톨라 파마슈티컬스, 인코포레이티드 filed Critical 포톨라 파마슈티컬스, 인코포레이티드
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    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • C12N9/48Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424Serine endopeptidases (3.4.21)
    • C12N9/6432Coagulation factor Xa (3.4.21.6)
    • 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
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46Hydrolases (3)
    • A61K38/48Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/482Serine endopeptidases (3.4.21)
    • A61K38/4846Factor 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)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/16Extraction; Separation; Purification by chromatography
    • C07K1/18Ion-exchange chromatography
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/16Extraction; Separation; Purification by chromatography
    • C07K1/20Partition-, reverse-phase or hydrophobic interaction chromatography
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/16Extraction; Separation; Purification by chromatography
    • C07K1/22Affinity chromatography or related techniques based upon selective absorption processes
    • 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
    • C07K14/745Blood coagulation or fibrinolysis factors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Wood Science & Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020197000840A 2016-06-17 2017-06-19 인자 Xa 유도체의 제조 Active KR102373215B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662351841P 2016-06-17 2016-06-17
US62/351,841 2016-06-17
PCT/US2017/038169 WO2017219034A2 (en) 2016-06-17 2017-06-19 Preparation of factor xa derivatives

Publications (2)

Publication Number Publication Date
KR20190019134A KR20190019134A (ko) 2019-02-26
KR102373215B1 true KR102373215B1 (ko) 2022-03-10

Family

ID=60663351

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KR1020197000840A Active KR102373215B1 (ko) 2016-06-17 2017-06-19 인자 Xa 유도체의 제조

Country Status (22)

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US (4) US10604748B2 (enExample)
EP (3) EP3472314B1 (enExample)
JP (3) JP6959268B2 (enExample)
KR (1) KR102373215B1 (enExample)
CN (3) CN116425860B (enExample)
AU (2) AU2017283720C1 (enExample)
CA (1) CA3027457A1 (enExample)
CL (2) CL2018003654A1 (enExample)
CO (1) CO2019000120A2 (enExample)
DK (1) DK3472314T3 (enExample)
EA (1) EA037815B1 (enExample)
ES (2) ES3038834T3 (enExample)
HU (1) HUE054597T2 (enExample)
IL (1) IL263591B2 (enExample)
MX (1) MX2018015873A (enExample)
PE (1) PE20190661A1 (enExample)
PH (1) PH12018502614A1 (enExample)
PL (1) PL3472314T3 (enExample)
PT (1) PT3472314T (enExample)
SG (1) SG11201810915QA (enExample)
SI (1) SI3472314T1 (enExample)
WO (1) WO2017219034A2 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3604510B1 (en) * 2009-03-30 2025-03-26 Alexion Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
SG10201705189XA (en) * 2013-01-24 2017-07-28 Portola Pharm Inc INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR Xa DERIVATIVES
EP3472314B1 (en) * 2016-06-17 2021-05-05 Alexion Pharmaceuticals, Inc. Preparation of factor xa derivatives
US12195774B2 (en) 2018-06-19 2025-01-14 Alexion Pharmaceuticals, Inc. Antidotes to factor XA inhibitors
KR102337683B1 (ko) * 2018-09-21 2021-12-13 주식회사 녹십자 고효율 항-tfpi 항체 조성물

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5589571A (en) 1994-10-28 1996-12-31 Cor Therapeutics, Inc. Process for production of inhibited forms of activated blood factors
WO2014116275A1 (en) 2013-01-24 2014-07-31 Portola Pharmaceuticals, Inc. INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR Xa DERIVATIVES
US20150025011A1 (en) 2009-07-15 2015-01-22 Portola Pharmaceuticals, Inc. Unit dose formulation of antidotes for factor xa inhibitors and methods of using the same

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5189019A (en) * 1990-04-23 1993-02-23 Merck & Co., Inc. Antistasin derived anticoagulant protein
JPH1066572A (ja) * 1996-08-29 1998-03-10 Showa Sangyo Co Ltd 高純度の大豆トリプシンインヒビターの製造方法
CA2401778C (en) 2000-02-29 2010-12-21 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
PT1948608E (pt) 2005-11-08 2012-05-24 Millennium Pharm Inc Novos sais farmacêuticos e polimorfos de um inibidor do fator xa
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
EP3604510B1 (en) * 2009-03-30 2025-03-26 Alexion Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
CA2876361C (en) * 2012-06-14 2020-06-30 Portola Pharmaceuticals, Inc. Method for purification of recombinant factor xa derivatives
US20140346397A1 (en) * 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
KR101988705B1 (ko) * 2013-09-24 2019-06-12 화이자 인코포레이티드 재조합 인간 응고 인자 Xa 단백질의 이질적 집단을 포함하는 조성물
AU2015305413B2 (en) * 2014-08-20 2020-09-24 Alexion Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
EP3472314B1 (en) * 2016-06-17 2021-05-05 Alexion Pharmaceuticals, Inc. Preparation of factor xa derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5589571A (en) 1994-10-28 1996-12-31 Cor Therapeutics, Inc. Process for production of inhibited forms of activated blood factors
US20150025011A1 (en) 2009-07-15 2015-01-22 Portola Pharmaceuticals, Inc. Unit dose formulation of antidotes for factor xa inhibitors and methods of using the same
WO2014116275A1 (en) 2013-01-24 2014-07-31 Portola Pharmaceuticals, Inc. INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR Xa DERIVATIVES

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Protein Science, 2009, Vol.18, pp.1023-1032

Also Published As

Publication number Publication date
JP2022000477A (ja) 2022-01-04
KR20190019134A (ko) 2019-02-26
IL263591A (en) 2019-02-03
CN118271391A (zh) 2024-07-02
EA037815B1 (ru) 2021-05-25
JP6959268B2 (ja) 2021-11-02
US11845966B2 (en) 2023-12-19
AU2023200825A1 (en) 2023-03-16
ES3038834T3 (en) 2025-10-15
WO2017219034A2 (en) 2017-12-21
PE20190661A1 (es) 2019-05-08
CN110167575B (zh) 2024-03-15
US20170369862A1 (en) 2017-12-28
CL2020001733A1 (es) 2020-09-25
AU2017283720B2 (en) 2022-11-17
EP4588932A3 (en) 2025-10-01
US10604748B2 (en) 2020-03-31
US10954504B2 (en) 2021-03-23
JP7273918B2 (ja) 2023-05-15
US20200208131A1 (en) 2020-07-02
CO2019000120A2 (es) 2019-03-29
EP3472314B1 (en) 2021-05-05
AU2017283720A1 (en) 2019-01-03
ES2875538T3 (es) 2021-11-10
HUE054597T2 (hu) 2021-09-28
PH12018502614A1 (en) 2019-09-30
CL2018003654A1 (es) 2019-01-25
CN116425860B (zh) 2025-03-04
JP2023086970A (ja) 2023-06-22
SG11201810915QA (en) 2019-01-30
IL263591B2 (en) 2023-03-01
EP3472314A2 (en) 2019-04-24
EP4588932A2 (en) 2025-07-23
CA3027457A1 (en) 2017-12-21
AU2017283720C1 (en) 2024-07-25
EA201990052A1 (ru) 2019-05-31
MX2018015873A (es) 2019-08-12
PL3472314T3 (pl) 2021-11-22
EP3926044A1 (en) 2021-12-22
IL263591B (en) 2022-11-01
CN110167575A (zh) 2019-08-23
JP2019528242A (ja) 2019-10-10
US20240076642A1 (en) 2024-03-07
US20210348149A1 (en) 2021-11-11
EP3926044B1 (en) 2025-06-04
CN116425860A (zh) 2023-07-14
BR112018075964A2 (pt) 2019-04-02
WO2017219034A3 (en) 2019-03-14
SI3472314T1 (sl) 2021-11-30
EP3472314A4 (en) 2020-01-22
DK3472314T3 (da) 2021-07-26
PT3472314T (pt) 2021-06-18

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