ES2503570T3 - Conjugado del factor de coagulación sanguíneo VIIA y PEG - Google Patents

Conjugado del factor de coagulación sanguíneo VIIA y PEG Download PDF

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Publication number
ES2503570T3
ES2503570T3 ES11719041.3T ES11719041T ES2503570T3 ES 2503570 T3 ES2503570 T3 ES 2503570T3 ES 11719041 T ES11719041 T ES 11719041T ES 2503570 T3 ES2503570 T3 ES 2503570T3
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Prior art keywords
conjugate
fviia
bond
peg
blood clotting
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ES11719041.3T
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William Henry
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Abzena UK Ltd
Cantab Biopharmaceuticals Patents Ltd
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Polytherics Ltd
Cantab Biopharmaceuticals Patents Ltd
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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
    • C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
    • 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
    • A61K47/56—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/36—Blood coagulation or fibrinolysis factors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/006—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length of peptides containing derivatised side chain amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/113—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure
    • C07K1/1133—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure by redox-reactions involving cystein/cystin side chains
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Wood Science & Technology (AREA)
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  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Microbiology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Un conjugado factor FVIIa-polietilenglicol, donde uno o más grupos polietilenglicol están conjugados con FVIIa mediante un grupo conector que hace de puente entre los átomos de azufre de dos residuos de cisteína que formaban un enlace disulfuro en FVIIa, donde el conjugado tiene la estructura:**Fórmula** donde R1 es un sustituyente que es un enlace directo, un grupo alquileno (preferentemente un grupo alquileno C1- 10), o un grupo arilo o heteroarilo opcionalmente sustituido; donde los grupos arilo incluyen grupos fenilo, benzoílo o naftilo; donde los grupos heteroarilo adecuados incluyen piridina, pirrol, furano, pirano, imidazol, pirazol, oxazol, piridazina, pirimidina y purina; donde la unión al polímero es por medio de un enlace hidrolíticamente lábil o mediante un enlace no lábil.

Description

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Claims (1)

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ES11719041.3T 2010-04-30 2011-04-28 Conjugado del factor de coagulación sanguíneo VIIA y PEG Active ES2503570T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB201007356 2010-04-30
GBGB1007356.7A GB201007356D0 (en) 2010-04-30 2010-04-30 Conjugated factor VIIa
PCT/GB2011/000663 WO2011135308A1 (en) 2010-04-30 2011-04-28 Conjugated blood coagulation factor viia

Publications (1)

Publication Number Publication Date
ES2503570T3 true ES2503570T3 (es) 2014-10-07

Family

ID=42289986

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11719041.3T Active ES2503570T3 (es) 2010-04-30 2011-04-28 Conjugado del factor de coagulación sanguíneo VIIA y PEG

Country Status (28)

Country Link
US (1) US9309507B2 (es)
EP (1) EP2563403B1 (es)
JP (2) JP2013525415A (es)
KR (1) KR20130055620A (es)
CN (1) CN102971013B (es)
AP (1) AP2012006574A0 (es)
AU (1) AU2011247148B2 (es)
CA (1) CA2796870A1 (es)
CL (1) CL2012003038A1 (es)
CO (1) CO6660500A2 (es)
CR (1) CR20120580A (es)
DK (1) DK2563403T3 (es)
EA (1) EA201290941A1 (es)
EC (1) ECSP12012315A (es)
ES (1) ES2503570T3 (es)
GB (2) GB201007356D0 (es)
IL (1) IL222565A (es)
MX (1) MX2012012684A (es)
MY (1) MY160510A (es)
NI (1) NI201200161A (es)
NZ (1) NZ603938A (es)
PE (1) PE20130253A1 (es)
PH (1) PH12012502149A1 (es)
PL (1) PL2563403T3 (es)
RU (1) RU2012144554A (es)
SG (1) SG184573A1 (es)
WO (1) WO2011135308A1 (es)
ZA (1) ZA201208988B (es)

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Publication number Publication date
RU2012144554A (ru) 2014-06-10
GB2492738A8 (en) 2014-03-05
PE20130253A1 (es) 2013-03-16
PH12012502149A1 (en) 2013-02-04
JP2013525415A (ja) 2013-06-20
SG184573A1 (en) 2012-11-29
GB2492738B (en) 2014-05-21
CR20120580A (es) 2013-04-25
IL222565A (en) 2015-10-29
US20130129698A1 (en) 2013-05-23
PL2563403T3 (pl) 2015-03-31
IL222565A0 (en) 2012-12-31
GB2492738A (en) 2013-01-09
CA2796870A1 (en) 2011-11-03
CL2012003038A1 (es) 2014-01-24
GB201220669D0 (en) 2013-01-02
MX2012012684A (es) 2013-04-03
AP2012006574A0 (en) 2012-12-31
DK2563403T3 (da) 2014-09-15
MY160510A (en) 2017-03-15
WO2011135308A1 (en) 2011-11-03
EP2563403A1 (en) 2013-03-06
JP2015110636A (ja) 2015-06-18
GB201007356D0 (en) 2010-06-16
CN102971013A (zh) 2013-03-13
US9309507B2 (en) 2016-04-12
KR20130055620A (ko) 2013-05-28
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NI201200161A (es) 2013-04-19
ECSP12012315A (es) 2013-05-31
EA201290941A1 (ru) 2013-04-30
EP2563403B1 (en) 2014-06-18
CO6660500A2 (es) 2013-04-30
ZA201208988B (en) 2014-02-26
CN102971013B (zh) 2015-01-07
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