DK3045183T3 - Pegyleret apelin og anvendelser deraf - Google Patents

Pegyleret apelin og anvendelser deraf Download PDF

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Publication number
DK3045183T3
DK3045183T3 DK16155181.7T DK16155181T DK3045183T3 DK 3045183 T3 DK3045183 T3 DK 3045183T3 DK 16155181 T DK16155181 T DK 16155181T DK 3045183 T3 DK3045183 T3 DK 3045183T3
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DK
Denmark
Prior art keywords
apelin
peg
molecule
pegylated
disease
Prior art date
Application number
DK16155181.7T
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English (en)
Inventor
Zhiqiang Jia
Hou Lihui
Clark Q Pan
Geoffrey Y Akita
Original Assignee
Genzyme Corp
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.)
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Publication date
Application filed by Genzyme Corp filed Critical Genzyme Corp
Application granted granted Critical
Publication of DK3045183T3 publication Critical patent/DK3045183T3/da

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    • 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
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • 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
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Organic Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (11)

1. Pegyleret apelin 36-molekyle, der omfatter et eller flere polyethylenglycol (PEG)-molekyler, der er operabelt koblet til en leucin i N-terminalen af apelin 36.
2. Molekyle ifølge krav 1, hvor det pegylerede apelin 36 er i stand til at fremvise en forlænget cirkulationstid eller en forlænget inotrop virkning i forhold til ikke-pegyleret apelin 36.
3. Molekyle ifølge krav 1, hvor det pegylerede apelin 36 er et monopegyleret eller et dipegyleret apelin 36.
4. Molekyle ifølge krav 1, hvor det ene eller de flere PEG-molekyler er kovalent bundet til aminosyreresten enten direkte eller via en linker.
5. Molekyle ifølge krav 1, hvor hvert PEG-molekyle har en molekylvægt i intervallet fra ca. 5.000 til ca. 50.000 dalton.
6. Molekyle ifølge krav 1, hvor det pegylerede apelin 36 omfatter monomert apelin 36.
7. Molekyle ifølge krav 1, hvor det pegylerede apelin 36 omfatter et oligomert apelin 36, hvor en eller flere monomerer er operabelt koblet til hinanden.
8. Molekyle ifølge krav 1, hvor apelin 36 omfatter aminosyresekvensen ifølge aminosyreresterne 42-77 af SEQ ID NO: 1.
9. Molekyle ifølge krav 8, hvor aminosyresekvensen kodes af en nukleinsyresekvens, som er 123-234 bp af SEQ ID NO: 2.
10. Pegyleret apelin 36-molekyle ifølge et hvilket som helst af kravene 1-8 til anvendelse som et medikament.
11. Terapeutisk effektiv mængde af det pegylerede apelin 36-molekyle ifølge et hvilket som helst af kravene 1-8 til anvendelse til behandling af en sygdom eller forstyrrelse, der er forbundet med apelin, hvor sygdommen eller forstyrrelsen er en kardiovaskulær sygdom, en iskæmireperfusionsskade, myokardieinfarkt, akut dekompenseret hjerteinsufficiens, kronisk hjerteinsufficiens, kardiomyopati, endokrin forstyrrelse, metabolisk forstyrrelse eller pulmonal hypertension hos et menneske.
DK16155181.7T 2011-03-11 2012-03-08 Pegyleret apelin og anvendelser deraf DK3045183T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161451623P 2011-03-11 2011-03-11
EP12757055.4A EP2683360B1 (en) 2011-03-11 2012-03-08 Pegylated apelin and uses thereof

Publications (1)

Publication Number Publication Date
DK3045183T3 true DK3045183T3 (da) 2018-10-22

Family

ID=46831054

Family Applications (2)

Application Number Title Priority Date Filing Date
DK16155181.7T DK3045183T3 (da) 2011-03-11 2012-03-08 Pegyleret apelin og anvendelser deraf
DK12757055.4T DK2683360T3 (da) 2011-03-11 2012-03-08 Pegyleret apelin og anvendelser deraf

Family Applications After (1)

Application Number Title Priority Date Filing Date
DK12757055.4T DK2683360T3 (da) 2011-03-11 2012-03-08 Pegyleret apelin og anvendelser deraf

Country Status (14)

Country Link
US (1) US20140142049A1 (da)
EP (2) EP2683360B1 (da)
AU (2) AU2012229336B2 (da)
CA (1) CA2829693C (da)
CY (1) CY1117654T1 (da)
DK (2) DK3045183T3 (da)
ES (2) ES2690147T3 (da)
HR (2) HRP20160547T1 (da)
HU (1) HUE027579T2 (da)
LT (1) LT3045183T (da)
PL (2) PL3045183T3 (da)
PT (1) PT3045183T (da)
SI (2) SI3045183T1 (da)
WO (1) WO2012125408A1 (da)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3045183T1 (sl) 2011-03-11 2018-11-30 Genzyme Corporation Pegiliran Apelin in njegove uporabe
US20160067347A1 (en) * 2012-12-20 2016-03-10 Amgen Inc. Apj receptor agonists and uses thereof
US9353163B2 (en) 2013-03-14 2016-05-31 Regeneron Pharmaceuticals, Inc. Apelin fusion proteins and uses thereof
HK1218252A1 (zh) 2013-07-25 2017-02-10 Novartis Ag 合成apelin多肽之生物结合物
KR20160031551A (ko) 2013-07-25 2016-03-22 노파르티스 아게 심부전의 치료를 위한 시클릭 폴리펩티드
CN105612174A (zh) * 2013-07-25 2016-05-25 诺华股份有限公司 用于治疗心力衰竭的二硫化物环状多肽
WO2015013165A1 (en) * 2013-07-25 2015-01-29 Novartis Ag Cyclic apelin derivatives for the treatment of heart failure
WO2015077491A1 (en) 2013-11-20 2015-05-28 Regeneron Pharmaceuticals, Inc. Aplnr modulators and uses thereof
DK3122764T3 (da) 2014-03-25 2019-04-15 Lanthiopep Bv Cykliske apelin-analoger
WO2015191781A2 (en) * 2014-06-10 2015-12-17 Amgen Inc. Apelin polypeptides
MA41580A (fr) 2015-01-23 2017-11-29 Novartis Ag Conjugués d'acides gras de l'apeline synthétique présentant une demi-vie améliorée
CN110072531A (zh) 2016-10-19 2019-07-30 阿维夫公司 用于治疗心血管相关疾病的爱帕琳的新型聚乙二醇化的脂质体制剂
EP4168054A1 (en) * 2020-06-18 2023-04-26 Universite d'Aix Marseille Conjugated and labelled apelin, preparation and uses thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6420339B1 (en) * 1998-10-14 2002-07-16 Amgen Inc. Site-directed dual pegylation of proteins for improved bioactivity and biocompatibility
US20020102208A1 (en) 1999-03-01 2002-08-01 Paul Chinn Radiolabeling kit and binding assay
EP1613348B1 (en) * 2003-03-12 2010-06-23 The Arizona Board of Regents on Behalf of the University of Arizona Methods for modulating angiogenesis with apelin compositions
US7947280B2 (en) * 2003-05-22 2011-05-24 The Board Of Trustees Of The Leland Stanford Junior University Apelin and uses thereof
WO2007022123A2 (en) * 2005-08-11 2007-02-22 Amylin Pharmaceuticals, Inc. Hybrid polypeptides with selectable properties
WO2008051383A2 (en) * 2006-10-19 2008-05-02 Amgen Inc. Use of alcohol co-solvents to improve pegylation reaction yields
SI3045183T1 (sl) 2011-03-11 2018-11-30 Genzyme Corporation Pegiliran Apelin in njegove uporabe

Also Published As

Publication number Publication date
SI2683360T1 (sl) 2016-06-30
AU2017202919A1 (en) 2017-05-25
AU2012229336A1 (en) 2013-10-10
HRP20160547T1 (hr) 2016-06-17
WO2012125408A1 (en) 2012-09-20
CA2829693A1 (en) 2012-09-20
DK2683360T3 (da) 2016-05-30
HRP20181589T1 (hr) 2018-12-28
PL3045183T3 (pl) 2018-12-31
CA2829693C (en) 2020-04-21
EP2683360B1 (en) 2016-02-24
AU2012229336B2 (en) 2017-02-02
PT3045183T (pt) 2018-11-02
PL2683360T3 (pl) 2016-09-30
SI3045183T1 (sl) 2018-11-30
AU2017202919B2 (en) 2019-03-14
EP2683360A4 (en) 2014-09-03
EP3045183A1 (en) 2016-07-20
EP2683360A1 (en) 2014-01-15
CY1117654T1 (el) 2018-03-07
LT3045183T (lt) 2018-10-25
US20140142049A1 (en) 2014-05-22
WO2012125408A8 (en) 2018-01-25
HUE027579T2 (en) 2016-10-28
ES2690147T3 (es) 2018-11-19
EP3045183B1 (en) 2018-07-04
ES2573337T3 (es) 2016-06-07

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