HRP20160547T1 - Pegilirani apelin i njegova upotreba - Google Patents

Pegilirani apelin i njegova upotreba Download PDF

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Publication number
HRP20160547T1
HRP20160547T1 HRP20160547TT HRP20160547T HRP20160547T1 HR P20160547 T1 HRP20160547 T1 HR P20160547T1 HR P20160547T T HRP20160547T T HR P20160547TT HR P20160547 T HRP20160547 T HR P20160547T HR P20160547 T1 HRP20160547 T1 HR P20160547T1
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HR
Croatia
Prior art keywords
apelin
pegylated
molecule
amino acid
peg
Prior art date
Application number
HRP20160547TT
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English (en)
Inventor
Zhiqiang JIA
Lihui HOU
Clark Q. Pan
Geoffrey Y. Akita
Original Assignee
Genzyme Corporation
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 Corporation filed Critical Genzyme Corporation
Publication of HRP20160547T1 publication Critical patent/HRP20160547T1/hr

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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 (14)

1. Pegilirana molekula Apelin 36 koja sadrži jednu ili više molekula polietilen glikola (PEG) funkcionalno vezanu na najmanje jedan aminokiselinski ostatak na N-terminalnom kraju Apelina 36.
2. Molekula prema zahtjevu 1, naznačena time da je navedeni pegilirani Apelin 36 sposoban iskazivati produljeni cirkulirajući vijek ili prošireni inotropni učinak, u odnosu na ne-pegilirani Apelin 36.
3. Molekula prema zahtjevu 1, naznačena time da navedeni pegilirani Apelin 36 je mono-pegilirani ili di-pegilirani Apelin 36.
4. Molekula prema zahtjevu 1, naznačena time da su navedena jedna ili više PEG molekula kovalentno vezane na navedeni najmanje jedan aminokiselinski ostatak, bilo izravno ili preko linkera.
5. Molekula prema zahtjevu 1, naznačena time da svaka PEG molekula ima molekularnu težinu u rasponu od oko 5,000 do oko 50,000 daltona.
6. Molekula prema zahtjevu 1, naznačena time da navedeni pegilirani Apelin 36 sadrži monomerni Apelin 36.
7. Molekula prema zahtjevu 1, naznačena time da navedeni pegilirani Apelin 36 sadrži oligomerni Apelin 36, pri čemu su jedan ili više monomera funkcionalno vezani jedan za drugoga.
8. Molekula prema zahtjevu 1, naznačena time da Apelin 36 sadrži sekvencu aminokiseline od aminokiselinskih ostataka 42-77 iz SEQ ID NO: 1.
9. Molekula prema zahtjevu 8, naznačena time da navedena sekvenca aminokiseline je kodirana sa sekvencom nukleinske kiseline 123-234 bp iz SEQ ID NO: 2.
10. Postupak za proizvodnju molekula prema zahtjevu 1, naznačen time da sadrži korak: reakcije Apelina 36 s aktiviranim PEG-aldehidnim linkerom u prisutnosti redukcijskog sredstva da se dobije navedeni pegilirani Apelin 36 pod uvjetima u kojima je linker kovalentno vezan na ostatak Leucina na N-terminalnom kraju Apelina 36.
11. Postupak prema zahtjevu 10, naznačen time da redukcijsko sredstvo je cijanoborohidrid i reakcijski korak se izvodi kod pH od 5.0 do 7.5.
12. Farmaceutski pripravak koji sadrži terapijski učinkovitu količinu pegiliranog Apelina 36 koji sadrži jednu ili više molekula polietilen glikola (PEG) funkcionalno vezane na najmanje jedan aminokiselinski ostatak na N-terminalnom kraju od Apelina 36, naznačen time da navedeni najmanje jedan aminokiselinski ostatak je Leucin.
13. Terapijski učinkovita količina pegilirane molekule Apelina 36 prema zahtjevu 1 naznačena time da je za upotrebu u liječenju bolesti ili poremećaja povezanih sa Apelinom, pri čemu bolest ili poremećaj je kardiovaskularna bolest, ishemijsko-reperfuzijska ozljeda, infarkt miokarda, akutno dekompenzacijsko zatajenje srca, kronično zatajenje srca, kardiomiopatija, endokrini poremećaj, metabolički poremećaj ili plućna hipertenzija.
14. Pegilirana molekula Apelin 36 za uporabu prema zahtjevu 13, naznačena time da navedeni najmanje jedan aminokiselinski ostatak na N-terminalnom kraju od Apelina 36 je Leucin.
HRP20160547TT 2011-03-11 2016-05-23 Pegilirani apelin i njegova upotreba HRP20160547T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161451623P 2011-03-11 2011-03-11
PCT/US2012/028298 WO2012125408A1 (en) 2011-03-11 2012-03-08 Pegylated apelin and uses thereof
EP12757055.4A EP2683360B1 (en) 2011-03-11 2012-03-08 Pegylated apelin and uses thereof

Publications (1)

Publication Number Publication Date
HRP20160547T1 true HRP20160547T1 (hr) 2016-06-17

Family

ID=46831054

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20160547TT HRP20160547T1 (hr) 2011-03-11 2016-05-23 Pegilirani apelin i njegova upotreba
HRP20181589TT HRP20181589T1 (hr) 2011-03-11 2018-10-03 Pegilirani apelin i njegova upotreba

Family Applications After (1)

Application Number Title Priority Date Filing Date
HRP20181589TT HRP20181589T1 (hr) 2011-03-11 2018-10-03 Pegilirani apelin i njegova upotreba

Country Status (14)

Country Link
US (1) US20140142049A1 (hr)
EP (2) EP3045183B1 (hr)
AU (2) AU2012229336B2 (hr)
CA (1) CA2829693C (hr)
CY (1) CY1117654T1 (hr)
DK (2) DK3045183T3 (hr)
ES (2) ES2573337T3 (hr)
HR (2) HRP20160547T1 (hr)
HU (1) HUE027579T2 (hr)
LT (1) LT3045183T (hr)
PL (2) PL2683360T3 (hr)
PT (1) PT3045183T (hr)
SI (2) SI3045183T1 (hr)
WO (1) WO2012125408A1 (hr)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2683360T3 (pl) 2011-03-11 2016-09-30 Pegylowana apelina i jej zastosowania
WO2014099984A1 (en) * 2012-12-20 2014-06-26 Amgen Inc. Apj receptor agonists and uses thereof
JP6525951B2 (ja) 2013-03-14 2019-06-05 リジェネロン・ファーマシューティカルズ・インコーポレイテッドRegeneron Pharmaceuticals, Inc. アペリン融合タンパク質およびその使用
MX2016001021A (es) 2013-07-25 2016-08-03 Novartis Ag Bioconjugados de polipeptidos de apelina sinteticos.
US9683018B2 (en) * 2013-07-25 2017-06-20 Novartis Ag Disulfide cyclic polypeptides for the treatment of heart failure
KR20160031551A (ko) * 2013-07-25 2016-03-22 노파르티스 아게 심부전의 치료를 위한 시클릭 폴리펩티드
EP3024846A1 (en) * 2013-07-25 2016-06-01 Novartis AG Cyclic apelin derivatives for the treatment of heart failure
BR112016011401A2 (pt) 2013-11-20 2017-09-26 Regeneron Pharma moduladores de aplnr e utilizações dos mesmos
AU2015237357B2 (en) 2014-03-25 2019-04-18 Lanthiopep B.V. Cyclic apelin analogs
US10941182B2 (en) * 2014-06-10 2021-03-09 Amgen Inc. Apelin polypeptides
SG11201704758XA (en) 2015-01-23 2017-08-30 Novartis Ag Synthetic apelin fatty acid conjugates with improved half-life
CA3040517A1 (en) 2016-10-19 2018-04-26 Avive, Inc. Novel pegylated liposomal formulations of apelin for treatment of cardiovascular-related diseases
WO2021255282A1 (en) * 2020-06-18 2021-12-23 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
WO2004081198A2 (en) * 2003-03-12 2004-09-23 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
PL2683360T3 (pl) 2011-03-11 2016-09-30 Pegylowana apelina i jej zastosowania

Also Published As

Publication number Publication date
DK3045183T3 (en) 2018-10-22
WO2012125408A1 (en) 2012-09-20
US20140142049A1 (en) 2014-05-22
CY1117654T1 (el) 2018-03-07
EP2683360B1 (en) 2016-02-24
CA2829693A1 (en) 2012-09-20
AU2012229336A1 (en) 2013-10-10
PL3045183T3 (pl) 2018-12-31
AU2012229336B2 (en) 2017-02-02
HUE027579T2 (en) 2016-10-28
EP3045183B1 (en) 2018-07-04
WO2012125408A8 (en) 2018-01-25
EP3045183A1 (en) 2016-07-20
ES2573337T3 (es) 2016-06-07
HRP20181589T1 (hr) 2018-12-28
CA2829693C (en) 2020-04-21
AU2017202919B2 (en) 2019-03-14
EP2683360A4 (en) 2014-09-03
DK2683360T3 (en) 2016-05-30
LT3045183T (lt) 2018-10-25
SI2683360T1 (sl) 2016-06-30
SI3045183T1 (sl) 2018-11-30
EP2683360A1 (en) 2014-01-15
PL2683360T3 (pl) 2016-09-30
PT3045183T (pt) 2018-11-02
ES2690147T3 (es) 2018-11-19
AU2017202919A1 (en) 2017-05-25

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