DK2994152T3 - Konjugater til beskyttelse mod nefrotoxisk aktivstoffer - Google Patents

Konjugater til beskyttelse mod nefrotoxisk aktivstoffer Download PDF

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Publication number
DK2994152T3
DK2994152T3 DK14718515.1T DK14718515T DK2994152T3 DK 2994152 T3 DK2994152 T3 DK 2994152T3 DK 14718515 T DK14718515 T DK 14718515T DK 2994152 T3 DK2994152 T3 DK 2994152T3
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DK
Denmark
Prior art keywords
kidney
active compound
peptide
conjugate according
active compounds
Prior art date
Application number
DK14718515.1T
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English (en)
Inventor
Armin Kuebelbeck
Gregor Larbig
Stefan Arnold
Walter Mier
Uwe Haberkorn
Original Assignee
Merck Patent Gmbh
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
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Publication of DK2994152T3 publication Critical patent/DK2994152T3/da

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385—Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • 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
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Peptides Or Proteins (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)

Claims (9)

1. Konjugat indeholdende mindst et nyre-selektivt bærermolekyle og mindst én aktiv forbindelse der har en beskyttende virkning for nyren mod nefrotoxisk aktive forbindelser, kendetegnet ved at det mindst ene nyre-selektive bærermolekyle er et peptid der består af mere end 50% (baseret på antallet af aminosyreenheder) af sekvensafsnit valgt fra gruppen omfattende -(KKEEE)-, -(RREEE)-, -(KKEE)-, -(KKKEEE)- og -(KKKEE)- og hvor - peptidet består af mindst 80% (baseret på antallet af aminosyreenheder) af aminosyrerne K og E eller R og E, - og peptidet indeholder 3 til 5 sekvensafsnit som beskrevet ovenfor.
2. Konjugat ifølge krav 1, kendetegnet ved at peptidet står for et peptid valgt fra gruppen omfattende (RREEE)sR, (KKEE)sK, (KKKEE)sK, (KKKEEE)sK and (KKEEE)sK.
3. Konjugat ifølge krav 1 eller 2, kendetegnet ved at den mindst ene aktive forbindelse er valgt fra antioxidanter, apoptoseinhibitorer, aktive forbindelser med indflydelse på cellecyklus, aktive forbindelser der aktiverer reparationsmekanismen af cellerne, receptorinhibitorer og kombinationer deraf.
4. Konjugat ifølge krav 3, kendetegnet ved at den mindst ene aktive forbindelse er en antioxidant og/eller en apoptoseinhibitor.
5. Konjugat ifølge krav 4, kendetegnet ved at den aktive forbindelse er valgt fra liponsyre, resveratrol, kaffeinsyre, luteolin, quercetin, rutin, cyanidin, xanthohumol, ascorbinsyre, nikotinsyre, amifostin, alliin, thioler, tocopheroler, carotinoider, butylhydroxytoluen (BHT), pifithrin-μ, pifithrin-α, MDL 28170 og/eller NS3694.
6. Fremgangsmåde til fremstillingen af et konjugat ifølge ét eller flere af kravene 1 til 5, kendetegnet ved at en eventuelt aktiveret aktiv forbindelse der har en beskyttende virkning på nyren mod nefrotoxisk aktive forbindelser er konjugeret på bærermolekylet.
7. Konjugat ifølge ét eller flere af kravene 1 til 5 til anvendelse som medikament.
8. Konjugat ifølge ét eller flere af kravene 1 til 5 til anvendelse til beskyttelse af nyren mod nefrotoxisk aktive forbindelser.
9. Medikament omfattende mindst ét konjugat ifølge ét eller flere af kravene 1 til 5.
DK14718515.1T 2013-05-07 2014-04-16 Konjugater til beskyttelse mod nefrotoxisk aktivstoffer DK2994152T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13002431 2013-05-07
PCT/EP2014/001025 WO2014180533A2 (de) 2013-05-07 2014-04-16 Konjugate zum schutz vor nephrotoxischen wirkstoffen

Publications (1)

Publication Number Publication Date
DK2994152T3 true DK2994152T3 (da) 2018-11-26

Family

ID=48325357

Family Applications (1)

Application Number Title Priority Date Filing Date
DK14718515.1T DK2994152T3 (da) 2013-05-07 2014-04-16 Konjugater til beskyttelse mod nefrotoxisk aktivstoffer

Country Status (12)

Country Link
US (2) US9808535B2 (da)
EP (1) EP2994152B1 (da)
JP (1) JP6510493B2 (da)
CN (1) CN105188729B (da)
CA (1) CA2911478C (da)
DK (1) DK2994152T3 (da)
ES (1) ES2697250T3 (da)
HR (1) HRP20181883T1 (da)
HU (1) HUE039949T2 (da)
LT (1) LT2994152T (da)
SI (1) SI2994152T1 (da)
WO (1) WO2014180533A2 (da)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9808535B2 (en) * 2013-05-07 2017-11-07 Merck Patent Gmbh Conjugates for protection from nephrotoxic active substances
US10179095B2 (en) * 2017-06-07 2019-01-15 Dr. Raymond Laboratories Autophage activating resveratrol topical composition for skin improvement and treatment
JP2020526537A (ja) * 2017-07-14 2020-08-31 ユニバーシティ オブ マサチューセッツ 炎症を処置するための方法および組成物
CN115298198A (zh) 2020-01-21 2022-11-04 上海盟科药业股份有限公司 用于肾相关癌症靶向治疗的新型化合物和组合物
CN111567725A (zh) * 2020-04-30 2020-08-25 江苏师范大学 木犀草素作为抑制赭曲霉毒素a肾毒性的食物营养素的应用
JP2024529379A (ja) * 2021-07-21 2024-08-06 シャンハイ ミクウルク ファーマシューティカル シーオー．エルティーディー 腎臓疾患の標的療法のための化合物及び組成物
WO2024118760A1 (en) * 2022-11-29 2024-06-06 Cornell University Peptide-linked drug delivery system

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4645661A (en) * 1984-06-29 1987-02-24 St. Jude Children's Research Hospital Method for alleviating cisplatin-induced nephrotoxicity and dithiocarbamate compounds for effecting same
IL128828A0 (en) * 1996-09-09 2000-01-31 Zealand Pharmaceuticals As Peptide prodrugs containing an alpha-hydroxy acid linker
DE10006572A1 (de) * 2000-02-14 2001-08-23 Deutsches Krebsforsch Oligonucleotid-Konjugate
NZ566489A (en) 2005-08-26 2008-10-31 Action Pharma As Therapeutically active alpha-MSH analogues
DE102007004424A1 (de) * 2007-01-23 2008-07-24 Bayer Schering Pharma Aktiengesellschaft Eisenoxid-bindende Peptide
EP2277547A1 (de) 2009-07-20 2011-01-26 Merck Patent GmbH Epsilon-Polylysin-Konjugate und deren Verwendung
WO2014180534A1 (de) * 2013-05-07 2014-11-13 Merck Patent Gmbh Peptide und peptid-wirkstoff-konjugate für renales targeting
US9808535B2 (en) * 2013-05-07 2017-11-07 Merck Patent Gmbh Conjugates for protection from nephrotoxic active substances

Also Published As

Publication number Publication date
ES2697250T3 (es) 2019-01-22
CN105188729B (zh) 2021-11-09
CN105188729A (zh) 2015-12-23
US10413614B2 (en) 2019-09-17
US20180015173A1 (en) 2018-01-18
CA2911478A1 (en) 2014-11-13
US20160114054A1 (en) 2016-04-28
CA2911478C (en) 2023-06-13
WO2014180533A2 (de) 2014-11-13
SI2994152T1 (sl) 2018-12-31
EP2994152A2 (de) 2016-03-16
US9808535B2 (en) 2017-11-07
WO2014180533A3 (de) 2015-01-22
EP2994152B1 (de) 2018-08-15
HRP20181883T1 (hr) 2019-01-11
LT2994152T (lt) 2018-11-26
JP6510493B2 (ja) 2019-05-08
HUE039949T2 (hu) 2019-02-28
JP2016523825A (ja) 2016-08-12

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