AU2014306021B2 - Polyconjugates for delivery of RNAi triggers to tumor cells in vivo - Google Patents

Polyconjugates for delivery of RNAi triggers to tumor cells in vivo Download PDF

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Publication number
AU2014306021B2
AU2014306021B2 AU2014306021A AU2014306021A AU2014306021B2 AU 2014306021 B2 AU2014306021 B2 AU 2014306021B2 AU 2014306021 A AU2014306021 A AU 2014306021A AU 2014306021 A AU2014306021 A AU 2014306021A AU 2014306021 B2 AU2014306021 B2 AU 2014306021B2
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polymer
mmol
rgd
peg
fmoc
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AU2014306021A
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AU2014306021A2 (en
AU2014306021A1 (en
Inventor
Aaron M. Almeida
Andrei V. Blokhin
Jeffrey C. Carlson
Weijun CHENG
David B. Rozema
So Wong
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Arrowhead Pharmaceuticals Inc
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Arrowhead Pharmaceuticals Inc
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Publication of AU2014306021A2 publication Critical patent/AU2014306021A2/en
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    • C—CHEMISTRY; METALLURGY
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    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C07K5/0817—Tripeptides with the first amino acid being basic the first amino acid being Arg
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/14—Type of nucleic acid interfering nucleic acids [NA]
    • C—CHEMISTRY; METALLURGY
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/322—2'-R Modification
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/35—Nature of the modification
    • C12N2310/351—Conjugate
    • C12N2310/3513—Protein; Peptide
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/35—Nature of the modification
    • C12N2310/353—Nature of the modification linked to the nucleic acid via an atom other than carbon
    • C12N2310/3535—Nitrogen
    • 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
    • C12N2320/00—Applications; Uses
    • C12N2320/30—Special therapeutic applications
    • C12N2320/32—Special delivery means, e.g. tissue-specific

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • Plant Pathology (AREA)
  • Physics & Mathematics (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
AU2014306021A 2013-08-07 2014-08-06 Polyconjugates for delivery of RNAi triggers to tumor cells in vivo Ceased AU2014306021B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361863056P 2013-08-07 2013-08-07
US61/863,056 2013-08-07
US14/452,626 2014-08-06
PCT/US2014/049851 WO2015021092A1 (en) 2013-08-07 2014-08-06 Polyconjugates for delivery of rnai triggers to tumor cells in vivo
US14/452,626 US9487556B2 (en) 2013-08-07 2014-08-06 Polyconjugates for delivery of RNAi triggers to tumor cells in vivo

Publications (3)

Publication Number Publication Date
AU2014306021A1 AU2014306021A1 (en) 2016-01-28
AU2014306021A2 AU2014306021A2 (en) 2016-11-24
AU2014306021B2 true AU2014306021B2 (en) 2018-12-13

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ID=52449177

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2014306021A Ceased AU2014306021B2 (en) 2013-08-07 2014-08-06 Polyconjugates for delivery of RNAi triggers to tumor cells in vivo

Country Status (13)

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US (3) US9487556B2 (OSRAM)
EP (1) EP3030244B1 (OSRAM)
JP (1) JP6433001B2 (OSRAM)
KR (1) KR20160035081A (OSRAM)
CN (1) CN105451743B (OSRAM)
AU (1) AU2014306021B2 (OSRAM)
CA (1) CA2919088A1 (OSRAM)
EA (1) EA201690051A1 (OSRAM)
IL (1) IL243941B (OSRAM)
MX (1) MX2016001006A (OSRAM)
SG (1) SG11201600379TA (OSRAM)
TW (1) TWI685347B (OSRAM)
WO (1) WO2015021092A1 (OSRAM)

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SG11201600379TA (en) * 2013-08-07 2016-02-26 Arrowhead Res Corp Polyconjugates for delivery of rnai triggers to tumor cells in vivo
EP3271482A4 (en) 2015-03-17 2019-02-13 Arrowhead Pharmaceuticals, Inc. COMPOSITIONS AND METHODS FOR INHIBITING THE GENE EXPRESSION OF FACTOR XII
CN107635550B (zh) * 2015-03-17 2021-12-24 箭头药业股份有限公司 改良的含二硫化物的炔烃交联剂
SG11201708602XA (en) 2015-05-29 2017-12-28 Arrowhead Pharmaceuticals Inc Biologically cleavable tetrapeptide linking agents
BR112017025698A2 (pt) 2015-05-29 2018-08-14 Arrowhead Pharmaceuticals Inc composições e métodos para inibir a expressão do gene de hif2alfa
EP3252082A1 (en) * 2016-05-31 2017-12-06 Galderma S.A. Method for deacetylation of biopolymers
SI3397651T1 (sl) 2015-12-29 2020-11-30 Galderma S.A. Oglikovodično zamreževalo
PT3623390T (pt) * 2016-05-31 2023-10-27 Galderma Sa Reticulador de hidrato de carbono
US11629122B2 (en) 2017-05-24 2023-04-18 The Board Of Regents Of The University Of Texas System Linkers for antibody drug conjugates
EP3784269B1 (en) 2018-04-27 2024-06-05 Arrowhead Pharmaceuticals, Inc. Integrin targeting ligands and uses thereof
MX2021008261A (es) 2019-01-09 2021-08-16 Arrowhead Pharmaceuticals Inc Agentes de rnai para inhibir la expresion de hif-2 a (epas1), composiciones de estos y metodos de uso.
CN110240551B (zh) * 2019-06-25 2022-02-11 成都郑源生化科技有限公司 Fmoc-β-Ala-Gly-OH的制备方法
TWI894184B (zh) 2019-12-02 2025-08-21 瑞士商葛德瑪控股公司 高分子量美容組合物
CN113004515B (zh) * 2021-03-02 2023-02-24 厦门大学附属中山医院 一种仿透明质酸聚氨基酸衍生物、其制备方法及其应用

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US20120165393A1 (en) * 2010-12-17 2012-06-28 Arrowhead Madison Inc. Peptide-Based In Vivo siRNA Delivery System
US20120172412A1 (en) * 2010-12-29 2012-07-05 Arrowhead Madison Inc. In Vivo Polynucleotide Delivery Conjugates Having Enzyme Sensitive Linkages

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US20120165393A1 (en) * 2010-12-17 2012-06-28 Arrowhead Madison Inc. Peptide-Based In Vivo siRNA Delivery System
US20120172412A1 (en) * 2010-12-29 2012-07-05 Arrowhead Madison Inc. In Vivo Polynucleotide Delivery Conjugates Having Enzyme Sensitive Linkages

Also Published As

Publication number Publication date
WO2015021092A1 (en) 2015-02-12
EA201690051A1 (ru) 2016-06-30
MX2016001006A (es) 2016-04-19
CN105451743A (zh) 2016-03-30
US9487556B2 (en) 2016-11-08
HK1220397A1 (zh) 2017-05-05
IL243941B (en) 2019-06-30
EP3030244A4 (en) 2017-06-28
EP3030244B1 (en) 2021-04-21
IL243941A0 (en) 2016-04-21
CN105451743B (zh) 2019-11-19
JP2016535058A (ja) 2016-11-10
SG11201600379TA (en) 2016-02-26
US20170022497A1 (en) 2017-01-26
US20190062748A1 (en) 2019-02-28
US20150045573A1 (en) 2015-02-12
EP3030244A1 (en) 2016-06-15
AU2014306021A2 (en) 2016-11-24
TWI685347B (zh) 2020-02-21
CA2919088A1 (en) 2015-02-12
AU2014306021A1 (en) 2016-01-28
KR20160035081A (ko) 2016-03-30
TW201601742A (zh) 2016-01-16
JP6433001B2 (ja) 2018-12-05

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