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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AU2014306021A1 (en
AU2014306021A2 (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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    • 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
    • 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
    • C07K5/06043—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]
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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
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    • 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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • Wood Science & Technology (AREA)
  • Epidemiology (AREA)
  • General Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physics & Mathematics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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
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
US14/452,626 2014-08-06

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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Family Applications (1)

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

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CA2979703A1 (en) * 2015-03-17 2016-09-22 Arrowhead Pharmaceuticals, Inc. Compositions and methods for inhibiting gene expression of factor xii
CN107614002B (zh) 2015-05-29 2022-01-04 箭头药业股份有限公司 生物学可切割四肽连接剂
AR104754A1 (es) 2015-05-29 2017-08-09 Arrowhead Pharmaceuticals Inc Agentes de unión de tetrapéptido escindibles biológicamente
JOP20160211B1 (ar) 2015-10-01 2021-08-17 Arrowhead Pharmaceuticals Inc تراكيب وأساليب لتثبيط تعبير جيني للـ lpa
EP3397651B1 (en) 2015-12-29 2020-05-06 Galderma S.A. Carbohydrate crosslinker
EP3252082A1 (en) * 2016-05-31 2017-12-06 Galderma S.A. Method for deacetylation of biopolymers
PT3623390T (pt) * 2016-05-31 2023-10-27 Galderma Sa Reticulador de hidrato de carbono
WO2018218004A1 (en) 2017-05-24 2018-11-29 The Board Of Regents Of The University Of Texas System Linkers for antibody drug conjugates
SG11202009734VA (en) * 2018-04-27 2020-11-27 Arrowhead Pharmaceuticals Inc Integrin targeting ligands and uses thereof
SG11202105577TA (en) 2019-01-09 2021-06-29 Arrowhead Pharmaceuticals Inc Rnai agents for inhibiting expression of hif-2 alpha (epas1), compositions thereof, and methods of use
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
CA3160575A1 (en) 2019-12-02 2021-06-10 Johan Olsson High molecular weight esthetic compositions
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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Also Published As

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

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