WO2003004603A3 - Methods of modulating pharmacokinetics of oligonucleotides - Google Patents

Methods of modulating pharmacokinetics of oligonucleotides Download PDF

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Publication number
WO2003004603A3
WO2003004603A3 PCT/US2002/020940 US0220940W WO03004603A3 WO 2003004603 A3 WO2003004603 A3 WO 2003004603A3 US 0220940 W US0220940 W US 0220940W WO 03004603 A3 WO03004603 A3 WO 03004603A3
Authority
WO
WIPO (PCT)
Prior art keywords
oligonucleotides
methods
moe
modified oligonucleotides
modulating pharmacokinetics
Prior art date
Application number
PCT/US2002/020940
Other languages
French (fr)
Other versions
WO2003004603A2 (en
Inventor
Thazha P Prakash
Muthiah Manoharan
Original Assignee
Isis Pharmaceuticals Inc
Thazha P Prakash
Muthiah Manoharan
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
Priority claimed from US10/058,740 external-priority patent/US6921812B1/en
Application filed by Isis Pharmaceuticals Inc, Thazha P Prakash, Muthiah Manoharan filed Critical Isis Pharmaceuticals Inc
Priority to EP02742381A priority Critical patent/EP1409731A2/en
Priority to CA002452310A priority patent/CA2452310A1/en
Publication of WO2003004603A2 publication Critical patent/WO2003004603A2/en
Publication of WO2003004603A3 publication Critical patent/WO2003004603A3/en

Links

Classifications

    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • 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
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/321—2'-O-R Modification

Landscapes

  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Engineering & Computer Science (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

2'-O-(2-Methylthioethyl), has been incorporated into oligonucleotides and evaluated for antisense properties in comparison with the known 2'-O-(2-methoxyethyl)2'-O-MOE modification. The 2'-O-MOE modified oligonucleotides exhibit improved binding to human serum albumin compared with the 2'-O-MOE modified oligonucleotides and maintain high binding affinity to target RNA.
PCT/US2002/020940 2001-07-03 2002-07-01 Methods of modulating pharmacokinetics of oligonucleotides WO2003004603A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP02742381A EP1409731A2 (en) 2001-07-03 2002-07-01 Methods of modulating pharmacokinetics of oligonucleotides
CA002452310A CA2452310A1 (en) 2001-07-03 2002-07-01 Methods of modulating pharmacokinetics of oligonucleotides

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US30268301P 2001-07-03 2001-07-03
US60/302,683 2001-07-03
US10/058,740 US6921812B1 (en) 2001-07-03 2002-01-28 Methods of modulating pharmacokinetics of oligonucleotides
US10/058,740 2002-01-28

Publications (2)

Publication Number Publication Date
WO2003004603A2 WO2003004603A2 (en) 2003-01-16
WO2003004603A3 true WO2003004603A3 (en) 2003-12-04

Family

ID=26737983

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/020940 WO2003004603A2 (en) 2001-07-03 2002-07-01 Methods of modulating pharmacokinetics of oligonucleotides

Country Status (3)

Country Link
EP (1) EP1409731A2 (en)
CA (1) CA2452310A1 (en)
WO (1) WO2003004603A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7947817B2 (en) * 2003-06-30 2011-05-24 Roche Molecular Systems, Inc. Synthesis and compositions of 2'-terminator nucleotides
FR2860143B1 (en) * 2003-09-26 2008-06-27 Oreal COSMETIC COMPOSITION COMPRISING A SEQUENCE POLYMER AND A NON-VOLATILE SILICONE OIL
US7928207B2 (en) * 2004-06-28 2011-04-19 Roche Molecular Systems, Inc Synthesis and compositions of nucleic acids comprising 2′-terminator nucleotides
US7745125B2 (en) 2004-06-28 2010-06-29 Roche Molecular Systems, Inc. 2′-terminator related pyrophosphorolysis activated polymerization
TW201422633A (en) 2012-08-31 2014-06-16 Kyowa Hakko Kirin Co Ltd Oligonucleotide
JP6586078B2 (en) * 2014-03-03 2019-10-02 協和キリン株式会社 Oligonucleotides having unnatural nucleotides at the 5 'end
US11518780B2 (en) 2019-07-31 2022-12-06 Shiyue Fang Sensitive oligonucleotide synthesis using sulfur-based functions as protecting groups and linkers

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6147200A (en) * 1999-08-19 2000-11-14 Isis Pharmaceuticals, Inc. 2'-O-acetamido modified monomers and oligomers
US6239272B1 (en) * 1995-04-20 2001-05-29 Ribozyme Pharmaceutical 2'-O-alkylthioalkyl and 2'-c-alkylthioalkyl-containing nucleic acids

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6239272B1 (en) * 1995-04-20 2001-05-29 Ribozyme Pharmaceutical 2'-O-alkylthioalkyl and 2'-c-alkylthioalkyl-containing nucleic acids
US6147200A (en) * 1999-08-19 2000-11-14 Isis Pharmaceuticals, Inc. 2'-O-acetamido modified monomers and oligomers

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PRAKASH T. ET AL.: "2'-O-(2-(methylthio)ethyl)-modified oligonucleotide: An analogue of 2'-O-(2-(methoxy)ethyl)-modified oligonucleotide with improved protein binding properties and high binding affinity to target RNA", BIOCHEMISTRY, vol. 41, September 2002 (2002-09-01), pages 11642 - 11648, XP002962878 *

Also Published As

Publication number Publication date
WO2003004603A2 (en) 2003-01-16
CA2452310A1 (en) 2003-01-16
EP1409731A2 (en) 2004-04-21

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