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DK0552766T3 - Oligonucleotide analogues, their preparation and use - Google Patents

Oligonucleotide analogues, their preparation and use

Info

Publication number
DK0552766T3
DK0552766T3 DK93100892T DK93100892T DK0552766T3 DK 0552766 T3 DK0552766 T3 DK 0552766T3 DK 93100892 T DK93100892 T DK 93100892T DK 93100892 T DK93100892 T DK 93100892T DK 0552766 T3 DK0552766 T3 DK 0552766T3
Authority
DK
Denmark
Prior art keywords
aryl
alkyl
preparation
seh
alkoxy
Prior art date
Application number
DK93100892T
Other languages
Danish (da)
Inventor
Irvin Dr Winkler
Eugen Dr Uhlmann
Anuschirwan Dr Peyman
Gerard Dr O'malley
Matthias Dr Helsberg
Original Assignee
Aventis Pharma 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 Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Application granted granted Critical
Publication of DK0552766T3 publication Critical patent/DK0552766T3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • 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
    • A61K31/7125—Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/11—Compounds covalently bound to a solid support

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Biotechnology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)

Abstract

The invention relates to compounds of the formula I <IMAGE> in which R<1> is H, alkyl, acyl, aryl or a phosphate residue; R<2> is H, OH, alkoxy, NH2 or halogen; B is a base customary in nucleotide chemistry; a is O or CH2; n is an integer from 1 to 100; W is O, S or Se; V is O, S or NH; Y is O, S, NH or CH2; Y' is O, S, NH or alkylene; X is OH or SH; U is OH, SH, SeH, alkyl, aryl or amine, and Z is OH, SH, SeH, an optionally substituted radical from the series comprising alkyl, aryl, heteroaryl, alkoxy or amino or a group which favours intracellular uptake or as labelling of a DNA probe or which on hybridisation interacts with the target nucleic acid, where if Z is OH, SH, CH3 or OC2H5, at least one of the groups X, Y, Y', V, W is not equal to OH or O, or R<1> is not equal to H; process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.
DK93100892T 1992-01-22 1993-01-21 Oligonucleotide analogues, their preparation and use DK0552766T3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE4201662 1992-01-22

Publications (1)

Publication Number Publication Date
DK0552766T3 true DK0552766T3 (en) 2002-08-19

Family

ID=6450030

Family Applications (1)

Application Number Title Priority Date Filing Date
DK93100892T DK0552766T3 (en) 1992-01-22 1993-01-21 Oligonucleotide analogues, their preparation and use

Country Status (17)

Country Link
EP (1) EP0552766B1 (en)
JP (1) JP3717081B2 (en)
KR (1) KR930016437A (en)
AT (1) ATE217880T1 (en)
AU (1) AU661365B2 (en)
CA (1) CA2087818C (en)
DE (1) DE59310285D1 (en)
DK (1) DK0552766T3 (en)
ES (1) ES2177532T3 (en)
FI (1) FI115214B (en)
HU (1) HU227794B1 (en)
IL (1) IL104461A (en)
NO (1) NO308215B1 (en)
NZ (1) NZ245720A (en)
PL (1) PL172257B1 (en)
PT (1) PT552766E (en)
ZA (1) ZA93422B (en)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5378825A (en) * 1990-07-27 1995-01-03 Isis Pharmaceuticals, Inc. Backbone modified oligonucleotide analogs
US5646261A (en) * 1992-01-22 1997-07-08 Hoechst Aktiengesellschaft 3'-derivatized oligonucleotide analogs with non-nucleotidic groupings, their preparation and use
ES2103408T3 (en) * 1992-09-24 1997-09-16 Hoechst Ag ANALOGS OF OLIGORRIBONUCLEOTIDES AND RIBOZYMES WITH TERMINAL JOINTS IN 3'-3 'OR 5'-5' RESPECTIVELY.
EP0602524A1 (en) * 1992-12-15 1994-06-22 Hoechst Aktiengesellschaft Chemiluminescence marked sequences and their use in sequence testing
US6087491A (en) 1993-01-08 2000-07-11 Hybridon, Inc. Extremely high purity oligonucleotides and methods of synthesizing them using dimer blocks
ES2100051T3 (en) * 1993-01-08 1997-06-01 Hybridon Inc SYNTHESIS OF DIMER BLOCKS AND THEIR USE IN THE ASSEMBLY OF OLIGONUCLEOTIDES.
ES2086997T3 (en) * 1993-01-25 1996-07-01 Hybridon Inc OLIGONUCLEOTIDE-ALKYLPHOSPHONATES AND -ALKYLPHOSPHONOTIOATES.
CA2114355A1 (en) * 1993-01-29 1994-07-30 Hidehiko Furukawa Modified oligodeoxyribonucleotides, their preparation and their therapeutic use
US5532130A (en) * 1993-07-20 1996-07-02 Dyad Pharmaceutical Corporation Methods and compositions for sequence-specific hybridization of RNA by 2'-5' oligonucleotides
DE4331670A1 (en) * 1993-09-17 1995-03-23 Hoechst Ag Antisense oligonucleotides against HSV-1 and the preparation thereof
DE4338704A1 (en) 1993-11-12 1995-05-18 Hoechst Ag Stabilized oligonucleotides and their use
DE4408528A1 (en) * 1994-03-14 1995-09-28 Hoechst Ag Peptide oligonucleotide derivatives, their preparation and use
US6919441B2 (en) 1994-03-14 2005-07-19 Aventis Pharma Deutschland Gmbh Polyamide-oligonucleotide derivatives, their preparation and use
CA2184375C (en) * 1994-03-18 2006-05-02 Sergei M. Gryaznov Oligonucleotide n3'-p5' phosphoramidates: synthesis and compounds; hybridization and nuclease resistance properties
US5599922A (en) 1994-03-18 1997-02-04 Lynx Therapeutics, Inc. Oligonucleotide N3'-P5' phosphoramidates: hybridization and nuclease resistance properties
US5726297A (en) * 1994-03-18 1998-03-10 Lynx Therapeutics, Inc. Oligodeoxyribonucleotide N3' P5' phosphoramidates
DE4415370A1 (en) * 1994-05-02 1995-11-09 Hoechst Ag Modified oligonucleotides, their preparation and their use
US5986076A (en) * 1994-05-11 1999-11-16 Trustees Of Boston University Photocleavable agents and conjugates for the detection and isolation of biomolecules
US5696248A (en) * 1994-06-15 1997-12-09 Hoechst Aktiengesellschaft 3'-modified oligonucleotide derivatives
DE4438918A1 (en) * 1994-11-04 1996-05-09 Hoechst Ag Modified oligonucleotides, their preparation and their use
US6150510A (en) * 1995-11-06 2000-11-21 Aventis Pharma Deutschland Gmbh Modified oligonucleotides, their preparation and their use
DE19502912A1 (en) 1995-01-31 1996-08-01 Hoechst Ag G-Cap Stabilized Oligonucleotides
DK0739898T3 (en) * 1995-03-13 2001-12-10 Aventis Pharma Gmbh Phosphonone monosternucleic acids, process for their preparation and use thereof
US6326487B1 (en) 1995-06-05 2001-12-04 Aventis Pharma Deutschland Gmbh 3 modified oligonucleotide derivatives
US5859233A (en) * 1996-02-21 1999-01-12 Lynx Therapeutics, Inc. Synthons for synthesis of oligonucleotide N3-P5 phosphoramidates
US5684143A (en) * 1996-02-21 1997-11-04 Lynx Therapeutics, Inc. Oligo-2'-fluoronucleotide N3'->P5' phosphoramidates
GB9606158D0 (en) * 1996-03-23 1996-05-29 Ciba Geigy Ag Chemical compounds
EP0808898B1 (en) * 1996-05-24 2004-05-19 Aventis Pharma Deutschland GmbH Reagent and method for inhibition of N-ras expression
DE19627898A1 (en) * 1996-07-11 1998-01-15 Hoechst Ag Solid phase synthesis of oligonucleotides
JP2002501505A (en) * 1997-05-05 2002-01-15 アベンティス、ファルマ、ドイチュラント、ゲゼルシャフト、ミット、ベシュレンクテル、ハフツング Modified antisense nucleotide complementary to human Ha-ras gene fragment
WO1999019474A1 (en) * 1997-10-14 1999-04-22 Sankyo Company, Limited Modified oligodeoxyribonucleotides having tggg sequence
EP1004661A1 (en) 1998-11-11 2000-05-31 DALLI-WERKE WÄSCHE- und KÖRPERPFLEGE GmbH & Co. KG High density granule, method for production thereof, and its use as disintegrant in tablets
DE19935303A1 (en) 1999-07-28 2001-02-08 Aventis Pharma Gmbh Oligonucleotides to inhibit the expression of human eg5
DE19935302A1 (en) 1999-07-28 2001-02-08 Aventis Pharma Gmbh Conjugates and processes for their preparation and their use for the transport of molecules across biological membranes
DE10133915A1 (en) 2001-07-12 2003-02-06 Aventis Pharma Gmbh New oligoribonucleotide derivatives for targeted inhibition of gene expression
RU2399671C2 (en) 2003-08-28 2010-09-20 Новартис Аг Rna duplex capable of interference and having blunt ends and 3'-modifications
GB0608838D0 (en) 2006-05-04 2006-06-14 Novartis Ag Organic compounds
WO2009102427A2 (en) 2008-02-11 2009-08-20 Rxi Pharmaceuticals Corp. Modified rnai polynucleotides and uses thereof
WO2010008582A2 (en) 2008-07-18 2010-01-21 Rxi Pharmaceuticals Corporation Phagocytic cell drug delivery system
CA3027780A1 (en) 2008-09-22 2010-03-25 Phio Pharmaceuticals Corp. Reduced size self-delivering rnai compounds
WO2010059226A2 (en) 2008-11-19 2010-05-27 Rxi Pharmaceuticals Corporation Inhibition of map4k4 through rnai
WO2010090762A1 (en) 2009-02-04 2010-08-12 Rxi Pharmaceuticals Corporation Rna duplexes with single stranded phosphorothioate nucleotide regions for additional functionality
CN103200945B (en) 2010-03-24 2016-07-06 雷克西制药公司 RNA interference in eye disease
KR102453078B1 (en) 2010-03-24 2022-10-11 피오 파마슈티칼스 코프. Rna interference in dermal and fibrotic indications
RU2615143C2 (en) 2010-03-24 2017-04-04 Адвирна Self-delivered rnai compounds of reduced size
CN106061488B (en) 2013-12-02 2021-04-09 菲奥医药公司 Immunotherapy of cancer
WO2015125845A1 (en) * 2014-02-20 2015-08-27 塩野義製薬株式会社 Phosphate site modification of nucleic acid containing nitrogen-containing non-aromatic heterocycle
WO2015168108A2 (en) 2014-04-28 2015-11-05 Rxi Pharmaceuticals Corporation Methods for treating cancer using nucleic targeting mdm2 or mycn
KR102689262B1 (en) 2014-09-05 2024-07-30 피오 파마슈티칼스 코프. Methods for treating aging and skin disorders using nucleic acids targeting tyr or mmp1
US10808247B2 (en) 2015-07-06 2020-10-20 Phio Pharmaceuticals Corp. Methods for treating neurological disorders using a synergistic small molecule and nucleic acids therapeutic approach
EP3319614B1 (en) 2015-07-06 2020-12-23 Phio Pharmaceuticals Corp. Nucleic acid molecules targeting superoxide dismutase 1 (sod1)
CA3002744A1 (en) 2015-10-19 2017-04-27 Rxi Pharmaceuticals Corporation Reduced size self-delivering nucleic acid compounds targeting long non-coding rna
CN112400018A (en) 2018-05-07 2021-02-23 阿尔尼拉姆医药品有限公司 Extrahepatic delivery

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3239888A1 (en) * 1982-10-28 1984-05-03 Hubert Prof. Dr. 2000 Hamburg Köster METHOD FOR PRODUCING OLIGONUCLEOSIDE PHOSPHONATES
US4739044A (en) * 1985-06-13 1988-04-19 Amgen Method for derivitization of polynucleotides
DE3751468T2 (en) * 1986-10-30 1996-02-29 Daicel Chem METHOD FOR PRODUCING OLIGONUCLEOTIDES AND COMPOUNDS FOR FORMING HIGH-MOLECULAR PROTECTION GROUPS.
US4816571A (en) * 1987-06-04 1989-03-28 Applied Biosystems, Inc. Chemical capping by phosphitylation during oligonucleotide synthesis
DK0497875T3 (en) * 1989-10-24 2000-07-03 Gilead Sciences Inc 2'-modified oligonucleotides
US5210015A (en) * 1990-08-06 1993-05-11 Hoffman-La Roche Inc. Homogeneous assay system using the nuclease activity of a nucleic acid polymerase
GB9021625D0 (en) * 1990-10-04 1990-11-21 Ici Plc Synthesis of oligonucleotides

Also Published As

Publication number Publication date
JPH05310779A (en) 1993-11-22
HU227794B1 (en) 2012-03-28
HUT63173A (en) 1993-07-28
EP0552766A2 (en) 1993-07-28
IL104461A (en) 2001-05-20
NZ245720A (en) 1995-12-21
ZA93422B (en) 1993-09-16
NO930199D0 (en) 1993-01-21
JP3717081B2 (en) 2005-11-16
NO930199L (en) 1993-07-23
AU3191093A (en) 1993-07-29
ES2177532T3 (en) 2002-12-16
FI115214B (en) 2005-03-31
DE59310285D1 (en) 2002-06-27
EP0552766B1 (en) 2002-05-22
FI930220A (en) 1993-07-23
IL104461A0 (en) 1993-05-13
EP0552766A3 (en) 1994-09-07
PL297515A1 (en) 1993-09-06
PL172257B1 (en) 1997-08-29
NO308215B1 (en) 2000-08-14
HU9300162D0 (en) 1993-04-28
PT552766E (en) 2002-10-31
ATE217880T1 (en) 2002-06-15
CA2087818C (en) 2007-07-10
FI930220A0 (en) 1993-01-20
CA2087818A1 (en) 1993-07-23
KR930016437A (en) 1993-08-26
AU661365B2 (en) 1995-07-20

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