FI930220A - OLIGONUCLEOTIDS ANALOGGER, DERAS FRAMSTAELLNING OCH ANVAENDNING - Google Patents

OLIGONUCLEOTIDS ANALOGGER, DERAS FRAMSTAELLNING OCH ANVAENDNING Download PDF

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Publication number
FI930220A
FI930220A FI930220A FI930220A FI930220A FI 930220 A FI930220 A FI 930220A FI 930220 A FI930220 A FI 930220A FI 930220 A FI930220 A FI 930220A FI 930220 A FI930220 A FI 930220A
Authority
FI
Finland
Prior art keywords
aryl
alkyl
analogger
oligonucleotids
seh
Prior art date
Application number
FI930220A
Other languages
Finnish (fi)
Other versions
FI115214B (en
FI930220A0 (en
Inventor
Eugen Uhlmann
Anuschirwan Peyman
Gerard O'malley
Matthias Helsberg
Irvin Winkler
Original Assignee
Hoechst Ag
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Publication date
Application filed by Hoechst Ag filed Critical Hoechst Ag
Publication of FI930220A0 publication Critical patent/FI930220A0/en
Publication of FI930220A publication Critical patent/FI930220A/en
Application granted granted Critical
Publication of FI115214B publication Critical patent/FI115214B/en

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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (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.
FI930220A 1992-01-22 1993-01-20 Process for Preparation of Oligonucleotide Analogs and Their Use FI115214B (en)

Applications Claiming Priority (2)

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

Publications (3)

Publication Number Publication Date
FI930220A0 FI930220A0 (en) 1993-01-20
FI930220A true FI930220A (en) 1993-07-23
FI115214B FI115214B (en) 2005-03-31

Family

ID=6450030

Family Applications (1)

Application Number Title Priority Date Filing Date
FI930220A FI115214B (en) 1992-01-22 1993-01-20 Process for Preparation of Oligonucleotide Analogs and Their 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)

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DE59306170D1 (en) * 1992-09-24 1997-05-22 Hoechst Ag Oligoribonucleotide and ribozyme analogs with terminal 3'-3 'and 5'-5' linkages
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
JPH08507752A (en) * 1993-01-08 1996-08-20 ハイブライドン インコーポレイテッド Synthesis of dimer block and oligonucleotide ligation method using dimer block
EP0677056B1 (en) * 1993-01-25 1996-05-22 HYBRIDON, Inc. Oligonucleotide alkylphosphonates and alkylphosphonothioates
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
US5726297A (en) * 1994-03-18 1998-03-10 Lynx Therapeutics, Inc. Oligodeoxyribonucleotide N3' P5' phosphoramidates
US5599922A (en) * 1994-03-18 1997-02-04 Lynx Therapeutics, Inc. Oligonucleotide N3'-P5' phosphoramidates: hybridization and nuclease resistance properties
JP3482209B2 (en) * 1994-03-18 2003-12-22 ジェロン・コーポレーション Oligonucleotides N3 '→ P5' phosphoramidate: synthesis and compounds; hybridization and nuclease resistance properties
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
US6150510A (en) 1995-11-06 2000-11-21 Aventis Pharma Deutschland Gmbh Modified oligonucleotides, their preparation and their use
DE4438918A1 (en) * 1994-11-04 1996-05-09 Hoechst Ag Modified oligonucleotides, their preparation and their use
DE19502912A1 (en) * 1995-01-31 1996-08-01 Hoechst Ag G-Cap Stabilized Oligonucleotides
ES2165446T3 (en) * 1995-03-13 2002-03-16 Aventis Pharma Gmbh PHOSPHONOMONOSTER-NUCLEIC ACIDS, PROCEDURE FOR PREPARATION AND USE.
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
PT808898E (en) * 1996-05-24 2004-10-29 Aventis Pharma Gmbh REAGENT AND METHOD FOR INHIBITING N-RAS EXPRESSION
DE19627898A1 (en) * 1996-07-11 1998-01-15 Hoechst Ag Solid phase synthesis of oligonucleotides
KR100518108B1 (en) * 1997-05-05 2005-10-04 아벤티스 파마 도이칠란트 게엠베하 Modified antisense nucleotides complementary to a section of the human Ha-ras gene
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
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
DE19935303A1 (en) 1999-07-28 2001-02-08 Aventis Pharma Gmbh Oligonucleotides to inhibit the expression of human eg5
DE10133915A1 (en) 2001-07-12 2003-02-06 Aventis Pharma Gmbh New oligoribonucleotide derivatives for targeted inhibition of gene expression
KR101059315B1 (en) 2003-08-28 2011-08-24 노파르티스 아게 Interfering rna duplex having blunt-ends and 3'-modifications
GB0608838D0 (en) 2006-05-04 2006-06-14 Novartis Ag Organic compounds
CN104975020B (en) 2008-02-11 2020-01-17 菲奥医药公司 Modified RNAi polynucleotides and uses thereof
WO2010008582A2 (en) 2008-07-18 2010-01-21 Rxi Pharmaceuticals Corporation Phagocytic cell drug delivery system
JP6209309B2 (en) 2008-09-22 2017-10-04 アールエックスアイ ファーマシューティカルズ コーポレーション Reduced size RNAi compound for self delivery
US9074211B2 (en) 2008-11-19 2015-07-07 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
US9340786B2 (en) 2010-03-24 2016-05-17 Rxi Pharmaceuticals Corporation RNA interference in dermal and fibrotic indications
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US10934550B2 (en) 2013-12-02 2021-03-02 Phio Pharmaceuticals Corp. 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
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CN107073294A (en) 2014-09-05 2017-08-18 阿克赛医药公司 Use the method for targeting TYR or MMP1 exonuclease treatment aging and skin disorder
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WO2017007825A1 (en) 2015-07-06 2017-01-12 Rxi Pharmaceuticals Corporation Methods for treating neurological disorders using a synergistic small molecule and nucleic acids therapeutic approach
CA3002744A1 (en) 2015-10-19 2017-04-27 Rxi Pharmaceuticals Corporation Reduced size self-delivering nucleic acid compounds targeting long non-coding rna
JP7353301B2 (en) 2018-05-07 2023-09-29 アルニラム ファーマスーティカルズ インコーポレイテッド Extrahepatic delivery

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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
ATE190981T1 (en) * 1989-10-24 2000-04-15 Isis Pharmaceuticals Inc 2'-MODIFIED NUCLEOTIDES
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
AU3191093A (en) 1993-07-29
ZA93422B (en) 1993-09-16
DE59310285D1 (en) 2002-06-27
EP0552766A2 (en) 1993-07-28
AU661365B2 (en) 1995-07-20
EP0552766A3 (en) 1994-09-07
JPH05310779A (en) 1993-11-22
PL297515A1 (en) 1993-09-06
NZ245720A (en) 1995-12-21
EP0552766B1 (en) 2002-05-22
PT552766E (en) 2002-10-31
JP3717081B2 (en) 2005-11-16
CA2087818C (en) 2007-07-10
FI115214B (en) 2005-03-31
HU227794B1 (en) 2012-03-28
ES2177532T3 (en) 2002-12-16
IL104461A0 (en) 1993-05-13
NO930199D0 (en) 1993-01-21
CA2087818A1 (en) 1993-07-23
IL104461A (en) 2001-05-20
KR930016437A (en) 1993-08-26
FI930220A0 (en) 1993-01-20
PL172257B1 (en) 1997-08-29
ATE217880T1 (en) 2002-06-15
DK0552766T3 (en) 2002-08-19
HU9300162D0 (en) 1993-04-28
HUT63173A (en) 1993-07-28
NO308215B1 (en) 2000-08-14
NO930199L (en) 1993-07-23

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