AU3191093A - Oligonucleotide analogs, their preparation and use - Google Patents
Oligonucleotide analogs, their preparation and useInfo
- Publication number
- AU3191093A AU3191093A AU31910/93A AU3191093A AU3191093A AU 3191093 A AU3191093 A AU 3191093A AU 31910/93 A AU31910/93 A AU 31910/93A AU 3191093 A AU3191093 A AU 3191093A AU 3191093 A AU3191093 A AU 3191093A
- Authority
- AU
- Australia
- Prior art keywords
- aryl
- alkyl
- preparation
- seh
- alkoxy
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
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.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE4201662 | 1992-01-22 | ||
DE4201662 | 1992-01-22 |
Publications (2)
Publication Number | Publication Date |
---|---|
AU3191093A true AU3191093A (en) | 1993-07-29 |
AU661365B2 AU661365B2 (en) | 1995-07-20 |
Family
ID=6450030
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AU31910/93A Expired AU661365B2 (en) | 1992-01-22 | 1993-01-21 | Oligonucleotide analogs, 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) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU657191B2 (en) * | 1992-01-22 | 1995-03-02 | Hoechst Aktiengesellschaft | 3'-derivatized oligonucleotide analogs with nonnucleotidic groupings, their preparation and use |
AU666121B2 (en) * | 1991-05-21 | 1996-02-01 | Isis Pharmaceuticals, Inc. | Backbone modified oligonucleotide analogues |
AU704549B2 (en) * | 1994-03-18 | 1999-04-29 | Lynx Therapeutics, Inc. | Oligonucleotide N3'-P5' phosphoramidates: synthesis and compounds; hybridization and nuclease resistance properties |
Families Citing this family (49)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE151773T1 (en) | 1992-09-24 | 1997-05-15 | Hoechst Ag | OLIGORIBONUCLEOTIDE AND RIBOZYME ANALOGUES WITH TERMINAL 3'-3' AND 5'-5' LINKAGES, 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 |
DE69402177T2 (en) * | 1993-01-08 | 1997-06-26 | Hybridon Inc | SYNTHESIS OF DIMER BLOCKS AND THEIR USE IN THE COMPOSITION OF OLIGONUCLEOTIDES |
CA2154578A1 (en) * | 1993-01-25 | 1994-08-04 | Ekambar R. Kandimalla | 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 |
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 |
DE59607750D1 (en) * | 1995-03-13 | 2001-10-31 | Aventis Pharma Gmbh | Phosphonomonoester nucleic acids, process for their preparation and their use |
US6326487B1 (en) | 1995-06-05 | 2001-12-04 | Aventis Pharma Deutschland Gmbh | 3 modified oligonucleotide derivatives |
US5684143A (en) * | 1996-02-21 | 1997-11-04 | Lynx Therapeutics, Inc. | Oligo-2'-fluoronucleotide N3'->P5' phosphoramidates |
US5859233A (en) * | 1996-02-21 | 1999-01-12 | Lynx Therapeutics, Inc. | Synthons for synthesis of oligonucleotide 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 |
US6723706B2 (en) | 1997-05-05 | 2004-04-20 | Aventis Pharma Deutschland Gmbh | Modified antisense nucleotides complementary to a section of the human Ha-ras gene |
AU9460898A (en) * | 1997-10-14 | 1999-05-03 | 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 |
SG152279A1 (en) | 2003-08-28 | 2009-05-29 | Novartis Ag | Interfering rna duplex having blunt-ends and 3æ-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 |
US8815818B2 (en) | 2008-07-18 | 2014-08-26 | Rxi Pharmaceuticals Corporation | Phagocytic cell delivery of RNAI |
EP3336188B1 (en) | 2008-09-22 | 2020-05-06 | 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 |
WO2011119852A1 (en) | 2010-03-24 | 2011-09-29 | Rxi Pharmaceuticals Corporation | Reduced size self-delivering rnai compounds |
EP2550001B1 (en) | 2010-03-24 | 2019-05-22 | Phio Pharmaceuticals Corp. | Rna interference in ocular indications |
WO2011119887A1 (en) | 2010-03-24 | 2011-09-29 | Rxi Pharmaceuticals Corporation | Rna interference in dermal and fibrotic indications |
RU2744194C2 (en) | 2013-12-02 | 2021-03-03 | Фио Фармасьютикалс Корп | Cancer immunotherapy |
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 |
US11279934B2 (en) | 2014-04-28 | 2022-03-22 | Phio Pharmaceuticals Corp. | Methods for treating cancer using nucleic acids targeting MDM2 or MYCN |
KR102506169B1 (en) | 2014-09-05 | 2023-03-08 | 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 |
KR20180026739A (en) | 2015-07-06 | 2018-03-13 | 알엑스아이 파마슈티칼스 코포레이션 | A nucleic acid molecule targeting superoxide dismutase 1 (SOD1) |
EP3365446A4 (en) | 2015-10-19 | 2019-06-26 | Phio Pharmaceuticals Corp. | Reduced size self-delivering nucleic acid compounds targeting long non-coding rna |
Family Cites Families (7)
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 |
EP0289619B1 (en) * | 1986-10-30 | 1995-08-16 | Daicel Chemical Industries, Ltd. | Process for synthesizing oligonucleotides and compounds for forming high-molecular protective group |
US4816571A (en) * | 1987-06-04 | 1989-03-28 | Applied Biosystems, Inc. | Chemical capping by phosphitylation during oligonucleotide synthesis |
AU658562B2 (en) * | 1989-10-24 | 1995-04-27 | Isis Pharmaceuticals, 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 |
-
1993
- 1993-01-20 NZ NZ245720A patent/NZ245720A/en not_active IP Right Cessation
- 1993-01-20 FI FI930220A patent/FI115214B/en not_active IP Right Cessation
- 1993-01-20 KR KR1019930000675A patent/KR930016437A/en not_active Application Discontinuation
- 1993-01-20 IL IL10446193A patent/IL104461A/en not_active IP Right Cessation
- 1993-01-21 CA CA002087818A patent/CA2087818C/en not_active Expired - Lifetime
- 1993-01-21 DE DE59310285T patent/DE59310285D1/en not_active Expired - Lifetime
- 1993-01-21 AT AT93100892T patent/ATE217880T1/en active
- 1993-01-21 JP JP00839193A patent/JP3717081B2/en not_active Expired - Lifetime
- 1993-01-21 ES ES93100892T patent/ES2177532T3/en not_active Expired - Lifetime
- 1993-01-21 PT PT93100892T patent/PT552766E/en unknown
- 1993-01-21 ZA ZA93422A patent/ZA93422B/en unknown
- 1993-01-21 HU HU9300162A patent/HU227794B1/en unknown
- 1993-01-21 NO NO930199A patent/NO308215B1/en not_active IP Right Cessation
- 1993-01-21 AU AU31910/93A patent/AU661365B2/en not_active Expired
- 1993-01-21 DK DK93100892T patent/DK0552766T3/en active
- 1993-01-21 EP EP93100892A patent/EP0552766B1/en not_active Expired - Lifetime
- 1993-01-22 PL PL93297515A patent/PL172257B1/en unknown
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU666121B2 (en) * | 1991-05-21 | 1996-02-01 | Isis Pharmaceuticals, Inc. | Backbone modified oligonucleotide analogues |
AU657191B2 (en) * | 1992-01-22 | 1995-03-02 | Hoechst Aktiengesellschaft | 3'-derivatized oligonucleotide analogs with nonnucleotidic groupings, their preparation and use |
AU704549B2 (en) * | 1994-03-18 | 1999-04-29 | Lynx Therapeutics, Inc. | Oligonucleotide N3'-P5' phosphoramidates: synthesis and compounds; hybridization and nuclease resistance properties |
Also Published As
Publication number | Publication date |
---|---|
PT552766E (en) | 2002-10-31 |
HU9300162D0 (en) | 1993-04-28 |
IL104461A (en) | 2001-05-20 |
NZ245720A (en) | 1995-12-21 |
ES2177532T3 (en) | 2002-12-16 |
EP0552766A2 (en) | 1993-07-28 |
JP3717081B2 (en) | 2005-11-16 |
DK0552766T3 (en) | 2002-08-19 |
NO308215B1 (en) | 2000-08-14 |
PL297515A1 (en) | 1993-09-06 |
HU227794B1 (en) | 2012-03-28 |
NO930199D0 (en) | 1993-01-21 |
PL172257B1 (en) | 1997-08-29 |
CA2087818C (en) | 2007-07-10 |
JPH05310779A (en) | 1993-11-22 |
DE59310285D1 (en) | 2002-06-27 |
IL104461A0 (en) | 1993-05-13 |
ATE217880T1 (en) | 2002-06-15 |
EP0552766B1 (en) | 2002-05-22 |
CA2087818A1 (en) | 1993-07-23 |
EP0552766A3 (en) | 1994-09-07 |
KR930016437A (en) | 1993-08-26 |
HUT63173A (en) | 1993-07-28 |
FI930220A (en) | 1993-07-23 |
FI115214B (en) | 2005-03-31 |
NO930199L (en) | 1993-07-23 |
FI930220A0 (en) | 1993-01-20 |
AU661365B2 (en) | 1995-07-20 |
ZA93422B (en) | 1993-09-16 |
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