ES2177532T3 - Compuestos analogos a oligonucleotidos, su preparacion y utilizacion. - Google Patents

Compuestos analogos a oligonucleotidos, su preparacion y utilizacion.

Info

Publication number
ES2177532T3
ES2177532T3 ES93100892T ES93100892T ES2177532T3 ES 2177532 T3 ES2177532 T3 ES 2177532T3 ES 93100892 T ES93100892 T ES 93100892T ES 93100892 T ES93100892 T ES 93100892T ES 2177532 T3 ES2177532 T3 ES 2177532T3
Authority
ES
Spain
Prior art keywords
equivalate
rent
arilo
equivalent
equival
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.)
Expired - Lifetime
Application number
ES93100892T
Other languages
English (en)
Inventor
Eugen Dr Uhlmann
Anuschirwan Dr Peyman
Gerard Dr O'malley
Matthias Dr Helsberg
Irvin Dr Winkler
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi Aventis Deutschland GmbH
Original Assignee
Aventis Pharma Deutschland 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 Deutschland GmbH filed Critical Aventis Pharma Deutschland GmbH
Application granted granted Critical
Publication of ES2177532T3 publication Critical patent/ES2177532T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biotechnology (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

LA INVENCION CONCIERNE A COMPUESTOS DE FORMULA I, DONDE R1 EQUIVALE A ALQUILO, ACILO, ARILO O A UN RESTO FOSFATO; R2 EQUIVALE A H, OH, ALCOXI, NH2 O HALOGENO; B EQUIVALE A UNA BASE USUAL EN LA QUIMICA DE LOS NUCLEOTIDOS; A EQUIVALE A O O CH2; N EQUIVALE A UNA CIFRA ENTERA DE 1 A 100; W = O, S O EQUIVALE A SE; V = O, S O EQUIVALE A NH; Y = O, S, NH O CH2; Y'' = O, S, NH O EQUIVALE A ALQUILENO; X = OH O EQUIVALE A SH; U = OH, SH, SEH O EQUIVALE A ALQUILO, ARILO O AMINO, Y Z = OH, SH, SEH, A UN RESTO DADO EL CASO SUSTITUIDO DE LA SERIE ALQUILO, ARILO, HETEROARILO, ALCOXI O AMINO, O EQUIVALE A UN GRUPO QUE FAVORECE LA ABSORCION INTRACELULAR, O COMO MARCADOR DE UNA SONDA DNA, O QUE ATACA EN LA HIBRIDIZACION LA PROTECCION DEL ACIDO NUCLEINICO, POR LO QUE EN CASO DE QUE Z = OH, SH, CH3 O OC2H5, AL MENOS UNO DEL GRUPO X, Y, Y'', V, W ES DIFERENTE DE OH U O, O R1 ES DIFERENTE DE H; PROCEDIMIENTO PARA SU OBTENCION Y SU UTILIZACION COMO INHIBIDORES DE LA EXPRESION DE GENES, COMO SONDAS PARA LA COMPROBACION DE ACIDOS NUCLEINICOS Y COMO AGENTE AUXILIAR EN LA BIOLOGIA MOLECULAR.
ES93100892T 1992-01-22 1993-01-21 Compuestos analogos a oligonucleotidos, su preparacion y utilizacion. Expired - Lifetime ES2177532T3 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ES2177532T3 true ES2177532T3 (es) 2002-12-16

Family

ID=6450030

Family Applications (1)

Application Number Title Priority Date Filing Date
ES93100892T Expired - Lifetime ES2177532T3 (es) 1992-01-22 1993-01-21 Compuestos analogos a oligonucleotidos, su preparacion y utilizacion.

Country Status (17)

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

Families Citing this family (54)

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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
EP0593901B2 (de) * 1992-09-24 2008-04-09 Sanofi-Aventis Deutschland GmbH Oligoribonucleotid- und Ribozym-Analoga mit terminalen 3'-3'-bzw.5'-5'-Verknüpfungen
EP0602524A1 (de) * 1992-12-15 1994-06-22 Hoechst Aktiengesellschaft Chemilumineszenzmarkierte Gensonden und ihre Verwendung in Gensondentesten
EP0678096B1 (en) * 1993-01-08 1997-03-19 HYBRIDON, Inc. Synthesis of dimmer blocks and their use in assembling oligonucleotides
US6087491A (en) * 1993-01-08 2000-07-11 Hybridon, Inc. Extremely high purity oligonucleotides and methods of synthesizing them using dimer blocks
ATE138384T1 (de) * 1993-01-25 1996-06-15 Hybridon Inc Olionukleotidalkylphosphonate und - phosphonothioate
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 (de) * 1993-09-17 1995-03-23 Hoechst Ag Neue Antisense-Oligonucleotide gegen HSV-1 sowie deren Herstellung
DE4338704A1 (de) 1993-11-12 1995-05-18 Hoechst Ag Stabilisierte Oligonucleotide und deren Verwendung
US6919441B2 (en) 1994-03-14 2005-07-19 Aventis Pharma Deutschland Gmbh Polyamide-oligonucleotide derivatives, their preparation and use
DE4408528A1 (de) * 1994-03-14 1995-09-28 Hoechst Ag Peptid-Oligonucleotid-Derivate, deren Herstellung und Verwendung
US5726297A (en) * 1994-03-18 1998-03-10 Lynx Therapeutics, Inc. Oligodeoxyribonucleotide N3' P5' phosphoramidates
CZ274596A3 (en) * 1994-03-18 1997-03-12 Lynx Therapeutics Oligonucleotide n3 - p5 phosphoramidates and process of their synthesis and hybridization
US5599922A (en) * 1994-03-18 1997-02-04 Lynx Therapeutics, Inc. Oligonucleotide N3'-P5' phosphoramidates: hybridization and nuclease resistance properties
DE4415370A1 (de) * 1994-05-02 1995-11-09 Hoechst Ag Modifizierte Oligonukleotide, deren Herstellung sowie deren Verwendung
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 (de) * 1994-11-04 1996-05-09 Hoechst Ag Modifizierte Oligonukleotide, deren Herstellung sowie deren Verwendung
US6150510A (en) * 1995-11-06 2000-11-21 Aventis Pharma Deutschland Gmbh Modified oligonucleotides, their preparation and their use
DE19502912A1 (de) * 1995-01-31 1996-08-01 Hoechst Ag G-Cap Stabilisierte Oligonucleotide
ATE206131T1 (de) * 1995-03-13 2001-10-15 Aventis Pharma Gmbh Phosphonomonoesternnukleinsäuren, verfahren zu ihrer herstellung und ihre verwendung
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
ES2221942T3 (es) * 1996-05-24 2005-01-16 Aventis Pharma Deutschland Gmbh Reactivo y metodo para inhibir la expresion de n-ras.
DE19627898A1 (de) * 1996-07-11 1998-01-15 Hoechst Ag Festphasensynthese von Oligonucleotiden
WO1998050540A1 (en) * 1997-05-05 1998-11-12 Hoechst Marion Roussel Deutschland Gmbh 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 (de) 1998-11-11 2000-05-31 DALLI-WERKE WÄSCHE- und KÖRPERPFLEGE GmbH & Co. KG Verdichtetes Granulat, Herstellungsverfahren und Verwendung als Sprengmittel für gepresste Formkörper (2)
DE19935302A1 (de) 1999-07-28 2001-02-08 Aventis Pharma Gmbh Konjugate und Verfahren zu deren Herstellung sowie deren Verwendung zum Transport von Molekülen über biologische Membranen
DE19935303A1 (de) 1999-07-28 2001-02-08 Aventis Pharma Gmbh Oligonukleotide zur Inhibierung der Expression von humanem eg5
DE10133915A1 (de) 2001-07-12 2003-02-06 Aventis Pharma Gmbh Neue Oligoribonucleotid-Derivate zur gezielten Hemmung der Genexpression
EP1660657A1 (en) 2003-08-28 2006-05-31 Novartis AG Interfering rna duplex having blunt-ends and 3'-modifications
GB0608838D0 (en) 2006-05-04 2006-06-14 Novartis Ag Organic compounds
CA2715289C (en) 2008-02-11 2019-12-24 Rxi Pharmaceuticals Corporation Modified rnai polynucleotides and uses thereof
US8815818B2 (en) 2008-07-18 2014-08-26 Rxi Pharmaceuticals Corporation Phagocytic cell delivery of RNAI
EP2342340A1 (en) 2008-09-22 2011-07-13 Rxi Pharmaceuticals Corporation Rna interference in skin indications
WO2010059226A2 (en) 2008-11-19 2010-05-27 Rxi Pharmaceuticals Corporation Inhibition of map4k4 through rnai
US9745574B2 (en) 2009-02-04 2017-08-29 Rxi Pharmaceuticals Corporation RNA duplexes with single stranded phosphorothioate nucleotide regions for additional functionality
CN103200945B (zh) 2010-03-24 2016-07-06 雷克西制药公司 眼部症候中的rna干扰
EP3560503B1 (en) 2010-03-24 2021-11-17 Phio Pharmaceuticals Corp. Rna interference in dermal and fibrotic indications
RU2615143C2 (ru) 2010-03-24 2017-04-04 Адвирна Самодоставляющие PHKi соединения уменьшенного размера
CN106061488B (zh) 2013-12-02 2021-04-09 菲奥医药公司 癌症的免疫治疗
WO2015125845A1 (ja) * 2014-02-20 2015-08-27 塩野義製薬株式会社 含窒素非芳香族複素環を含む核酸のリン酸部位修飾
WO2015168108A2 (en) 2014-04-28 2015-11-05 Rxi Pharmaceuticals Corporation Methods for treating cancer using nucleic targeting mdm2 or mycn
US10900039B2 (en) 2014-09-05 2021-01-26 Phio Pharmaceuticals Corp. Methods for treating aging and skin disorders using nucleic acids targeting Tyr or MMP1
EP3862005A1 (en) 2015-07-06 2021-08-11 Phio Pharmaceuticals Corp. Nucleic acid molecules targeting superoxide dismutase 1 (sod1)
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
WO2017070151A1 (en) 2015-10-19 2017-04-27 Rxi Pharmaceuticals Corporation Reduced size self-delivering nucleic acid compounds targeting long non-coding rna
US12544344B2 (en) 2017-04-19 2026-02-10 Phio Pharmaceuticals Corp. Topical delivery of nucleic acid compounds
MX2020011570A (es) 2018-05-07 2020-11-24 Alnylam Pharmaceuticals Inc Administracion extrahepatica.

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3239888A1 (de) * 1982-10-28 1984-05-03 Hubert Prof. Dr. 2000 Hamburg Köster Verfahren zur herstellung von oligonucleosidphosphonaten
US4739044A (en) * 1985-06-13 1988-04-19 Amgen Method for derivitization of polynucleotides
DE3751468T2 (de) * 1986-10-30 1996-02-29 Daicel Chem Verfahren zur herstellung von oligonukleotiden und verbindungen zur bildung hochmolekularer schutzgruppen.
US4816571A (en) * 1987-06-04 1989-03-28 Applied Biosystems, Inc. Chemical capping by phosphitylation during oligonucleotide synthesis
DE69034150T2 (de) * 1989-10-24 2005-08-25 Isis Pharmaceuticals, Inc., Carlsbad 2'-Modifizierte Oligonukleotide
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
NZ245720A (en) 1995-12-21
NO308215B1 (no) 2000-08-14
EP0552766A3 (en) 1994-09-07
JP3717081B2 (ja) 2005-11-16
FI115214B (fi) 2005-03-31
IL104461A0 (en) 1993-05-13
FI930220L (fi) 1993-07-23
HU9300162D0 (en) 1993-04-28
EP0552766A2 (de) 1993-07-28
PL297515A1 (en) 1993-09-06
NO930199L (no) 1993-07-23
ATE217880T1 (de) 2002-06-15
DE59310285D1 (de) 2002-06-27
HUT63173A (en) 1993-07-28
FI930220A0 (fi) 1993-01-20
NO930199D0 (no) 1993-01-21
AU3191093A (en) 1993-07-29
EP0552766B1 (de) 2002-05-22
KR930016437A (ko) 1993-08-26
HU227794B1 (en) 2012-03-28
ZA93422B (en) 1993-09-16
IL104461A (en) 2001-05-20
PT552766E (pt) 2002-10-31
JPH05310779A (ja) 1993-11-22
CA2087818A1 (en) 1993-07-23
AU661365B2 (en) 1995-07-20
CA2087818C (en) 2007-07-10
DK0552766T3 (da) 2002-08-19
PL172257B1 (pl) 1997-08-29

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