CA2925500C - Phosphorodiamidate backbone linkage for oligonucleotides - Google Patents

Phosphorodiamidate backbone linkage for oligonucleotides Download PDF

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CA2925500C
CA2925500C CA2925500A CA2925500A CA2925500C CA 2925500 C CA2925500 C CA 2925500C CA 2925500 A CA2925500 A CA 2925500A CA 2925500 A CA2925500 A CA 2925500A CA 2925500 C CA2925500 C CA 2925500C
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alkyl
hydrogen
compound
salt
oligonucleotide
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French (fr)
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CA2925500A1 (en
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Krisztina Pongracz
Mahesh Ramaseshan
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Geron Corp
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Geron Corp
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    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
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CA2925500A 2013-09-30 2014-09-26 Phosphorodiamidate backbone linkage for oligonucleotides Active CA2925500C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361884848P 2013-09-30 2013-09-30
US61/884,848 2013-09-30
PCT/US2014/057876 WO2015048558A1 (en) 2013-09-30 2014-09-26 Phosphorodiamidate backbone linkage for oligonucleotides

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Publication Number Publication Date
CA2925500A1 CA2925500A1 (en) 2015-04-02
CA2925500C true CA2925500C (en) 2023-03-14

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CA2925500A Active CA2925500C (en) 2013-09-30 2014-09-26 Phosphorodiamidate backbone linkage for oligonucleotides

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US (2) US9708360B2 (enExample)
EP (2) EP3052512A4 (enExample)
JP (2) JP6794258B2 (enExample)
CA (1) CA2925500C (enExample)
WO (1) WO2015048558A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2925500C (en) * 2013-09-30 2023-03-14 Geron Corporation Phosphorodiamidate backbone linkage for oligonucleotides
CN109160931A (zh) * 2017-08-17 2019-01-08 王秀香 一种1/2水胞磷胆碱钠化合物
WO2020086311A1 (en) * 2018-10-23 2020-04-30 The Regents Of The University Of California Thiophosphorodichloridate reagents for chemoselective histidine bioconjugation

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4394448A (en) 1978-02-24 1983-07-19 Szoka Jr Francis C Method of inserting DNA into living cells
NZ209840A (en) 1983-10-17 1988-11-29 Kaji Akira A method of inhibiting viral propagation by hybridising dna with the viral rna thus blocking its action
US5550111A (en) 1984-07-11 1996-08-27 Temple University-Of The Commonwealth System Of Higher Education Dual action 2',5'-oligoadenylate antiviral derivatives and uses thereof
US4897355A (en) 1985-01-07 1990-01-30 Syntex (U.S.A.) Inc. N[ω,(ω-1)-dialkyloxy]- and N-[ω,(ω-1)-dialkenyloxy]-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor
US6448392B1 (en) 1985-03-06 2002-09-10 Chimerix, Inc. Lipid derivatives of antiviral nucleosides: liposomal incorporation and method of use
US5217866A (en) 1985-03-15 1993-06-08 Anti-Gene Development Group Polynucleotide assay reagent and method
US5034506A (en) 1985-03-15 1991-07-23 Anti-Gene Development Group Uncharged morpholino-based polymers having achiral intersubunit linkages
EP0215942B1 (en) 1985-03-15 1995-07-12 Antivirals Inc. Polynucleotide assay reagent and method
US5185444A (en) 1985-03-15 1993-02-09 Anti-Gene Deveopment Group Uncharged morpolino-based polymers having phosphorous containing chiral intersubunit linkages
US5166315A (en) 1989-12-20 1992-11-24 Anti-Gene Development Group Sequence-specific binding polymers for duplex nucleic acids
US5506337A (en) 1985-03-15 1996-04-09 Antivirals Inc. Morpholino-subunit combinatorial library and method
US5521063A (en) 1985-03-15 1996-05-28 Antivirals Inc. Polynucleotide reagent containing chiral subunits and methods of use
US5194428A (en) 1986-05-23 1993-03-16 Worcester Foundation For Experimental Biology Inhibition of influenza virus replication by oligonucleotide phosphorothioates
US4806463A (en) 1986-05-23 1989-02-21 Worcester Foundation For Experimental Biology Inhibition of HTLV-III by exogenous oligonucleotides
US5264423A (en) 1987-03-25 1993-11-23 The United States Of America As Represented By The Department Of Health And Human Services Inhibitors for replication of retroviruses and for the expression of oncogene products
US5276019A (en) 1987-03-25 1994-01-04 The United States Of America As Represented By The Department Of Health And Human Services Inhibitors for replication of retroviruses and for the expression of oncogene products
US4924624A (en) 1987-10-22 1990-05-15 Temple University-Of The Commonwealth System Of Higher Education 2,',5'-phosphorothioate oligoadenylates and plant antiviral uses thereof
US5188897A (en) 1987-10-22 1993-02-23 Temple University Of The Commonwealth System Of Higher Education Encapsulated 2',5'-phosphorothioate oligoadenylates
WO1989009221A1 (en) 1988-03-25 1989-10-05 University Of Virginia Alumni Patents Foundation Oligonucleotide n-alkylphosphoramidates
US5278302A (en) 1988-05-26 1994-01-11 University Patents, Inc. Polynucleotide phosphorodithioates
US5194599A (en) 1988-09-23 1993-03-16 Gilead Sciences, Inc. Hydrogen phosphonodithioate compositions
US5004810A (en) 1988-09-30 1991-04-02 Schering Corporation Antiviral oligomers
US5098890A (en) 1988-11-07 1992-03-24 Temple University-Of The Commonwealth System Of Higher Education Antisence oligonucleotides to c-myb proto-oncogene and uses thereof
US5087617A (en) 1989-02-15 1992-02-11 Board Of Regents, The University Of Texas System Methods and compositions for treatment of cancer using oligonucleotides
US5411947A (en) 1989-06-28 1995-05-02 Vestar, Inc. Method of converting a drug to an orally available form by covalently bonding a lipid to the drug
US5399676A (en) 1989-10-23 1995-03-21 Gilead Sciences Oligonucleotides with inverted polarity
US5721218A (en) 1989-10-23 1998-02-24 Gilead Sciences, Inc. Oligonucleotides with inverted polarity
US5177198A (en) 1989-11-30 1993-01-05 University Of N.C. At Chapel Hill Process for preparing oligoribonucleoside and oligodeoxyribonucleoside boranophosphates
US5587361A (en) 1991-10-15 1996-12-24 Isis Pharmaceuticals, Inc. Oligonucleotides having phosphorothioate linkages of high chiral purity
US5321131A (en) 1990-03-08 1994-06-14 Hybridon, Inc. Site-specific functionalization of oligodeoxynucleotides for non-radioactive labelling
US5470967A (en) * 1990-04-10 1995-11-28 The Dupont Merck Pharmaceutical Company Oligonucleotide analogs with sulfamate linkages
US5166195A (en) 1990-05-11 1992-11-24 Isis Pharmaceuticals, Inc. Antisense inhibitors of the human immunodeficiency virus phosphorothioate oligonucleotides
US5135917A (en) 1990-07-12 1992-08-04 Nova Pharmaceutical Corporation Interleukin receptor expression inhibiting antisense oligonucleotides
US5177196A (en) 1990-08-16 1993-01-05 Microprobe Corporation Oligo (α-arabinofuranosyl nucleotides) and α-arabinofuranosyl precursors thereof
US5672697A (en) 1991-02-08 1997-09-30 Gilead Sciences, Inc. Nucleoside 5'-methylene phosphonates
US5242906A (en) 1991-04-22 1993-09-07 University Of North Carolina At Chapel Hill Antisense oligonucleotides against Epstein-Barr virus
US5571799A (en) 1991-08-12 1996-11-05 Basco, Ltd. (2'-5') oligoadenylate analogues useful as inhibitors of host-v5.-graft response
US6033909A (en) 1992-01-22 2000-03-07 Hoechst Aktiengesellschaft Oligonucleotide analogs, their preparation and use
US5629154A (en) 1993-11-12 1997-05-13 Geron Corporation Telomerase activity assays
US5837453A (en) 1992-05-13 1998-11-17 Geron Corporation Telomerase activity assays
US5476925A (en) 1993-02-01 1995-12-19 Northwestern University Oligodeoxyribonucleotides including 3'-aminonucleoside-phosphoramidate linkages and terminal 3'-amino groups
GB9304618D0 (en) 1993-03-06 1993-04-21 Ciba Geigy Ag Chemical compounds
US5863726A (en) 1993-11-12 1999-01-26 Geron Corporation Telomerase activity assays
US5726297A (en) 1994-03-18 1998-03-10 Lynx Therapeutics, Inc. Oligodeoxyribonucleotide N3' P5' phosphoramidates
US5625050A (en) 1994-03-31 1997-04-29 Amgen Inc. Modified oligonucleotides and intermediates useful in nucleic acid therapeutics
DE4415370A1 (de) * 1994-05-02 1995-11-09 Hoechst Ag Modifizierte Oligonukleotide, deren Herstellung sowie deren Verwendung
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
AU2445997A (en) * 1996-04-10 1997-10-29 Lynx Therapeutics, Inc. Telomerase inhibitors
DE19627898A1 (de) * 1996-07-11 1998-01-15 Hoechst Ag Festphasensynthese von Oligonucleotiden
WO1998028442A1 (en) 1996-12-20 1998-07-02 Geron Corporation Methods for detecting and inhibiting the rna component of telomerase
US6191120B1 (en) * 1998-03-25 2001-02-20 Wayne Hughes Institute Spermicidally active 5-halo-6-alkoxy-5,6-dihydro-2′,3′-dideoxy-uridines and their pharamaceutical compositions
US6482805B2 (en) * 1998-03-25 2002-11-19 Parker Hughes Institute AZT derivatives exhibiting spermicidal and anti-viral activity
KR100858465B1 (ko) 1999-09-10 2008-09-16 제론 코포레이션 올리고뉴클레오티드 엔3'→피5' 티오포스포라미데이트,이의 합성 및 용도
US7321029B2 (en) 2000-01-21 2008-01-22 Geron Corporation 2′-arabino-fluorooligonucleotide N3′→P5′ phosphoramidates: their synthesis and use
EP1379689B1 (en) * 2001-03-23 2012-09-26 Geron Corporation Oligonucleotide conjugates
EP1485396A2 (en) 2002-02-28 2004-12-15 Biota, Inc. Nucleoside 5'-monophosphate mimics and their prodrugs
BRPI0414222B8 (pt) 2003-09-09 2021-05-25 Geron Corp compostos oligonucleotídeos modificados para inibição da telomerase, métodos, composição farmacêutica e usos relacionados
ATE503014T1 (de) * 2003-11-04 2011-04-15 Geron Corp Rna-amidate und thioamidateur rnai
CA2571601C (en) 2004-07-02 2013-01-08 Geron Corporation Synthesis of protected 3'-amino nucleoside monomers
EP1876893B1 (en) * 2005-04-15 2012-04-11 Geron Corporation Cancer treatment by combined inhibition of proteasome and telomerase activities
WO2007127163A2 (en) 2006-04-24 2007-11-08 Geron Corporation Cns-tumor treatment method and composition
US8785409B2 (en) * 2007-01-30 2014-07-22 Geron Corporation Compounds having anti-adhesive effects on cancer cells
HRP20140646T1 (hr) 2007-11-15 2014-09-26 Sarepta Therapeutics, Inc. Postupak sinteze morfolino oligomera
CA2925500C (en) * 2013-09-30 2023-03-14 Geron Corporation Phosphorodiamidate backbone linkage for oligonucleotides

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CA2925500A1 (en) 2015-04-02
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US20150111958A1 (en) 2015-04-23
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