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WO2004096233A3 - Nucleoside phosphonate conjugates - Google Patents

Nucleoside phosphonate conjugates Download PDF

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Publication number
WO2004096233A3
WO2004096233A3 PCT/US2004/013060 US2004013060W WO2004096233A3 WO 2004096233 A3 WO2004096233 A3 WO 2004096233A3 US 2004013060 W US2004013060 W US 2004013060W WO 2004096233 A3 WO2004096233 A3 WO 2004096233A3
Authority
WO
WIPO (PCT)
Prior art keywords
nucleoside phosphonate
phosphonate conjugates
compounds
conjugates
nucleoside
Prior art date
Application number
PCT/US2004/013060
Other languages
French (fr)
Other versions
WO2004096233A2 (en
Inventor
Constantine G Boojamara
James M Chen
Xiaowu Chen
Aesop Cho
Lee S Chong
Maria Fardis
Alan X Huang
Choung X Kim
Thorsten A Kirschberg
Christopher P Lee
David Oare
Vidya K Prasad
Adrian S Ray
Sundaramoorthi Swaminathan
Will Watkins
Original Assignee
Gilead Sciences Inc
Constantine G Boojamara
James M Chen
Xiaowu Chen
Aesop Cho
Lee S Chong
Maria Fardis
Alan X Huang
Choung X Kim
Thorsten A Kirschberg
Christopher P Lee
David Oare
Vidya K Prasad
Adrian S Ray
Sundaramoorthi Swaminathan
Will Watkins
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 Gilead Sciences Inc, Constantine G Boojamara, James M Chen, Xiaowu Chen, Aesop Cho, Lee S Chong, Maria Fardis, Alan X Huang, Choung X Kim, Thorsten A Kirschberg, Christopher P Lee, David Oare, Vidya K Prasad, Adrian S Ray, Sundaramoorthi Swaminathan, Will Watkins filed Critical Gilead Sciences Inc
Publication of WO2004096233A2 publication Critical patent/WO2004096233A2/en
Publication of WO2004096233A3 publication Critical patent/WO2004096233A3/en

Links

Classifications

    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention is related to phosphorus substituted nucleoside compounds and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
PCT/US2004/013060 2003-04-25 2004-04-26 Nucleoside phosphonate conjugates WO2004096233A2 (en)

Applications Claiming Priority (130)

Application Number Priority Date Filing Date Title
US46575903P 2003-04-25 2003-04-25
US46572003P 2003-04-25 2003-04-25
US46560203P 2003-04-25 2003-04-25
US46534703P 2003-04-25 2003-04-25
US46546303P 2003-04-25 2003-04-25
US46563303P 2003-04-25 2003-04-25
US46555303P 2003-04-25 2003-04-25
US46558403P 2003-04-25 2003-04-25
US46566703P 2003-04-25 2003-04-25
US46558703P 2003-04-25 2003-04-25
US46555403P 2003-04-25 2003-04-25
US46554803P 2003-04-25 2003-04-25
US46582103P 2003-04-25 2003-04-25
US46555903P 2003-04-25 2003-04-25
US46563403P 2003-04-25 2003-04-25
US46559103P 2003-04-25 2003-04-25
US46569603P 2003-04-25 2003-04-25
US46554403P 2003-04-25 2003-04-25
US46560803P 2003-04-25 2003-04-25
US46568403P 2003-04-25 2003-04-25
US46557403P 2003-04-25 2003-04-25
US46556103P 2003-04-25 2003-04-25
US46569803P 2003-04-25 2003-04-25
US46560003P 2003-04-25 2003-04-25
US46540003P 2003-04-25 2003-04-25
US46561003P 2003-04-25 2003-04-25
US46546703P 2003-04-25 2003-04-25
US46553703P 2003-04-25 2003-04-25
US46555003P 2003-04-25 2003-04-25
US60/465,347 2003-04-25
US60/465,821 2003-04-25
US60/465,591 2003-04-25
US60/465,400 2003-04-25
US60/465,600 2003-04-25
US60/465,698 2003-04-25
US60/465,548 2003-04-25
US60/465,610 2003-04-25
US60/465,634 2003-04-25
US60/465,561 2003-04-25
US60/465,584 2003-04-25
US60/465,550 2003-04-25
US60/465,574 2003-04-25
US60/465,559 2003-04-25
US60/465,602 2003-04-25
US60/465,554 2003-04-25
US60/465,537 2003-04-25
US60/465,667 2003-04-25
US60/465,720 2003-04-25
US60/465,696 2003-04-25
US60/465,587 2003-04-25
US60/465,544 2003-04-25
US60/465,759 2003-04-25
US60/465,463 2003-04-25
US60/465,553 2003-04-25
US60/465,467 2003-04-25
US60/465,633 2003-04-25
US60/465,684 2003-04-25
US60/465,608 2003-04-25
US49556403P 2003-08-15 2003-08-15
US49577203P 2003-08-15 2003-08-15
US49538703P 2003-08-15 2003-08-15
US49549103P 2003-08-15 2003-08-15
US49545303P 2003-08-15 2003-08-15
US49549003P 2003-08-15 2003-08-15
US49576003P 2003-08-15 2003-08-15
US49527803P 2003-08-15 2003-08-15
US49552503P 2003-08-15 2003-08-15
US49534403P 2003-08-15 2003-08-15
US49576303P 2003-08-15 2003-08-15
US49560003P 2003-08-15 2003-08-15
US49559203P 2003-08-15 2003-08-15
US49531703P 2003-08-15 2003-08-15
US49534903P 2003-08-15 2003-08-15
US49553903P 2003-08-15 2003-08-15
US49568403P 2003-08-15 2003-08-15
US49569603P 2003-08-15 2003-08-15
US49563303P 2003-08-15 2003-08-15
US49534303P 2003-08-15 2003-08-15
US49527703P 2003-08-15 2003-08-15
US49580503P 2003-08-15 2003-08-15
US49541703P 2003-08-15 2003-08-15
US49563103P 2003-08-15 2003-08-15
US49567103P 2003-08-15 2003-08-15
US49527303P 2003-08-15 2003-08-15
US49596403P 2003-08-15 2003-08-15
US49533403P 2003-08-15 2003-08-15
US60/495,600 2003-08-15
US60/495,805 2003-08-15
US60/495,592 2003-08-15
US60/495,343 2003-08-15
US60/495,525 2003-08-15
US60/495,273 2003-08-15
US60/495,453 2003-08-15
US60/495,334 2003-08-15
US60/495,490 2003-08-15
US60/495,633 2003-08-15
US60/495,539 2003-08-15
US60/495,760 2003-08-15
US60/495,772 2003-08-15
US60/495,317 2003-08-15
US60/495,387 2003-08-15
US60/495,344 2003-08-15
US60/495,671 2003-08-15
US60/495,696 2003-08-15
US60/495,964 2003-08-15
US60/495,631 2003-08-15
US60/495,278 2003-08-15
US60/495,684 2003-08-15
US60/495,491 2003-08-15
US60/495,564 2003-08-15
US60/495,763 2003-08-15
US60/495,417 2003-08-15
US60/495,277 2003-08-15
US60/495,349 2003-08-15
US51024503P 2003-10-10 2003-10-10
US60/510,245 2003-10-10
US51415903P 2003-10-24 2003-10-24
US51394903P 2003-10-24 2003-10-24
US51408303P 2003-10-24 2003-10-24
US51392603P 2003-10-24 2003-10-24
US51414403P 2003-10-24 2003-10-24
US51393203P 2003-10-24 2003-10-24
US60/513,932 2003-10-24
US60/514,083 2003-10-24
US60/514,144 2003-10-24
US60/514,159 2003-10-24
US60/513,926 2003-10-24
US60/513,949 2003-10-24
US53194003P 2003-12-22 2003-12-22
US60/531,940 2003-12-22

Publications (2)

Publication Number Publication Date
WO2004096233A2 WO2004096233A2 (en) 2004-11-11
WO2004096233A3 true WO2004096233A3 (en) 2005-06-16

Family

ID=33425963

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/013060 WO2004096233A2 (en) 2003-04-25 2004-04-26 Nucleoside phosphonate conjugates

Country Status (1)

Country Link
WO (1) WO2004096233A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9243025B2 (en) 2011-03-31 2016-01-26 Idenix Pharmaceuticals, Llc Compounds and pharmaceutical compositions for the treatment of viral infections
US9579332B2 (en) 2004-07-27 2017-02-28 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds

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* Cited by examiner, † Cited by third party
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PT1628685E (en) 2003-04-25 2011-03-16 Gilead Sciences Inc Antiviral phosphonate analogs
EP1720890B1 (en) 2004-03-04 2015-05-20 K.U.Leuven Research & Development Phosponate nucleosides useful as active ingredients in pharmaceutical compositions for the treatment of viral infections, and intermediates for their production
WO2006037090A2 (en) * 2004-09-28 2006-04-06 Purdue Research Foundation Drug-phosphate conjugates as prodrugs
EP2561872B1 (en) 2004-12-17 2014-09-10 Anadys Pharmaceuticals, Inc. 3, 5-DISUBSTITUTED AND 3,5,7-TRISUBSTITUTED-3H-OXAZOLO [4,5-d]PYRIMIDIN-2-ONE COMPOUNDS AND PRODRUGS THEREOF
CA2616314A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
NZ544187A (en) * 2005-12-15 2008-07-31 Ind Res Ltd Deazapurine analogs of 1'-aza-l-nucleosides
US8895531B2 (en) 2006-03-23 2014-11-25 Rfs Pharma Llc 2′-fluoronucleoside phosphonates as antiviral agents
WO2008005542A2 (en) 2006-07-07 2008-01-10 Gilead Sciences, Inc., Antiviral phosphinate compounds
US7951789B2 (en) 2006-12-28 2011-05-31 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
DK2307435T3 (en) 2008-07-08 2012-09-10 Gilead Sciences Inc Salts of HIV inhibitor compounds
US9394333B2 (en) 2008-12-02 2016-07-19 Wave Life Sciences Japan Method for the synthesis of phosphorus atom modified nucleic acids
RU2612521C2 (en) 2009-07-06 2017-03-09 Онтории, Инк. Novel prodrugs of nucleic acids and their application methods
WO2011123586A1 (en) 2010-04-01 2011-10-06 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
EP2620428B1 (en) 2010-09-24 2019-05-22 Wave Life Sciences Ltd. Asymmetric auxiliary group
JP6128529B2 (en) 2011-07-19 2017-05-17 ウェイブ ライフ サイエンシズ リミテッドＷａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｌｔｄ． Methods for the synthesis of functionalized nucleic acids
CN104684893B (en) 2012-07-13 2016-10-26 日本波涛生命科学公司 Asymmetric auxiliary group
EP3094728B1 (en) 2014-01-16 2022-03-09 Wave Life Sciences Ltd. Chiral design
JP7125144B2 (en) * 2016-09-09 2022-08-24 キャリセラ バイオサイエンシーズ， インコーポレイテッド Ectonucleotidase inhibitors and methods of use thereof
EP3518934A4 (en) * 2016-10-03 2020-06-24 Arcus Biosciences, Inc. Inhibitors of adenosine 5'-nucleotidase
MX383880B (en) 2016-12-22 2025-03-14 Antengene Therapeutics Ltd ECTONUCLEOTIDASE INHIBITORS AND METHODS OF USING THEM.
ES2892402T3 (en) 2017-08-01 2022-02-04 Gilead Sciences Inc Crystal forms of ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl Ethyl)(phenoxy)phosphoryl)-L-alaninate to treat viral infections
JP7538047B2 (en) 2018-06-21 2024-08-21 アンテンジーン セラピューティクス リミテッド Ectonucleotidase inhibitors and methods of use thereof

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991019721A1 (en) * 1990-06-13 1991-12-26 Arnold Glazier Phosphorous produgs
WO1992000988A1 (en) * 1990-07-13 1992-01-23 Bodor Nicholas S Targeted drug delivery via phosphonate derivatives
WO1992018520A1 (en) * 1991-04-10 1992-10-29 Knoll Ag Novel cytarabine derivatives, their production and use
WO1993024510A1 (en) * 1992-05-25 1993-12-09 Centre National De La Recherche Scientifique (Cnrs) Phosphotriester-type biologically active compounds
WO1999062921A1 (en) * 1998-06-01 1999-12-09 S & T Science And Technology Inc. Antiviral phosphorus derivatives of 4'-thio-5-ethyl-2'-deoxyuridine
US20030109498A1 (en) * 2001-06-20 2003-06-12 Mitsubishi Pharma Corporation Antiviral agent for drug-resistant virus
WO2003080078A1 (en) * 2002-03-18 2003-10-02 Mitsubishi Pharma Corporation Treatment of pre-core hepatitis b virus mutant infections
WO2003090690A2 (en) * 2002-04-26 2003-11-06 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991019721A1 (en) * 1990-06-13 1991-12-26 Arnold Glazier Phosphorous produgs
WO1992000988A1 (en) * 1990-07-13 1992-01-23 Bodor Nicholas S Targeted drug delivery via phosphonate derivatives
WO1992018520A1 (en) * 1991-04-10 1992-10-29 Knoll Ag Novel cytarabine derivatives, their production and use
WO1993024510A1 (en) * 1992-05-25 1993-12-09 Centre National De La Recherche Scientifique (Cnrs) Phosphotriester-type biologically active compounds
WO1999062921A1 (en) * 1998-06-01 1999-12-09 S & T Science And Technology Inc. Antiviral phosphorus derivatives of 4'-thio-5-ethyl-2'-deoxyuridine
US20030109498A1 (en) * 2001-06-20 2003-06-12 Mitsubishi Pharma Corporation Antiviral agent for drug-resistant virus
WO2003080078A1 (en) * 2002-03-18 2003-10-02 Mitsubishi Pharma Corporation Treatment of pre-core hepatitis b virus mutant infections
WO2003090690A2 (en) * 2002-04-26 2003-11-06 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PARANG K ET AL: "NOVEL APPROACHES FOR DESIGNING 5'-O-ESTER PRODRUGS OF 3'-AZIDO-2',3'-DIDEOXYTHYMIDINE (AZT)", CURRENT MEDICINAL CHEMISTRY, BENTHAM SCIENCE PUBLISHERS BV, BE, vol. 7, no. 10, October 2000 (2000-10-01), pages 995 - 1039, XP009038285, ISSN: 0929-8673 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9579332B2 (en) 2004-07-27 2017-02-28 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds
US9243025B2 (en) 2011-03-31 2016-01-26 Idenix Pharmaceuticals, Llc Compounds and pharmaceutical compositions for the treatment of viral infections

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