WO2008134578A3 - Synthèse d'inhibiteurs de transcriptase inverse radiomarqués actifs optiquement - Google Patents

Synthèse d'inhibiteurs de transcriptase inverse radiomarqués actifs optiquement Download PDF

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Publication number
WO2008134578A3
WO2008134578A3 PCT/US2008/061664 US2008061664W WO2008134578A3 WO 2008134578 A3 WO2008134578 A3 WO 2008134578A3 US 2008061664 W US2008061664 W US 2008061664W WO 2008134578 A3 WO2008134578 A3 WO 2008134578A3
Authority
WO
WIPO (PCT)
Prior art keywords
reverse transcriptase
transcriptase inhibitors
synthesis
optically active
active radio
Prior art date
Application number
PCT/US2008/061664
Other languages
English (en)
Other versions
WO2008134578A2 (fr
Inventor
Dale O Kiesewetter
Mascio Michele Di
Esther Lim
Original Assignee
Us Gov Health & Human Serv
Dale O Kiesewetter
Mascio Michele Di
Esther Lim
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 Us Gov Health & Human Serv, Dale O Kiesewetter, Mascio Michele Di, Esther Lim filed Critical Us Gov Health & Human Serv
Publication of WO2008134578A2 publication Critical patent/WO2008134578A2/fr
Publication of WO2008134578A3 publication Critical patent/WO2008134578A3/fr

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Classifications

    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

L'invention concerne des inhibiteurs de transcriptase inverse marqués de manière isotope, y compris des composés selon la formule (I) dans laquelle R1 et R2 sont sélectionnés indépendamment parmi H, un groupe alkyle inférieur, aralkyle et acyle, et Z1 et Z2 forment indépendamment un phosphoester ou un phosphoamide. Des procédés pour synthétiser de tels composés sous des formes optiquement pures et racémiques sont également décrits. Des procédés d'utilisation des composés marqués, par exemple dans la surveillance par tomographie par émission de positons (PET), de l'activité rétrovirale sont également décrits.
PCT/US2008/061664 2007-04-28 2008-04-25 Synthèse d'inhibiteurs de transcriptase inverse radiomarqués actifs optiquement WO2008134578A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US91473207P 2007-04-28 2007-04-28
US60/914,732 2007-04-28

Publications (2)

Publication Number Publication Date
WO2008134578A2 WO2008134578A2 (fr) 2008-11-06
WO2008134578A3 true WO2008134578A3 (fr) 2008-12-31

Family

ID=39577875

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/061664 WO2008134578A2 (fr) 2007-04-28 2008-04-25 Synthèse d'inhibiteurs de transcriptase inverse radiomarqués actifs optiquement

Country Status (1)

Country Link
WO (1) WO2008134578A2 (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101928302B (zh) * 2010-04-29 2012-09-12 浙江康多利药业有限公司 N-苄基-9-[2-(二烷基磷酰基甲氧基)烷基]腺嘌呤及其制备方法和应用
CN102885846B (zh) * 2011-07-18 2014-02-19 中国医学科学院医药生物技术研究所 2-硫代-6-氮杂尿苷在制备抗hiv-1病毒的药物中的应用
DK2794624T3 (da) 2011-12-22 2019-07-22 Geron Corp Guanin-analoger som telomerase-substrater og påvirkere af telomer-længde
CN103665043B (zh) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 一种替诺福韦前药及其在医药上的应用
EP3714907A1 (fr) * 2019-03-29 2020-09-30 Santopietro, Riccardo Protocoles d'élution et dosages pour système d'élution radiopharmaceutique
CN114761014A (zh) * 2019-09-20 2022-07-15 雅培快速诊断国际无限公司 针对替诺福韦及其衍生物的抗体

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KIESEWETTER ET AL: "Enantiomeric radiochemical synthesis of R and S (1-(6-amino-9H-purin-9-yl)-3-fluoropropan-2-yloxy)methylphosphonic acid (FPMPA)", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 51, 13 March 2008 (2008-03-13), pages 187 - 194, XP002487665 *
KIESEWETTER ET AL: "Labelling methods and radiosynthesis-Organic positron emitters; (P053) R AND S [18F]FPMPA: NUCLEOTIDE ANALOGUE REVERSE TRANSCRIPTASE INHIBITOR FOR BIODISTRIBUTION STUDIES", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS SUPPLEMENT: 17TH INTERNATIONAL SYMPOSIUM ON RADIOPHARMACEUTICAL SCIENCES, vol. 50, no. S1, 11 April 2007 (2007-04-11), XP002487635 *

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Publication number Publication date
WO2008134578A2 (fr) 2008-11-06

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