BR9912951A - Método de fabricação de nucleotìdoes de 1,3-oxatiolano - Google Patents

Método de fabricação de nucleotìdoes de 1,3-oxatiolano

Info

Publication number
BR9912951A
BR9912951A BR9912951-5A BR9912951A BR9912951A BR 9912951 A BR9912951 A BR 9912951A BR 9912951 A BR9912951 A BR 9912951A BR 9912951 A BR9912951 A BR 9912951A
Authority
BR
Brazil
Prior art keywords
oxathiolane
nucleotides
making
preparation
processes
Prior art date
Application number
BR9912951-5A
Other languages
English (en)
Other versions
BR9912951B1 (pt
Inventor
Dennis C Liotta
Merrick Almond
Darryl Cleary
Jose Soria
George R Painter
Marcos Sznaidman
Original Assignee
Triangle Pharmaceuticals Inc
Univ Emory
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 Triangle Pharmaceuticals Inc, Univ Emory filed Critical Triangle Pharmaceuticals Inc
Publication of BR9912951A publication Critical patent/BR9912951A/pt
Publication of BR9912951B1 publication Critical patent/BR9912951B1/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D327/00—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D327/02—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
    • C07D327/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • AIDS & HIV (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)

Abstract

<B>MéTODO DE FABRICAçãO DE NUCLEOTìDEOS DE 1, 3-OXATIOLANO<D> Processos para a preparação de nucleotídeos de 1, 3-oxatiolano são fornecidos, os quais incluem métodos eficientes para a preparação do ciclo de 1, 3 - oxatiolano e a subseq³ente condensação do 1, 3 - oxatiolano com uma base de piridina ou purina. Usando-se os processos descritos aqui, os compostos podem ser fornecidos como enantiómeros isolados.
BRPI9912951-5A 1998-08-12 1999-08-12 método de fabricação de nucleotìdeos de 1,3-oxatiolano. BR9912951B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US9621498P 1998-08-12 1998-08-12
US60/096.214 1998-08-12
US12284199P 1999-03-04 1999-03-04
US60/122.841 1999-03-04
PCT/US1999/018584 WO2000009494A1 (en) 1998-08-12 1999-08-12 Method of manufacture of 1,3-oxathiolane nucleosides

Publications (2)

Publication Number Publication Date
BR9912951A true BR9912951A (pt) 2001-10-02
BR9912951B1 BR9912951B1 (pt) 2012-01-10

Family

ID=26791450

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI9912951-5A BR9912951B1 (pt) 1998-08-12 1999-08-12 método de fabricação de nucleotìdeos de 1,3-oxatiolano.

Country Status (17)

Country Link
US (4) US6215004B1 (pt)
EP (4) EP1535921A1 (pt)
JP (4) JP4249393B2 (pt)
KR (3) KR101208429B1 (pt)
CN (1) CN1141305C (pt)
AT (2) ATE282034T1 (pt)
AU (2) AU771779B2 (pt)
BR (1) BR9912951B1 (pt)
CA (3) CA2340214C (pt)
DE (2) DE69924651D1 (pt)
ES (2) ES2537540T3 (pt)
HK (2) HK1038921A1 (pt)
IL (4) IL141359A0 (pt)
MX (1) MXPA01001552A (pt)
PT (2) PT2322518E (pt)
RU (2) RU2439069C2 (pt)
WO (1) WO2000009494A1 (pt)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5684164A (en) * 1988-04-11 1997-11-04 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
ES2537540T3 (es) * 1998-08-12 2015-06-09 Gilead Sciences, Inc. Método de fabricación de nucleósidos de 1,3-dioxolano y 1,3-oxatiolano
CA2308559C (en) 2000-05-16 2005-07-26 Brantford Chemicals Inc. 1,3-oxathiolan-5-ones useful in the production of antiviral nucleoside analogues
AU2008202336B2 (en) * 2001-03-01 2011-11-10 Abbvie Inc. Polymorphic and other crystalline forms of cis-FTC
CN102911166B (zh) * 2001-03-01 2016-08-17 基利得科学公司 顺-ftc的多晶型物及其它晶型
ATE313542T1 (de) * 2001-06-15 2006-01-15 Shire Biochem Inc Stereoselektives verfahren zur herstellung von nukleosidanaloga
CA2351049C (en) 2001-06-18 2007-03-13 Brantford Chemicals Inc. Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
CA2470202A1 (en) * 2001-12-14 2003-06-26 Kyoichi A. Watanabe Preparation of intermediates useful in the synthesis of antiviral nucleosides
DK1556371T3 (da) * 2002-07-19 2006-08-21 Winston Pharmaceuticals Llc Benzimidazol-derivater og deres anvendelse som prodrugs for protonpumpe-inhibitorer
ES2360096T3 (es) 2002-08-06 2011-05-31 Pharmasset, Inc. Procedimientos de preparación de nucleosidos de 1,3-dioxolano.
US20060246130A1 (en) 2003-01-14 2006-11-02 Dahl Terrence C Compositions and methods for combination antiviral therapy
EP1693482A4 (en) * 2003-12-09 2008-04-30 Asahi Glass Co Ltd TITANIUM OXIDE FILM HAVING PHOTOCATALYTIC ACTIVITY ON VISIBLE LIGHT IRRADIATION AND METHOD FOR PRODUCING THE SAME
CN105039489A (zh) * 2004-02-03 2015-11-11 埃莫里大学 制备1,3-二氧戊环核苷的方法
EP2086955A2 (en) * 2006-10-30 2009-08-12 Lupin Ltd. An improved process for the manufacture of cis(-)-lamivudine
US8318934B2 (en) * 2007-09-28 2012-11-27 Avexa Limited Process for chiral resolution of 2-substituted 4-substituted 1,3-oxathiolanes
EP2050757A1 (en) * 2007-10-10 2009-04-22 Cilag AG Method of producing 2' -deoxy-5-azacytidine (Decitabine)
EP2048151A1 (en) * 2007-10-10 2009-04-15 Cilag AG Method for producing nucleosides by direct glycosylation of the nucleoside base
WO2010055526A1 (en) * 2008-11-12 2010-05-20 Lupin Limited A novel polymorph of emtricitabine and a process for preparing of the same
US20110282046A1 (en) 2009-01-19 2011-11-17 Rama Shankar Process for preparation of cis-nucleoside derivative
EP2454244B1 (en) 2009-07-15 2013-06-26 Lupin Limited An improved process for preparation of efavirenz
WO2011141805A2 (en) 2010-05-14 2011-11-17 Lupin Limited An improved process for the manufacture of lamivudine
US20130296562A1 (en) 2011-08-05 2013-11-07 Lupin Limited Stereoselective process for preparation of 1,3-oxathiolane nucleosides
CN106478618A (zh) * 2016-10-14 2017-03-08 上海礼泰医药科技有限公司 恩曲他滨氢卤酸盐的制备方法
CN109553610B (zh) * 2018-12-21 2020-10-27 江西富祥药业股份有限公司 一种恩曲他滨异构体的制备方法
CN115043823A (zh) * 2022-06-28 2022-09-13 江苏普信制药有限公司 一种恩曲他滨的合成方法

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5041449A (en) 1988-04-11 1991-08-20 Iaf Biochem International, Inc. 4-(nucleoside base)-substituted-1,3-dioxolanes useful for treatment of retroviral infections
US5466806A (en) 1989-02-08 1995-11-14 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
US5047407A (en) 1989-02-08 1991-09-10 Iaf Biochem International, Inc. 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties
US5684164A (en) 1988-04-11 1997-11-04 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
NZ228645A (en) 1988-04-11 1991-09-25 Iaf Biochem Int 1,3-dioxolane derivatives substituted in the 5th position by a purine or pyrimidine radical; treatment of viral infections
US5700937A (en) 1990-02-01 1997-12-23 Emory University Method for the synthesis, compositions and use of 2'-deoxy-5-fluoro-3'-thiacytidine and related compounds
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US5276151A (en) * 1990-02-01 1994-01-04 Emory University Method of synthesis of 1,3-dioxolane nucleosides
US6642245B1 (en) 1990-02-01 2003-11-04 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
US6069252A (en) 1990-02-01 2000-05-30 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers
GB9009861D0 (en) 1990-05-02 1990-06-27 Glaxo Group Ltd Chemical compounds
US5587480A (en) 1990-11-13 1996-12-24 Biochem Pharma, Inc. Substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes with antiviral properties
WO1992010496A1 (en) * 1990-12-05 1992-06-25 University Of Georgia Research Foundation, Inc. ENANTIOMERICALLY PURE β-L-(-)-1,3-OXATHIOLANE NUCLEOSIDES
US5248776A (en) 1990-12-05 1993-09-28 University Of Georgia Research Foundation, Inc. Process for enantiomerically pure β-L-1,3-oxathiolane nucleosides
US5444063A (en) 1990-12-05 1995-08-22 Emory University Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity
IL100965A (en) 1991-02-22 1999-12-31 Univ Emory 2 - Hydroxymethyl - 5 -) 5 - Fluorocytocin - 1 - Eyal (- 1, 3 - Oxathiolane, its resolution and pharmaceuticals containing it
GB9104740D0 (en) 1991-03-06 1991-04-17 Wellcome Found Antiviral nucleoside combination
JP3479068B2 (ja) 1991-03-06 2003-12-15 エモリー・ユニバーシティ ５−フルオロ−２’−デオキシ−３’−チアシチジンのｂ型肝炎治療への使用
IT1244501B (it) 1991-03-22 1994-07-15 Sigma Tau Ind Farmaceuti Derivati amminoacilici e oligopeptidici dell'allopurinolo dotati di attivita' immunostimolante e composizioni farmaceutiche che li contengono
WO1992018517A1 (en) 1991-04-17 1992-10-29 Yale University Method of treating or preventing hepatitis b virus
GB9110874D0 (en) 1991-05-20 1991-07-10 Iaf Biochem Int Medicaments
ZA923641B (en) 1991-05-21 1993-02-24 Iaf Biochem Int Processes for the diastereoselective synthesis of nucleosides
GB9116601D0 (en) 1991-08-01 1991-09-18 Iaf Biochem Int 1,3-oxathiolane nucleoside analogues
GB9311709D0 (en) 1993-06-07 1993-07-21 Iaf Biochem Int Stereoselective synthesis of nucleoside analogues using bicycle intermediate
IL113432A (en) * 1994-04-23 2000-11-21 Glaxo Group Ltd Process for the diastereoselective synthesis of nucleoside analogues
CN1068894C (zh) 1994-07-08 2001-07-25 三井化学株式会社 热塑性聚酯树脂组合物
GB9506644D0 (en) 1995-03-31 1995-05-24 Wellcome Found Preparation of nucleoside analogues
GB9525606D0 (en) * 1995-12-14 1996-02-14 Iaf Biochem Int Method and compositions for the synthesis of dioxolane nucleosides with › - configuration
TW318283B (en) 1996-12-09 1997-10-21 United Microelectronics Corp Multi-level read only memory structure and manufacturing method thereof
ES2537540T3 (es) * 1998-08-12 2015-06-09 Gilead Sciences, Inc. Método de fabricación de nucleósidos de 1,3-dioxolano y 1,3-oxatiolano
US9308044B2 (en) 2002-04-08 2016-04-12 Medtronic Ardian Luxembourg S.A.R.L. Methods for therapeutic renal neuromodulation
US9109124B2 (en) 2011-06-01 2015-08-18 Xerox Corporation Solid ink compositions comprising semicrystalline oligomer resins
JP5800924B2 (ja) 2014-01-20 2015-10-28 ファナック株式会社 回転工具の回転振れ及び動バランス調整機構

Also Published As

Publication number Publication date
AU2004202930B2 (en) 2008-05-08
AU2004202930C1 (en) 2008-11-13
IL141359A (en) 2006-07-05
US6215004B1 (en) 2001-04-10
CA2340214A1 (en) 2000-02-24
US6939965B2 (en) 2005-09-06
KR100856416B1 (ko) 2008-09-04
KR100687194B1 (ko) 2007-02-27
US20030144532A1 (en) 2003-07-31
HK1156604A1 (en) 2012-06-15
IL141359A0 (en) 2002-03-10
DE69924651D1 (de) 2005-05-12
JP2014132026A (ja) 2014-07-17
JP2012176974A (ja) 2012-09-13
IL173745A0 (en) 2006-07-05
CA2714085C (en) 2013-02-05
CA2563022A1 (en) 2000-02-24
EP2322518B1 (en) 2015-02-25
PT1104415E (pt) 2005-03-31
WO2000009494A1 (en) 2000-02-24
EP1361223A1 (en) 2003-11-12
EP2322518A1 (en) 2011-05-18
ES2232169T3 (es) 2005-05-16
JP5547772B2 (ja) 2014-07-16
RU2439069C2 (ru) 2012-01-10
JP5203897B2 (ja) 2013-06-05
KR20010072428A (ko) 2001-07-31
RU2244712C2 (ru) 2005-01-20
JP4249393B2 (ja) 2009-04-02
DE69921829T2 (de) 2005-10-27
RU2004125183A (ru) 2006-01-27
JP2002522534A (ja) 2002-07-23
EP1104415B1 (en) 2004-11-10
CN1313858A (zh) 2001-09-19
CN1141305C (zh) 2004-03-10
EP1361223B1 (en) 2005-04-06
EP1104415A1 (en) 2001-06-06
PT2322518E (pt) 2015-06-08
AU771779B2 (en) 2004-04-01
CA2714085A1 (en) 2000-02-24
KR20070094667A (ko) 2007-09-20
IL173745A (en) 2010-05-31
IL201293A0 (en) 2010-05-31
KR101208429B1 (ko) 2012-12-05
US6576776B1 (en) 2003-06-10
US6518425B1 (en) 2003-02-11
ATE282034T1 (de) 2004-11-15
CA2340214C (en) 2007-10-30
IL201293A (en) 2011-02-28
BR9912951B1 (pt) 2012-01-10
AU5675299A (en) 2000-03-06
CA2563022C (en) 2010-11-23
AU2004202930A1 (en) 2004-07-29
ES2537540T3 (es) 2015-06-09
EP1535921A1 (en) 2005-06-01
MXPA01001552A (es) 2004-08-23
JP2009108080A (ja) 2009-05-21
DE69921829D1 (de) 2004-12-16
HK1038921A1 (en) 2002-04-04
JP5956492B2 (ja) 2016-07-27
KR20060063991A (ko) 2006-06-12
ATE292631T1 (de) 2005-04-15

Similar Documents

Publication Publication Date Title
IL173745A0 (en) Method of manufacture of 1,3-oxathiolane nucleosides
DK82093A (da) Fremgangsmaade til fremstilling af 6-chlor-7-iod-7-deazapuriner
DE122011100004I1 (de) Triazolo[4,5-D]pyrimidin-derivate.
MA26520A1 (fr) Derives de la 5h-thiazolo (3,2-a) pyrimidine.
DK1249281T3 (da) Selvrensende overflade med hydrofob overfladestruktur og fremgangsmåde til fremstilling af denne
TR199701647A3 (tr) Ikame edilmis purin türevleri,bunlarin imalat usulü
NO975293D0 (no) Fremgangsmåte for mottaking, samt mottaker
HUP0303590A3 (en) Method for the production of 4,6-diaminopyrimido[5,4-d]pyrimidines
DE68923171D1 (de) Aluminiumhydroxyd, verfahren zur herstellung und zusammensetzung.
ATE483691T1 (de) Verfahren zur herstellung von unsymmetrischen 4,6-bis(aryloxy)pyrimidin-derivaten
DE50003553D1 (de) Verfahren zur enantiomerentrennung von cis-8-benzyl-7,9-dioxo-2,8-diazabicyclo 4.3.0]nonan
DK1140933T3 (da) Fremgangsmåde til fremstilling af N6-substituerede deaza-adenosinderivater
DK1068209T3 (da) Fremgangsmåde til fremstilling af purinderivater og deres mellemprodukter
PT794177E (pt) Processo para a preparacao de compostos de 4,6-bis(ariloxi) pirimidina assimetricos
BR9607850A (pt) Processo para a preparação de um composto e composto
DE60335805D1 (de) Verfahren zur herstellung von 1,3-dioxolan-nucleosiden
ATE209636T1 (de) Verbessertes verfahren zur herstellung von unsymmetrischen 4,6- bis(aryloxy)pyrimidinverbindungen
DE69801454T2 (de) Verfahren zur Herstellung von 2-Methyl-1,4-Benzochinon
IT1292595B1 (it) Processo per la produzione della dexfenfluramina cloridrato.
DK1104415T3 (da) Fremgangsmåde til fremstilling af 1,3-oxathiolan-nukleosider
BR9702918A (pt) Processo de produção obtenção purificação e atividade antitumoralde 3-(1,2-dihidro-5-(5-hidroxi- 1H-indol-3-il)-2-oxo-3H-pirrol-3-ilideno)-1,3-dihidro-2H-i ndol-2-ona
IT1302010B1 (it) Processo per la preparazione di oxaprozina.
ES293286Y (es) Base-soporte, de apoyos orientables independientes
ES1033459Y (es) Criolla de adorno.
DE59709211D1 (de) Verfahren zur Herstellung von 4,6-Dihydroxypyrimidin

Legal Events

Date Code Title Description
B25A Requested transfer of rights approved

Owner name: EMORY UNIVERSITY (US) , GILEAD SCIENCES, INC. (US)

Free format text: TRANSFERIDO DE: TRIANGLE PHARMACEUTICALS, INC.

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 10/01/2012, OBSERVADAS AS CONDICOES LEGAIS.

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 21A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2595 DE 29-09-2020 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.