AU2012255029B2 - Processes and intermediates for preparing anti-HIV agents - Google Patents

Processes and intermediates for preparing anti-HIV agents Download PDF

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Publication number
AU2012255029B2
AU2012255029B2 AU2012255029A AU2012255029A AU2012255029B2 AU 2012255029 B2 AU2012255029 B2 AU 2012255029B2 AU 2012255029 A AU2012255029 A AU 2012255029A AU 2012255029 A AU2012255029 A AU 2012255029A AU 2012255029 B2 AU2012255029 B2 AU 2012255029B2
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Australia
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compound
formula
salt
alkyl
pho
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AU2012255029A
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AU2012255029A1 (en
Inventor
Brandon Heath BROWN
Benjamin R. Graetz
Kenneth M. Kent
Steven Pfeiffer
Richard P. Polniaszek
Keiko Sujino
Duong Duc-Phi TRAN
Alan Scott TRIMAN
Richard Hung Chiu Yu
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Gilead Sciences Inc
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Gilead Sciences Inc
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Publication of AU2012255029A1 publication Critical patent/AU2012255029A1/en
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Priority to AU2016208292A priority Critical patent/AU2016208292B2/en
Assigned to GILEAD SCIENCES, INC. reassignment GILEAD SCIENCES, INC. Amend patent request/document other than specification (104) Assignors: ALAN SCOTT TRIMAN, BENJAMIN R. GRAETZ, BRANDON HEATH BROWN, DUONG DUC-PHI TRAN, GILEAD SCIENCES, INC., KEIKO SUJINO, KENNETH M. KENT, RICHARD HUNG CHIU YU, RICHARD P. POLNIASZEK, STEVEN PFEIFFER
Priority to AU2018200776A priority patent/AU2018200776B2/en
Priority to AU2019226278A priority patent/AU2019226278A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4075—Esters with hydroxyalkyl compounds
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/44—Amides thereof
    • C07F9/4434—Amides thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4449—Esters with hydroxyaryl compounds
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/173—Purine radicals with 2-deoxyribosyl as the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
AU2012255029A 2011-05-19 2012-05-18 Processes and intermediates for preparing anti-HIV agents Active AU2012255029B2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU2016208292A AU2016208292B2 (en) 2011-05-19 2016-07-26 Processes and intermediates for preparing anti-HIV agents
AU2018200776A AU2018200776B2 (en) 2011-05-19 2018-02-01 Processes and intermediates for preparing anti-HIV agents
AU2019226278A AU2019226278A1 (en) 2011-05-19 2019-09-09 Processes and intermediates for preparing anti-hiv agents

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161488133P 2011-05-19 2011-05-19
US61/488,133 2011-05-19
PCT/US2012/038615 WO2012159047A1 (en) 2011-05-19 2012-05-18 Processes and intermediates for preparing anti-hiv agents

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2016208292A Division AU2016208292B2 (en) 2011-05-19 2016-07-26 Processes and intermediates for preparing anti-HIV agents

Publications (2)

Publication Number Publication Date
AU2012255029A1 AU2012255029A1 (en) 2013-05-02
AU2012255029B2 true AU2012255029B2 (en) 2016-04-28

Family

ID=46208163

Family Applications (4)

Application Number Title Priority Date Filing Date
AU2012255029A Active AU2012255029B2 (en) 2011-05-19 2012-05-18 Processes and intermediates for preparing anti-HIV agents
AU2016208292A Active AU2016208292B2 (en) 2011-05-19 2016-07-26 Processes and intermediates for preparing anti-HIV agents
AU2018200776A Active AU2018200776B2 (en) 2011-05-19 2018-02-01 Processes and intermediates for preparing anti-HIV agents
AU2019226278A Abandoned AU2019226278A1 (en) 2011-05-19 2019-09-09 Processes and intermediates for preparing anti-hiv agents

Family Applications After (3)

Application Number Title Priority Date Filing Date
AU2016208292A Active AU2016208292B2 (en) 2011-05-19 2016-07-26 Processes and intermediates for preparing anti-HIV agents
AU2018200776A Active AU2018200776B2 (en) 2011-05-19 2018-02-01 Processes and intermediates for preparing anti-HIV agents
AU2019226278A Abandoned AU2019226278A1 (en) 2011-05-19 2019-09-09 Processes and intermediates for preparing anti-hiv agents

Country Status (10)

Country Link
US (5) US8987437B2 (enExample)
EP (3) EP3199537B1 (enExample)
JP (4) JP5951757B2 (enExample)
AR (1) AR086492A1 (enExample)
AU (4) AU2012255029B2 (enExample)
CA (1) CA2835932C (enExample)
ES (2) ES2629913T3 (enExample)
PT (2) PT2710019T (enExample)
TW (1) TWI635093B (enExample)
WO (1) WO2012159047A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3199537B1 (en) 2011-05-19 2018-10-17 Gilead Sciences, Inc. Processes and intermediates for preparing anti-hiv agents
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
US20180085387A1 (en) 2016-09-27 2018-03-29 Gilead Sciences, Inc. Therapeutic compositions for treatment of human immunodeficiency virus
PT3661937T (pt) 2017-08-01 2021-09-24 Gilead Sciences Inc Formas cristalinas de ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-il)-4-fluoro-2,5-dihidrofurano-2-il)oxi)metil)(fenoxi)fosforil)-l-alaninato de etil (gs-9131) para tratamento de infeções virais
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ， インコーポレイテッド Ｈｂｖ複製阻害剤としての置換ピロリジン化合物
CN114409706B (zh) * 2019-07-01 2023-11-28 上海医药工业研究院 一种苯基氢膦酸酯及其中间体的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050009043A1 (en) * 2000-07-21 2005-01-13 Gilead Sciences, Inc. Prodrugs of phosphonate nucleotide analogues
WO2007014352A2 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
WO2010005986A1 (en) * 2008-07-08 2010-01-14 Gilead Sciences, Inc. Salts of hiv inhibitor compounds

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US599431A (en) 1898-02-22 Clothes-wringer
GB835785A (en) * 1956-04-30 1960-05-25 Victor Chemical Works Method of making diaryl phosphites
MX3898E (es) * 1975-12-29 1981-09-10 Monsanto Co Procedimiento mejorado para la preparacion de triesteres de n-fosfonometilglicina
US4198355A (en) * 1977-03-28 1980-04-15 Mobil Oil Corporation Preparation of tertiary alkylphosphorodichloridite derivatives
US5459256A (en) * 1987-04-17 1995-10-17 The Government Of The United States Of America As Represented By The Department Of Health And Human Services Lipophilic, aminohydrolase-activated prodrugs
HU906976D0 (en) 1989-11-13 1991-05-28 Bristol Myers Squibb Co Process for producing 2', 3'-didesoxy-2'-fluoarabinonucleoside analogues
US5672697A (en) * 1991-02-08 1997-09-30 Gilead Sciences, Inc. Nucleoside 5'-methylene phosphonates
TW200408645A (en) 2002-04-26 2004-06-01 Gilead Sciences Inc Non nucleoside reverse transcriptase inhibitors
JP2010535701A (ja) * 2003-04-25 2010-11-25 ギリアード サイエンシーズ， インコーポレイテッド 抗癌ホスホネートアナログ
SG182849A1 (en) 2003-04-25 2012-08-30 Gilead Sciences Inc Antiviral phosphonate analogs
KR20070034119A (ko) * 2004-07-16 2007-03-27 길리애드 사이언시즈, 인코포레이티드 항바이러스 화합물
PT2258376T (pt) 2004-07-27 2019-05-31 Gilead Sciences Inc Análogos fosfonatados de compostos inibidores do vih
CA2644961A1 (en) * 2006-03-17 2007-09-27 Invista Technologies S.A.R.L. Method for the purification of triorganophosphites by treatment with a basic additive
WO2008100447A2 (en) 2007-02-09 2008-08-21 Gilead Sciences, Inc. Nucleoside analogs for antiviral treatment
US9790252B2 (en) * 2009-07-01 2017-10-17 Cornell University 2-fluorinated riboses and arabinoses and methods of use and synthesis
EP3199537B1 (en) 2011-05-19 2018-10-17 Gilead Sciences, Inc. Processes and intermediates for preparing anti-hiv agents

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050009043A1 (en) * 2000-07-21 2005-01-13 Gilead Sciences, Inc. Prodrugs of phosphonate nucleotide analogues
WO2007014352A2 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
WO2010005986A1 (en) * 2008-07-08 2010-01-14 Gilead Sciences, Inc. Salts of hiv inhibitor compounds

Also Published As

Publication number Publication date
US20180079773A1 (en) 2018-03-22
PT2710019T (pt) 2017-07-21
US20160340379A1 (en) 2016-11-24
JP6621772B2 (ja) 2019-12-18
US10196419B2 (en) 2019-02-05
AU2019226278A1 (en) 2019-09-26
AU2016208292B2 (en) 2018-02-22
JP6282295B2 (ja) 2018-02-21
JP2016128459A (ja) 2016-07-14
AR086492A1 (es) 2013-12-18
US9783567B2 (en) 2017-10-10
US20190359644A1 (en) 2019-11-28
EP2710019B1 (en) 2017-05-03
JP2019089808A (ja) 2019-06-13
TWI635093B (zh) 2018-09-11
AU2012255029A1 (en) 2013-05-02
US20150203525A1 (en) 2015-07-23
ES2700470T3 (es) 2019-02-15
AU2016208292A1 (en) 2016-08-11
JP2017110025A (ja) 2017-06-22
EP3199537B1 (en) 2018-10-17
WO2012159047A1 (en) 2012-11-22
JP2014516968A (ja) 2014-07-17
EP2710019A1 (en) 2014-03-26
TW201309715A (zh) 2013-03-01
JP5951757B2 (ja) 2016-07-13
US8987437B2 (en) 2015-03-24
US9296779B2 (en) 2016-03-29
EP3450438A1 (en) 2019-03-06
US20120296076A1 (en) 2012-11-22
AU2018200776B2 (en) 2019-10-03
EP3199537A1 (en) 2017-08-02
ES2629913T3 (es) 2017-08-16
CA2835932C (en) 2020-03-24
AU2018200776A1 (en) 2018-02-22
CA2835932A1 (en) 2012-11-22
PT3199537T (pt) 2019-01-17
NZ618939A (en) 2015-11-27

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DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE APPLICANT TO READ GILEAD SCIENCES, INC. .

FGA Letters patent sealed or granted (standard patent)
HB Alteration of name in register

Owner name: GILEAD SCIENCES, INC.

Free format text: FORMER NAME(S): KENNETH M. KENT; ALAN SCOTT TRIMAN; DUONG DUC-PHI TRAN; BENJAMIN R. GRAETZ; STEVEN PFEIFFER; BRANDON HEATH BROWN; RICHARD P. POLNIASZEK; RICHARD HUNG CHIU YU; GILEAD SCIENCES, INC.; KEIKO SUJINO