ES2629913T3 - Procesos e intermediarios para la preparación de agentes anti-VIH - Google Patents

Procesos e intermediarios para la preparación de agentes anti-VIH Download PDF

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Publication number
ES2629913T3
ES2629913T3 ES12725570.1T ES12725570T ES2629913T3 ES 2629913 T3 ES2629913 T3 ES 2629913T3 ES 12725570 T ES12725570 T ES 12725570T ES 2629913 T3 ES2629913 T3 ES 2629913T3
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Spain
Prior art keywords
compound
formula
aryl
alkyl
salt
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Application number
ES12725570.1T
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English (en)
Spanish (es)
Inventor
Richard Hung Chiu Yu
Brandon Heath BROWN
Richard P. Polniaszek
Benjamin R. Graetz
Keiko Sujino
Duong Duc-Phi TRAN
Alan Scott TRIMAN
Kenneth M. Kent
Steven Pfeiffer
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Gilead Sciences Inc
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Gilead Sciences Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/20Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4071Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4075Esters with hydroxyalkyl compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/44Amides thereof
    • C07F9/4434Amides thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4449Esters with hydroxyaryl compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • C07F9/65616Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/173Purine radicals with 2-deoxyribosyl as the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus 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)
ES12725570.1T 2011-05-19 2012-05-18 Procesos e intermediarios para la preparación de agentes anti-VIH Active ES2629913T3 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
ES2629913T3 true ES2629913T3 (es) 2017-08-16

Family

ID=46208163

Family Applications (2)

Application Number Title Priority Date Filing Date
ES12725570.1T Active ES2629913T3 (es) 2011-05-19 2012-05-18 Procesos e intermediarios para la preparación de agentes anti-VIH
ES16204289T Active ES2700470T3 (es) 2011-05-19 2012-05-18 Procesos e intermediarios para la preparación de agentes anti-VIH

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES16204289T Active ES2700470T3 (es) 2011-05-19 2012-05-18 Procesos e intermediarios para la preparación de agentes anti-VIH

Country Status (10)

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

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR086492A1 (es) 2011-05-19 2013-12-18 Gilead Sciences Inc Procedimientos e intermediarios para preparar agentes anti-hiv
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
AU2019223182B2 (en) 2018-02-26 2021-08-19 Gilead Sciences, Inc. Substituted pyrrolizine compounds as HBV replication inhibitors
CN112175003B (zh) * 2019-07-01 2022-02-15 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

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
NZ536942A (en) 2000-07-21 2006-03-31 Gilead Sciences Inc Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
JP4942915B2 (ja) 2002-04-26 2012-05-30 ギリアード サイエンシーズ, インコーポレイテッド Hivプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積
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
PT1628685E (pt) 2003-04-25 2011-03-16 Gilead Sciences Inc Análogos de fosfonatos antivirais
US20080311077A1 (en) * 2004-07-16 2008-12-18 Kleem Chaudhary Antiviral Compounds
BRPI0512690A (pt) 2004-07-27 2007-11-27 Gilead Sciences Inc análogos de fosfonato de compostos inibidores de hiv
AU2006272521A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of HIV
CN101405292A (zh) * 2006-03-17 2009-04-08 因温斯特技术公司 通过用碱性添加剂处理提纯亚磷酸三有机酯的方法
WO2008100447A2 (en) 2007-02-09 2008-08-21 Gilead Sciences, Inc. Nucleoside analogs for antiviral treatment
PT2307435E (pt) 2008-07-08 2012-09-19 Gilead Sciences Inc Sais de compostos inibidores de vih
US9790252B2 (en) * 2009-07-01 2017-10-17 Cornell University 2-fluorinated riboses and arabinoses and methods of use and synthesis
AR086492A1 (es) 2011-05-19 2013-12-18 Gilead Sciences Inc Procedimientos e intermediarios para preparar agentes anti-hiv

Also Published As

Publication number Publication date
US20180079773A1 (en) 2018-03-22
AU2012255029A1 (en) 2013-05-02
US9296779B2 (en) 2016-03-29
TWI635093B (zh) 2018-09-11
US9783567B2 (en) 2017-10-10
PT3199537T (pt) 2019-01-17
EP2710019B1 (en) 2017-05-03
EP3450438A1 (en) 2019-03-06
US20160340379A1 (en) 2016-11-24
TW201309715A (zh) 2013-03-01
JP6282295B2 (ja) 2018-02-21
AU2018200776B2 (en) 2019-10-03
US20120296076A1 (en) 2012-11-22
JP6621772B2 (ja) 2019-12-18
JP2016128459A (ja) 2016-07-14
EP3199537A1 (en) 2017-08-02
JP2017110025A (ja) 2017-06-22
CA2835932A1 (en) 2012-11-22
EP2710019A1 (en) 2014-03-26
US10196419B2 (en) 2019-02-05
JP2019089808A (ja) 2019-06-13
EP3199537B1 (en) 2018-10-17
NZ618939A (en) 2015-11-27
AU2016208292A1 (en) 2016-08-11
US8987437B2 (en) 2015-03-24
PT2710019T (pt) 2017-07-21
ES2700470T3 (es) 2019-02-15
AU2012255029B2 (en) 2016-04-28
JP5951757B2 (ja) 2016-07-13
CA2835932C (en) 2020-03-24
AU2016208292B2 (en) 2018-02-22
AU2019226278A1 (en) 2019-09-26
AU2018200776A1 (en) 2018-02-22
US20190359644A1 (en) 2019-11-28
US20150203525A1 (en) 2015-07-23
WO2012159047A1 (en) 2012-11-22
JP2014516968A (ja) 2014-07-17
AR086492A1 (es) 2013-12-18

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