AR086492A1 - Procedimientos e intermediarios para preparar agentes anti-hiv - Google Patents

Procedimientos e intermediarios para preparar agentes anti-hiv

Info

Publication number
AR086492A1
AR086492A1 ARP120101777A ARP120101777A AR086492A1 AR 086492 A1 AR086492 A1 AR 086492A1 AR P120101777 A ARP120101777 A AR P120101777A AR P120101777 A ARP120101777 A AR P120101777A AR 086492 A1 AR086492 A1 AR 086492A1
Authority
AR
Argentina
Prior art keywords
aryl
alkyl
cycloalkyl
optionally substituted
independently
Prior art date
Application number
ARP120101777A
Other languages
English (en)
Original Assignee
Gilead Sciences Inc
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 filed Critical Gilead Sciences Inc
Publication of AR086492A1 publication Critical patent/AR086492A1/es

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Classifications

    • 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 System
    • 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, i.e. RP(=X)(XH)2 (X = S, 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 System
    • 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, i.e. RP(=X)(XH)2 (X = S, 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 System
    • 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, 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

Abstract

La presente proporciona procesos sintéticos e intermediarios sintéticos que se pueden usar para preparar compuestos que tienen propiedades anti-HIV útiles.Reivindicación 1: Un compuesto seleccionado del grupo de fórmulas (1), donde: Bn está opcionalmente sustituido con uno o más grupos seleccionados de alquilo C1-6 y -O-alquilo C1-6; cada R1 es independientemente -C(=O)alquilo C1-6, -C(=O)cicloalquilo C3-7 o -C(=O)arilo, donde -C(=O)cicloalquilo C3-7 o -C(=O)arilo está opcionalmente sustituido con uno o más grupos alquilo C1-6; cada R2 es independientemente arilo o alquilo C1-6, donde arilo está opcionalmente sustituido con uno o más grupos alquilo C1-6; R3 es I, R5Se o R5S; cada R4 es independientemente alquilo C1-6, cicloalquilo C3-7 o arilo, donde arilo o cicloalquilo C3-7 está opcionalmente sustituido con uno o más grupos alquilo C1-6; y cada R5 es independientemente alquilo C1-6, cicloalquilo C3-7 o arilo, donde arilo o cicloalquilo C3-7 está opcionalmente sustituido con uno o más grupos alquilo C1-6; y sus sales.
ARP120101777A 2011-05-19 2012-05-18 Procedimientos e intermediarios para preparar agentes anti-hiv AR086492A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161488133P 2011-05-19 2011-05-19

Publications (1)

Publication Number Publication Date
AR086492A1 true AR086492A1 (es) 2013-12-18

Family

ID=46208163

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120101777A AR086492A1 (es) 2011-05-19 2012-05-18 Procedimientos e intermediarios para preparar agentes anti-hiv

Country Status (10)

Country Link
US (5) US8987437B2 (es)
EP (3) EP3199537B1 (es)
JP (4) JP5951757B2 (es)
AR (1) AR086492A1 (es)
AU (4) AU2012255029B2 (es)
CA (1) CA2835932C (es)
ES (2) ES2700470T3 (es)
PT (2) PT2710019T (es)
TW (1) TWI635093B (es)
WO (1) WO2012159047A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2710019T (pt) 2011-05-19 2017-07-21 Gilead Sciences Inc Processos e intermediários para preparar agentes anti-hiv
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
EP3518935A1 (en) 2016-09-27 2019-08-07 Gilead Sciences, Inc. Therapeutic compositions for treatment of human immunodeficiency virus
ES2892402T3 (es) 2017-08-01 2022-02-04 Gilead Sciences Inc Formas cristalinas de ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il)oxi)metil)(fenoxi)fosforil)-L-alaninato de etilo para tratar infecciones virales
CN111788204B (zh) 2018-02-26 2023-05-05 吉利德科学公司 作为hbv复制抑制剂的取代吡咯嗪化合物
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
JP7022970B1 (ja) 2021-06-09 2022-02-21 株式会社エクセノヤマミズ 船舶

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
AP1466A (en) 2000-07-21 2005-09-22 Gilead Sciences Inc Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same.
CA2481285A1 (en) 2002-04-26 2003-11-06 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors
WO2004096286A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Antiviral phosphonate analogs
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
ATE516293T1 (de) * 2004-07-16 2011-07-15 Gilead Sciences Inc Antivirale verbindungen
DK2258376T3 (en) * 2004-07-27 2019-04-15 Gilead Sciences Inc Phosphonate analogues of HIV inhibitor compounds
CA2616314A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
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
EP2307435B1 (en) 2008-07-08 2012-06-13 Gilead Sciences, Inc. Salts of hiv inhibitor compounds
US9790252B2 (en) * 2009-07-01 2017-10-17 Cornell University 2-fluorinated riboses and arabinoses and methods of use and synthesis
PT2710019T (pt) 2011-05-19 2017-07-21 Gilead Sciences Inc Processos e intermediários para preparar agentes anti-hiv

Also Published As

Publication number Publication date
ES2700470T3 (es) 2019-02-15
EP2710019B1 (en) 2017-05-03
US10196419B2 (en) 2019-02-05
US20180079773A1 (en) 2018-03-22
US20120296076A1 (en) 2012-11-22
JP2016128459A (ja) 2016-07-14
US20150203525A1 (en) 2015-07-23
EP3199537B1 (en) 2018-10-17
NZ618939A (en) 2015-11-27
AU2012255029B2 (en) 2016-04-28
AU2016208292A1 (en) 2016-08-11
ES2629913T3 (es) 2017-08-16
CA2835932A1 (en) 2012-11-22
JP6282295B2 (ja) 2018-02-21
JP6621772B2 (ja) 2019-12-18
PT2710019T (pt) 2017-07-21
EP3450438A1 (en) 2019-03-06
EP3199537A1 (en) 2017-08-02
US9783567B2 (en) 2017-10-10
US20160340379A1 (en) 2016-11-24
EP2710019A1 (en) 2014-03-26
JP2019089808A (ja) 2019-06-13
AU2019226278A1 (en) 2019-09-26
PT3199537T (pt) 2019-01-17
US8987437B2 (en) 2015-03-24
AU2018200776A1 (en) 2018-02-22
CA2835932C (en) 2020-03-24
WO2012159047A1 (en) 2012-11-22
US20190359644A1 (en) 2019-11-28
AU2012255029A1 (en) 2013-05-02
TWI635093B (zh) 2018-09-11
JP2014516968A (ja) 2014-07-17
JP5951757B2 (ja) 2016-07-13
US9296779B2 (en) 2016-03-29
AU2016208292B2 (en) 2018-02-22
JP2017110025A (ja) 2017-06-22
TW201309715A (zh) 2013-03-01
AU2018200776B2 (en) 2019-10-03

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