WO2002008241A3 - Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same - Google Patents

Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same Download PDF

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Publication number
WO2002008241A3
WO2002008241A3 PCT/US2001/023104 US0123104W WO0208241A3 WO 2002008241 A3 WO2002008241 A3 WO 2002008241A3 US 0123104 W US0123104 W US 0123104W WO 0208241 A3 WO0208241 A3 WO 0208241A3
Authority
WO
WIPO (PCT)
Prior art keywords
prodrugs
nucleotide analogues
selecting
methods
compounds
Prior art date
Application number
PCT/US2001/023104
Other languages
French (fr)
Other versions
WO2002008241A2 (en
Inventor
Mark W Becker
Harlan H Chapman
Tomas Cihlar
Eugene J Eisenberg
Gong-Xin He
Michael R Kernan
William A Lee
Ernest J Prisbe
John C Rohloff
Mark L Sparacino
Original Assignee
Gilead Sciences Inc
Mark W Becker
Harlan H Chapman
Tomas Cihlar
Eugene J Eisenberg
Gong-Xin He
Michael R Kernan
William A Lee
Ernest J Prisbe
John C Rohloff
Mark L Sparacino
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22821718&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2002008241(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to ES01961695T priority Critical patent/ES2536972T5/en
Priority to AU2001282941A priority patent/AU2001282941C1/en
Priority to NZ523438A priority patent/NZ523438A/en
Application filed by Gilead Sciences Inc, Mark W Becker, Harlan H Chapman, Tomas Cihlar, Eugene J Eisenberg, Gong-Xin He, Michael R Kernan, William A Lee, Ernest J Prisbe, John C Rohloff, Mark L Sparacino filed Critical Gilead Sciences Inc
Priority to HU0301307A priority patent/HU230960B1/en
Priority to HRP20160074AA priority patent/HRP20160074B1/en
Priority to KR1020067020061A priority patent/KR100749160B1/en
Priority to EP01961695.2A priority patent/EP1301519B2/en
Priority to DK01961695.2T priority patent/DK1301519T4/en
Priority to IL15365801A priority patent/IL153658A0/en
Priority to JP2002514146A priority patent/JP4651264B2/en
Priority to AU8294101A priority patent/AU8294101A/en
Priority to CNB018131611A priority patent/CN1291994C/en
Priority to MXPA03000587A priority patent/MXPA03000587A/en
Priority to KR1020037000872A priority patent/KR100767432B1/en
Priority to CA2416757A priority patent/CA2416757C/en
Priority to UA2003021482A priority patent/UA75889C2/en
Priority to EA200300188A priority patent/EA004926B1/en
Priority to EEP200300029A priority patent/EE05366B1/en
Priority to US10/333,107 priority patent/US20040018150A1/en
Priority to BR0112646A priority patent/BRPI0112646B8/en
Priority to SI200131040T priority patent/SI1301519T1/en
Priority to APAP/P/2003/002724A priority patent/AP1466A/en
Publication of WO2002008241A2 publication Critical patent/WO2002008241A2/en
Publication of WO2002008241A3 publication Critical patent/WO2002008241A3/en
Priority to ZA2002/10271A priority patent/ZA200210271B/en
Priority to IS6689A priority patent/IS2985B/en
Priority to NO20030270A priority patent/NO336718B1/en
Priority to HRP20030047AA priority patent/HRP20030047B1/en
Priority to BG107572A priority patent/BG66037B1/en
Priority to HK03105871.0A priority patent/HK1054238A1/en
Priority to AU2005225039A priority patent/AU2005225039B2/en
Priority to NO20120466A priority patent/NO20120466L/en
Priority to NO20131717A priority patent/NO20131717L/en
Priority to NO20150909A priority patent/NO20150909L/en
Priority to LTPA2016009C priority patent/LTC1301519I2/en
Priority to BE2016C018C priority patent/BE2016C018I2/fr
Priority to FR16C0013C priority patent/FR16C0013I2/en
Priority to CY2016008C priority patent/CY2016008I2/en
Priority to LU93029C priority patent/LU93029I2/en
Priority to NO2016006C priority patent/NO2016006I1/en
Priority to NL300803C priority patent/NL300803I2/nl
Priority to HUS1900027C priority patent/HUS000494I2/en
Priority to NO2023006C priority patent/NO2023006I1/en

Links

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
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/70—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving virus or bacteriophage
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • 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
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/02—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving viable microorganisms
    • C12Q1/18—Testing for antimicrobial activity of a material
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity

Abstract

A novel method is provided for screening prodrugs of methoxyphosphonate nucleotide analogues to identify prodrugs selectively targeting desired tissues with antiviral or antitumor activity. This method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided. Also provided is an improved method for the use of magnesium alkoxide for the preparation of starting materials and compounds for use herein.
PCT/US2001/023104 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same WO2002008241A2 (en)

Priority Applications (41)

Application Number Priority Date Filing Date Title
CNB018131611A CN1291994C (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
SI200131040T SI1301519T1 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
NZ523438A NZ523438A (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
AU2001282941A AU2001282941C1 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
HU0301307A HU230960B1 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and compositions thereof
HRP20160074AA HRP20160074B1 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
KR1020067020061A KR100749160B1 (en) 2000-07-21 2001-07-20 Methods for making prodrugs of phosphonate nucleotide analogues
EP01961695.2A EP1301519B2 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
DK01961695.2T DK1301519T4 (en) 2000-07-21 2001-07-20 PRODUCTS OF PHOSPHONATE NUCLEOTIDE ANALOGS AND METHODS OF SELECTION AND PREPARATION
IL15365801A IL153658A0 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
BR0112646A BRPI0112646B8 (en) 2000-07-21 2001-07-20 prodrugs of phosphonate nucleotide analogues and compositions comprising them
AU8294101A AU8294101A (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
APAP/P/2003/002724A AP1466A (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same.
MXPA03000587A MXPA03000587A (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same.
KR1020037000872A KR100767432B1 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
CA2416757A CA2416757C (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
UA2003021482A UA75889C2 (en) 2000-07-21 2001-07-20 Phosphonatnucleotide analogs prodrugs, a method for selection and preparation thereof
EA200300188A EA004926B1 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues, method for method for screening to identify thereof, method for anti-viral therapy or prophylaxis
EEP200300029A EE05366B1 (en) 2000-07-21 2001-07-20 Prodrugs and Screening Methods for Phosphonate Nucleotide Analogs
US10/333,107 US20040018150A1 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
JP2002514146A JP4651264B2 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogs and methods for selecting and making them.
ES01961695T ES2536972T5 (en) 2000-07-21 2001-07-20 Phosphonate nucleotide analog prodrugs and methods for selecting and preparing the same
ZA2002/10271A ZA200210271B (en) 2000-07-21 2002-12-19 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
IS6689A IS2985B (en) 2000-07-21 2003-01-17 Phosphonate-nucleotide analogues and methods for selecting and generating them
NO20030270A NO336718B1 (en) 2000-07-21 2003-01-20 Prodrugs of phosphonate nucleotide analogues, their preparation and its use in the therapeutic and prophylactic treatment of viral infections
HRP20030047AA HRP20030047B1 (en) 2000-07-21 2003-01-24 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
BG107572A BG66037B1 (en) 2000-07-21 2003-02-19 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
HK03105871.0A HK1054238A1 (en) 2000-07-21 2003-08-15 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
AU2005225039A AU2005225039B2 (en) 2000-07-21 2005-10-18 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
NO20120466A NO20120466L (en) 2000-07-21 2012-04-23 Prodrugs of Phosphonate Nucleotide Analogs, and Methods for Selecting and Preparing Them
NO20131717A NO20131717L (en) 2000-07-21 2013-12-20 Prodrugs of Phosphonate Nucleotide Analogs, and Methods for Selecting and Preparing Them
NO20150909A NO20150909L (en) 2000-07-21 2015-07-10 Prodrugs of Phosphonate Nucleotide Analogs, and Methods for Selecting and Preparing Them
LTPA2016009C LTC1301519I2 (en) 2000-07-21 2016-04-05 Prodrugs of nucleotide phosphonate analogues and methods for their selection and preparation
BE2016C018C BE2016C018I2 (en) 2000-07-21 2016-04-07
FR16C0013C FR16C0013I2 (en) 2000-07-21 2016-04-11 PRODRUGS BASED ON NUCLEOTIDE ANALOGUES OF PHOSPHONATE AND METHODS FOR THE SELECTION AND PREPARATION THEREOF
CY2016008C CY2016008I2 (en) 2000-07-21 2016-04-12 PRODRUGS OF NUCLEOTIDE PHOSPHONIC ANALOGUES AND METHODS FOR THEIR SELECTION AND PREPARATION
LU93029C LU93029I2 (en) 2000-07-21 2016-04-14 ALAFENAMIDE TENOFOVIR OR SALT OR SOLVATE THEREOF, IN PARTICULAR ALFENAMIDE FUMARATE TENOFOVIR
NO2016006C NO2016006I1 (en) 2000-07-21 2016-04-19 Prodrugs of phosphonate nucleotide analogues, their preparation and its use in the therapeutic and prophylactic treatment of viral infections
NL300803C NL300803I2 (en) 2000-07-21 2016-04-22
HUS1900027C HUS000494I2 (en) 2000-07-21 2019-05-09 Tenofovir alafenamide or a salt thereof, in particular tenofovir alafenamide fumarate
NO2023006C NO2023006I1 (en) 2000-07-21 2023-02-03 Tenofovir alafenamide or a salt or solvate thereof, especially tenofovir alafenamide fumarate - extension

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22002100P 2000-07-21 2000-07-21
US60/220,021 2000-07-21

Publications (2)

Publication Number Publication Date
WO2002008241A2 WO2002008241A2 (en) 2002-01-31
WO2002008241A3 true WO2002008241A3 (en) 2002-08-29

Family

ID=22821718

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/023104 WO2002008241A2 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same

Country Status (37)

Country Link
US (10) US20040018150A1 (en)
EP (3) EP2682397B1 (en)
JP (4) JP4651264B2 (en)
KR (2) KR100767432B1 (en)
CN (2) CN1291994C (en)
AP (1) AP1466A (en)
AU (3) AU2001282941C1 (en)
BE (1) BE2016C018I2 (en)
BG (1) BG66037B1 (en)
BR (1) BRPI0112646B8 (en)
CA (3) CA2893174A1 (en)
CY (2) CY2016008I2 (en)
CZ (2) CZ304734B6 (en)
DK (2) DK1301519T4 (en)
EA (1) EA004926B1 (en)
EE (1) EE05366B1 (en)
ES (2) ES2627903T3 (en)
FR (1) FR16C0013I2 (en)
HK (2) HK1054238A1 (en)
HR (2) HRP20160074B1 (en)
HU (2) HU230960B1 (en)
IL (1) IL153658A0 (en)
IS (1) IS2985B (en)
LT (2) LT2682397T (en)
LU (1) LU93029I2 (en)
MX (1) MXPA03000587A (en)
NL (1) NL300803I2 (en)
NO (6) NO336718B1 (en)
NZ (3) NZ535408A (en)
OA (1) OA12393A (en)
PL (1) PL213214B1 (en)
PT (2) PT1301519E (en)
SI (2) SI2682397T1 (en)
TR (1) TR200300055T2 (en)
UA (1) UA75889C2 (en)
WO (1) WO2002008241A2 (en)
ZA (1) ZA200210271B (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8871785B2 (en) 2003-04-25 2014-10-28 Gilead Sciences, Inc. Antiviral phosphonate analogs
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV
US9579332B2 (en) 2004-07-27 2017-02-28 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds
US9585906B2 (en) 2007-03-30 2017-03-07 Gilead Pharmasset Llc Nucleoside phosphoramidate prodrugs
US11845755B2 (en) 2022-03-02 2023-12-19 Gilead Sciences, Inc. Compounds and methods for treatment of viral infections

Families Citing this family (211)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1291994C (en) * 2000-07-21 2006-12-27 吉里德科学公司 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
US7388002B2 (en) * 2001-11-14 2008-06-17 Biocryst Pharmaceuticals, Inc. Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
MXPA04004621A (en) * 2001-11-14 2004-09-10 Biocryst Pharm Inc Nucleosides preparation thereof and use as inhibitors of rna viral polymerases.
DE60315023T2 (en) * 2002-04-26 2008-04-03 Gilead Sciences, Inc., Foster City ENRICHMENT IN THE CELL TO PHOSPHONATE ANALOGUE OF HIV PROTEASE INHIBITOR COMPOUNDS AND THE COMPOUNDS OF ITSELF
US20050239054A1 (en) * 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
JP4476811B2 (en) 2002-05-13 2010-06-09 メタバシス・セラピューティクス・インコーポレイテッド New phosphonic acid prodrugs of PMEA and its analogs
EP1583542B9 (en) * 2003-01-14 2008-10-22 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
WO2004096285A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7427636B2 (en) 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
CA2522845A1 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
US7452901B2 (en) * 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
CN101410120A (en) * 2003-04-25 2009-04-15 吉里德科学公司 Anti-inflammatory phosphonate compounds
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
WO2005002626A2 (en) * 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
WO2005042773A1 (en) * 2003-10-24 2005-05-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
WO2005044279A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
WO2005044308A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
CA2548753A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. 4-substituted carbovir and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity
BRPI0418031A (en) * 2003-12-22 2007-04-17 Gilead Sciences Inc phosphonate-substituted kinase inhibitors
US20050153990A1 (en) * 2003-12-22 2005-07-14 Watkins William J. Phosphonate substituted kinase inhibitors
AU2004312546B2 (en) * 2003-12-30 2010-10-14 Gilead Sciences, Inc. Phosphonates, monophosphonamidates, bisphosphonamidates for the treatment of viral diseases
US20050239753A1 (en) * 2004-01-21 2005-10-27 Gilead Sciences, Inc. Methods of inhibition of MMTV-like viruses
US8432394B1 (en) 2004-05-14 2013-04-30 Nvidia Corporation Method and system for implementing clamped z value interpolation in a raster stage of a graphics pipeline
US8416242B1 (en) 2004-05-14 2013-04-09 Nvidia Corporation Method and system for interpolating level-of-detail in graphics processors
US8411105B1 (en) 2004-05-14 2013-04-02 Nvidia Corporation Method and system for computing pixel parameters
US7079156B1 (en) 2004-05-14 2006-07-18 Nvidia Corporation Method and system for implementing multiple high precision and low precision interpolators for a graphics pipeline
RU2006138907A (en) 2004-06-08 2008-07-20 Метабазис Терапеутикс SYNTHESIS OF COMPLEX CYCLIC ETHERS USING LEWIS ACID
US20070003608A1 (en) * 2005-04-08 2007-01-04 Almond Merrick R Compounds, compositions and methods for the treatment of viral infections and other medical disorders
WO2006110655A2 (en) 2005-04-08 2006-10-19 Chimerix, Inc. Compounds, compositions and methods for the treatment of poxvirus infections
CN100359315C (en) * 2005-05-26 2008-01-02 林维宣 Animal remedy residual ability verification sample and method for preparing same
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
TWI471145B (en) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc Unitary pharmaceutical dosage form
US8076303B2 (en) 2005-12-13 2011-12-13 Spring Bank Pharmaceuticals, Inc. Nucleotide and oligonucleotide prodrugs
CN100396689C (en) * 2006-03-07 2008-06-25 中国医学科学院医药生物技术研究所 Tenoforv monoester compounds with HIV-1/HBV virus copying inhibiting activity
EP2020996B1 (en) 2006-05-16 2011-11-23 Gilead Sciences, Inc. Method and compositions for treating hematological malignancies
EP2046792B1 (en) 2006-07-12 2015-02-25 Mylan Laboratories Limited Process for the preparation of tenofovir
US20080261913A1 (en) * 2006-12-28 2008-10-23 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of liver disorders
WO2009038851A2 (en) * 2007-06-26 2009-03-26 University Of Wyoming Research Corporation D/B/A Western Research Institute Treatment and prevention systems for acid mine drainage and halogenated contaminants
US8441497B1 (en) * 2007-08-07 2013-05-14 Nvidia Corporation Interpolation of vertex attributes in a graphics processor
CN101977610B (en) * 2008-01-25 2012-05-16 奇默里克斯公司 Methods of treating viral infections
TWI444384B (en) 2008-02-20 2014-07-11 Gilead Sciences Inc Nucleotide analogues and their use in the treatment of malignancies
JP5757860B2 (en) * 2008-04-25 2015-08-05 シプラ・リミテッド Crystalline form of tenofovir disoproxil and process for producing the same
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
CN102177172A (en) * 2008-07-02 2011-09-07 埃迪尼克斯医药公司 Compounds and pharmaceutical compositions for the treatment of viral infections
US8658617B2 (en) 2008-07-08 2014-02-25 Gilead Sciences, Inc. Salts of HIV inhibitor compounds
CA2748057C (en) 2008-12-23 2018-07-03 Pharmasset, Inc. Nucleoside phosphoramidates
NZ617066A (en) 2008-12-23 2015-02-27 Gilead Pharmasset Llc Nucleoside analogs
EP2671888A1 (en) 2008-12-23 2013-12-11 Gilead Pharmasset LLC 3',5'-cyclic nucleoside phosphate analogues
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI576352B (en) 2009-05-20 2017-04-01 基利法瑪席特有限責任公司 Nucleoside phosphoramidates
US8614200B2 (en) 2009-07-21 2013-12-24 Chimerix, Inc. Compounds, compositions and methods for treating ocular conditions
MX2012003126A (en) 2009-09-21 2012-06-19 Gilead Sciences Inc Processes and intermediates for the preparation of 1'-substituted carba-nucleoside analogs.
PT2534150T (en) 2010-02-12 2017-05-02 Chimerix Inc Methods of treating viral infection
PL3290428T3 (en) 2010-03-31 2022-02-07 Gilead Pharmasset Llc Tablet comprising crystalline (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin-1 (2h)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate
CL2011000716A1 (en) 2010-03-31 2012-04-20 Gilead Pharmasset Llc Crystalline forms 1 6 of (s) -isopropyl-2 - (((s) - (((2r.3r.4r.5r) -5- (2,4-dioxo-3,4-dihydropyrimidin-1 (2h) -yl) -4-fluoro-3-hydroxy-4-methyl tetrahydrofuran-2-yl) methoxy) (phenoxy) phosphoryl) amino) propanoate; pharmaceutical composition and combination; and its use to treat a hepatitis c virus infection.
JP2013523765A (en) 2010-04-01 2013-06-17 イデニク プハルマセウティカルス，インコーポレイテッド Compounds and pharmaceutical compositions for the treatment of viral infections
WO2011139709A2 (en) 2010-04-26 2011-11-10 Chimerix, Inc. Methods of treating retroviral infections and related dosage regimes
JP5937073B2 (en) * 2010-07-19 2016-06-22 ギリード・サイエンシズ・インコーポレーテッド Process for the preparation of diastereomeric pure phosphoramidate prodrugs
SI2595980T1 (en) 2010-07-22 2014-11-28 Gilead Sciences, Inc. Methods and compounds for treating paramyxoviridae virus infections
AU2011336632B2 (en) 2010-11-30 2015-09-03 Gilead Pharmasset Llc Compounds
KR101880724B1 (en) 2010-12-10 2018-08-17 시그마팜 래보러토리즈, 엘엘씨 Highly stable compositions of orally active nucleotide analogues or orally active nucleotide analogue prodrugs
ZA201103820B (en) 2010-12-13 2012-01-25 Laurus Labs Private Ltd Process for the preparation of tenofovir
CN103842369A (en) 2011-03-31 2014-06-04 埃迪尼克斯医药公司 Compounds and pharmaceutical compositions for the treatment of viral infections
WO2012154698A2 (en) * 2011-05-06 2012-11-15 Mckenna Charles E Method to improve antiviral activity of nucleotide analogue drugs
JP5951757B2 (en) * 2011-05-19 2016-07-13 ギリアード サイエンシーズ， インコーポレイテッド Processes and intermediates for preparing anti-HIV agents
AU2014271320B2 (en) * 2011-08-16 2017-02-23 Gilead Sciences, Inc. Tenofovir alafenamide hemifumarate
UA115311C2 (en) * 2011-08-16 2017-10-25 Гіліад Сайєнсіз, Інк. Tenofovir alafenamide hemifumarate
AU2016228317B2 (en) * 2011-10-07 2018-07-19 Gilead Sciences, Inc. Methods for preparing anti-viral nucleotide analogs
CN113264959A (en) 2011-10-07 2021-08-17 吉利德科学公司 Process for preparing antiviral nucleotide analogs
AU2014215976B2 (en) * 2011-10-07 2016-06-30 Gilead Sciences, Inc. Methods for preparing anti-viral nucleotide analogs
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
WO2013095684A1 (en) 2011-12-22 2013-06-27 Geron Corporation Guanine analogs as telomerase substrates and telomere length affectors
MX2014009172A (en) * 2012-02-03 2014-08-27 Gilead Sciences Inc Combination therapy comprising tenofovir alafenamide hemifumarate and cobicistat for use in the treatment of viral infections.
AU2012327170A1 (en) 2012-02-03 2013-08-22 Gilead Sciences, Inc. Therapeutic compounds
CN103665043B (en) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 A kind of tenofovir prodrug and its application in medicine
GB201215696D0 (en) * 2012-09-03 2012-10-17 Ithemba Pharmaceuticals Pty Ltd A process for the preparation of (R)-9-[2-(Phosphonometh-Oxy)propyl]adenine (PMPA)
WO2014068265A1 (en) * 2012-10-29 2014-05-08 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
CN102899327B (en) * 2012-11-06 2014-06-11 清华大学深圳研究生院 Antiviral small nucleic acid and temperature-sensitive type gel preparation and application thereof
CA2891009A1 (en) * 2012-11-16 2014-05-22 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
CN103848868B (en) * 2012-12-04 2017-04-12 蚌埠丰原涂山制药有限公司 method for preparing tenofovir
CN103848869B (en) * 2012-12-04 2016-12-21 上海医药工业研究院 The method preparing tenofovir
MY172166A (en) 2013-01-31 2019-11-15 Gilead Pharmasset Llc Combination formulation of two antiviral compounds
CN104072539B (en) * 2013-03-25 2017-03-29 安徽贝克联合制药有限公司 Double (4 acetaminophenol epoxide) esters of tenofovir and preparation method thereof and its application
JP6262848B2 (en) * 2013-05-21 2018-01-17 成都先導薬物開発有限公司 How to capture drug targets
CA2914381A1 (en) 2013-06-07 2014-12-11 Cipla Limited An efficient process for separation of diastereomers of 9-[(r)-2-[[(r,s)-[[(s)-1-(isopropoxycarbonyl)ethyl]amino]-phenoxyphosphinyl] methoxy]propyl]adenine
EP4005560A1 (en) 2013-08-27 2022-06-01 Gilead Pharmasset LLC Combination formulation of two antiviral compounds
WO2015040640A2 (en) * 2013-09-20 2015-03-26 Laurus Labs Private Limited An improved process for the preparation of tenofovir alafenamide or pharmaceutically acceptable salts thereof
EP2860185A1 (en) 2013-10-09 2015-04-15 Zentiva, k.s. An improved process for the preparation of Tenofovir disoproxil and pharmaceutically acceptable salts thereof
IN2013CH05455A (en) * 2013-11-27 2015-08-07 Laurus Labs Private Ltd
WO2015107451A2 (en) 2014-01-14 2015-07-23 Mylan Laboratories Ltd. Purification of tenofovir alafenamide and its intermediates
TWI660965B (en) * 2014-01-15 2019-06-01 美商基利科學股份有限公司 Solid forms of tenofovir
CN104804042B (en) * 2014-01-24 2018-01-19 齐鲁制药有限公司 Phosphonate-nucleotide ester class compound, its pharmaceutical composition, Preparation method and use
WO2015120057A1 (en) 2014-02-05 2015-08-13 Gilead Sciences, Inc. Pharmaceutical combinations against co-infection with hiv and tuberculosis
CN114404427A (en) 2014-02-13 2022-04-29 配体药物公司 Prodrug compound and use thereof
CN105814068B (en) * 2014-02-27 2017-08-04 四川海思科制药有限公司 A kind of substituted phosphoramidic acid ester derivative, its preparation method and its application
CN105001262B (en) * 2014-04-18 2017-09-01 四川海思科制药有限公司 The phosphonaminate of aryl substitution and its application medically
CN105531281B (en) * 2014-04-21 2017-12-15 四川海思科制药有限公司 A kind of preparation method of nucleoside analog and its intermediate
CN105085571A (en) * 2014-05-20 2015-11-25 四川海思科制药有限公司 Tenofovir alafenamide compound, preparation method and purpose thereof
CN105518012B (en) * 2014-06-25 2018-03-02 四川海思科制药有限公司 A kind of substituted amino acid sulfur ester, its composition and application
CN106687118A (en) 2014-07-02 2017-05-17 配体药物公司 Prodrug compounds and uses thereof
CN106687467A (en) * 2014-09-30 2017-05-17 韩美精密化学株式会社 Method for preparing high-purity (r)-9-[2-(phosphonomethoxy)propyl]adenine
KR101703258B1 (en) 2014-12-30 2017-02-06 한미정밀화학주식회사 Preparation method for (r)-9-[2-(phosphonomethoxy)propyl]adenine with high purity
KR101703257B1 (en) 2014-09-30 2017-02-06 한미정밀화학주식회사 Preparation method for (r)-9-[2-(phosphonomethoxy)propyl]adenine with high purity
WO2016057866A1 (en) 2014-10-09 2016-04-14 Board Of Regents Of The University Of Nebraska Compositions and methods for the delivery of therapeutics
TWI740546B (en) 2014-10-29 2021-09-21 美商基利科學股份有限公司 Methods for the preparation of ribosides
CN108191913A (en) * 2014-11-12 2018-06-22 四川海思科制药有限公司 A kind of tenofovir Chinese mugwort draws phenol amine crystal form a and preparation method thereof
CN104558036A (en) * 2014-12-11 2015-04-29 杭州和泽医药科技有限公司 Tenofovir alafenamide hemi-fumarate crystal form and preparation method thereof
WO2016108205A1 (en) 2015-01-03 2016-07-07 Mylan Laboratories Limited Processes for the preparation of amorphous tenofovir alafenamide hemifumarate and a premix thereof
WO2016187160A1 (en) * 2015-05-16 2016-11-24 Godx, Inc. Point of need testing device and methods of use thereof
CN106188139B (en) * 2015-05-29 2020-02-18 江苏天士力帝益药业有限公司 Tenofovir monobenzyl phosphoric acid amide prodrug, preparation method and application thereof
CZ2015384A3 (en) 2015-06-05 2016-12-14 Zentiva, K.S. Tenofovir alafenamide solid forms
AU2016277859B2 (en) * 2015-06-17 2019-08-01 Gilead Sciences, Inc. Co-crystals, salts and solid forms of tenofovir alafenamide
KR102121329B1 (en) 2015-06-30 2020-06-17 길리애드 사이언시즈, 인코포레이티드 Pharmaceutical formulations containing tenofovir and emtricitabine
WO2017027434A1 (en) 2015-08-10 2017-02-16 Merck Sharp & Dohme Corp. Antiviral beta-amino acid ester phosphodiamide compounds
TWI616452B (en) * 2015-08-26 2018-03-01 Preparation method of nucleoside analog and intermediate thereof
TWI620754B (en) * 2015-08-26 2018-04-11 Method for preparing amino phosphate derivative and preparation method thereof
TWI616453B (en) * 2015-08-27 2018-03-01 Substituted amino acid thioester compounds, materials and uses thereof
WO2017037608A1 (en) * 2015-08-28 2017-03-09 Laurus Labs Private Limited Solid forms of tenofovir alafenamide and salts thereof, processes for its preparation and pharmaceutical compositions thereof
WO2017049060A1 (en) 2015-09-16 2017-03-23 Gilead Sciences, Inc. Methods for treating arenaviridae and coronaviridae virus infections
EP3632415A1 (en) 2015-11-09 2020-04-08 Gilead Sciences, Inc. Therapeutic compositions for treatment of human immunodeficiency virus
CN106800573B (en) * 2015-11-25 2020-03-10 四川海思科制药有限公司 Nucleotide phosphonate monohydrate, preparation method and medical application thereof
US10745428B2 (en) 2015-12-10 2020-08-18 Idenix Pharmaceuticals Llc Antiviral phosphodiamide prodrugs of tenofovir
CN106866737B (en) * 2015-12-11 2020-11-20 南京圣和药物研发有限公司 Phosphonic acid derivatives and their use
EP3390413B1 (en) 2015-12-15 2020-08-19 Merck Sharp & Dohme Corp. Antiviral oxime phosphoramide compounds
WO2017118928A1 (en) 2016-01-06 2017-07-13 Lupin Limited Process for the separation of diastereomers of tenofovir alafenamide
WO2017134089A1 (en) 2016-02-02 2017-08-10 Sandoz Ag Crystalline forms of tenofovir alafenamide monofumarate
WO2017133517A1 (en) * 2016-02-03 2017-08-10 四川海思科制药有限公司 Phosphamide derivative, method for manufacturing the same, and uses thereof
CN108350007B (en) * 2016-03-01 2020-04-10 深圳市塔吉瑞生物医药有限公司 Substituted adenine compound and pharmaceutical composition thereof
CN107179355B (en) * 2016-03-11 2021-08-10 广东东阳光药业有限公司 Method for separating and detecting tenofovir alafenamide and related substances thereof
CZ2016156A3 (en) 2016-03-17 2017-09-27 Zentiva, K.S. The method of preparation of diastereomerically pure Tenofovir Alafenamide or its salts
CN107226826A (en) * 2016-03-25 2017-10-03 江苏奥赛康药业股份有限公司 Tenofovir Chinese mugwort draws phenol amine fumarate compound and its pharmaceutical composition
WO2017211325A1 (en) * 2016-06-05 2017-12-14 上海诚妙医药科技有限公司 New crystal form of tenofovir alafenamide salt, preparation method and use thereof
CN107698621A (en) * 2016-06-20 2018-02-16 杭州和泽医药科技有限公司 A kind of phosphonate prodrugs of adenine derivative and its application in medicine
WO2017221189A1 (en) * 2016-06-22 2017-12-28 Laurus Labs Limited An improved process for the preparation of tenofovir alafenamide or pharmaceutically acceptable salts thereof
CN106317116A (en) * 2016-08-19 2017-01-11 张红利 Phosphamide nucleosides compound, pharmaceutically acceptable salt and application thereof, and pharmaceutical composition
WO2018039157A1 (en) 2016-08-25 2018-03-01 Merck Sharp & Dohme Corp. Antiviral prodrugs of tenofovir
CN106380484A (en) * 2016-08-29 2017-02-08 杭州百诚医药科技股份有限公司 New crystal form of tenofovir alafenamide and preparation method thereof
WO2018042331A1 (en) 2016-08-31 2018-03-08 Glaxosmithkline Intellectual Property (No.2) Limited Combinations and uses and treatments thereof
WO2018051250A1 (en) 2016-09-14 2018-03-22 Viiv Healthcare Company Combination comprising tenofovir alafenamide, bictegravir and 3tc
EP3532069A4 (en) 2016-10-26 2020-05-13 Merck Sharp & Dohme Corp. Antiviral aryl-amide phosphodiamide compounds
CN106565785B (en) * 2016-11-09 2019-11-12 周雨恬 One kind having the active nucleoside phosphoramidate class compound of Anti-HBV activity/HIV and its salt and purposes
CN108129514A (en) * 2016-12-01 2018-06-08 北京美倍他药物研究有限公司 The individual isomer and its medical usage of phosphoric acid/phosphonate derivative
JP6938637B2 (en) 2016-12-22 2021-09-22 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Tenofovir antiviral aliphatic ester prodrug
CA3046029A1 (en) * 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Antiviral benzyl-amine phosphodiamide compounds
WO2018115046A1 (en) 2016-12-23 2018-06-28 Sandoz Ag Crystalline solid forms of tenofovir alafenamide
TWI784370B (en) 2017-01-31 2022-11-21 美商基利科學股份有限公司 Crystalline forms of tenofovir alafenamide
WO2018153977A1 (en) 2017-02-24 2018-08-30 Hexal Ag Stable composition of tenofovir alafenamide
RU2647576C1 (en) * 2017-02-28 2018-03-16 Васильевич Иващенко Александр Cyclobutyl (s)-2-[[[r)-2-(6-aminopurin-9-yl)-1-methyl-etoxy]methyl-phenoxy-phosphoryl]amino]-propanoates, method of their production and application
RU2659388C1 (en) 2017-02-28 2018-07-02 Васильевич Иващенко Александр Nucleotides including n-[(s)-1-cyclobutoxycarbonyl]phosphoramidate fragment, their analogs and their application
CN106866739B (en) * 2017-03-10 2018-11-02 华东师范大学 The preparation method of one kind (R) -1- (6- amino -9H- purine -9- bases) 2- phenyl esters
EP4331677A2 (en) 2017-03-14 2024-03-06 Gilead Sciences, Inc. Methods of treating feline coronavirus infections
EP3600332B1 (en) 2017-03-20 2023-12-13 The United States of America, as represented by the Secretary, Department of Health and Human Services Hiv post-exposure prophylaxis
CN108794530A (en) * 2017-04-26 2018-11-13 上海医药工业研究院 A kind of the third phenol of tenofovir amidic-salt crystal form and its preparation method and application
EP3618929B1 (en) 2017-05-01 2022-12-07 Gilead Sciences, Inc. A crystalline form of (s) 2 ethylbutyl 2 (((s) (((2r,3s,4r,5r) 5 (4 aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2 yl)methoxy)(phenoxy) phosphoryl)amino)propanoate
KR102379965B1 (en) * 2017-05-19 2022-03-29 주식회사 종근당 Efficient preparation method of Tenofovir
CN107266499B (en) * 2017-06-05 2019-07-02 珠海优润医药科技有限公司 A kind of antiviral compound and preparation method thereof
US20200113919A1 (en) 2017-06-30 2020-04-16 Cipla Limited Pharmaceutical Compositions
US10675296B2 (en) 2017-07-11 2020-06-09 Gilead Sciences, Inc. Compositions comprising an RNA polymerase inhibitor and cyclodextrin for treating viral infections
WO2019021319A1 (en) 2017-07-27 2019-01-31 Cipla Limited Pharmaceutical compositions
EP3960740B1 (en) 2017-08-01 2023-11-15 Gilead Sciences, Inc. Crystalline forms of ethyl ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-l-alaninate (gs-9131) vanillate for treating viral infections
AR112412A1 (en) 2017-08-17 2019-10-23 Gilead Sciences Inc CHOLINE SALT FORMS OF AN HIV CAPSID INHIBITOR
CN107655987B (en) * 2017-09-08 2020-11-03 厦门蔚扬药业有限公司 HPLC detection method for tenofovir alafenamide and isomer thereof
CN107522743A (en) * 2017-09-30 2017-12-29 深圳科兴生物工程有限公司 A kind of half fumaric acid tenofovir Chinese mugwort draws phenol amine industrial continuous producing method
WO2019084020A1 (en) 2017-10-24 2019-05-02 Gilead Sciences, Inc. Methods of treating patients co-infected with a virus and tuberculosis
CN109942632B (en) * 2017-12-20 2021-08-31 上海博志研新药物研究有限公司 Preparation method of tenofovir alafenamide intermediate
CN109942633B (en) * 2017-12-20 2021-08-31 上海新礼泰药业有限公司 Preparation method of tenofovir alafenamide intermediate
US20200407382A1 (en) 2017-12-30 2020-12-31 Cipla Limited Polymorphic forms of (9-[(r)-2-[[(s)-[[(s)-1-(isopropoxycarbonyl)ethyl]amino]phenoxy phosphinyl]methoxy]propyl] adenine and pharmaceutically acceptable salts thereof
AU2019207626B2 (en) * 2018-01-10 2023-10-05 Nucorion Pharmaceuticals, Inc. Phosphor(n)amidatacetal and phosph(on)atalcetal compounds
US11839623B2 (en) * 2018-01-12 2023-12-12 Board Of Regents Of The University Of Nebraska Antiviral prodrugs and formulations thereof
KR102587510B1 (en) 2018-02-15 2023-10-11 길리애드 사이언시즈, 인코포레이티드 Pyridine derivatives and their use for treating HIV infection
KR102587504B1 (en) 2018-02-16 2023-10-11 길리애드 사이언시즈, 인코포레이티드 Methods and intermediates for preparing therapeutic compounds useful for the treatment of retroviridae virus infections
CN108101943B (en) * 2018-02-28 2020-11-24 顾世海 Tenofovir prodrug or pharmaceutically acceptable salt and application thereof in medicine
US11458136B2 (en) 2018-04-09 2022-10-04 Board Of Regents Of The University Of Nebraska Antiviral prodrugs and formulations thereof
CA3216031A1 (en) 2018-07-16 2020-01-23 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
EP3823629A4 (en) 2018-07-19 2022-05-04 Merck Sharp & Dohme Corp. Phosphinic amide prodrugs of tenofovir
AU2019344929B2 (en) 2018-09-19 2023-03-30 Gilead Sciences, Inc. Integrase inhibitors for the prevention of HIV
US20220257619A1 (en) 2019-07-18 2022-08-18 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
WO2021015818A1 (en) 2019-07-19 2021-01-28 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Hiv pre-exposure prophylaxis
US20220296619A1 (en) 2019-08-19 2022-09-22 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
KR20220083673A (en) * 2019-08-22 2022-06-20 에모리 유니버시티 Nucleoside prodrugs and uses related thereto
US20220372171A1 (en) * 2019-09-20 2022-11-24 Abbott Rapid Diagnostics International Unlimited Company Antibody directed against tenofovir and derivatives thereof
WO2021108544A1 (en) 2019-11-26 2021-06-03 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
TW202313067A (en) 2020-01-27 2023-04-01 美商基利科學股份有限公司 Methods for treating sars cov-2 infections
WO2021165995A1 (en) 2020-02-20 2021-08-26 Cipla Limited Novel salts and/or co-crystals of tenofovir alafenamide
CA3169340A1 (en) 2020-03-12 2021-09-16 Pavel R. Badalov Methods of preparing 1'-cyano nucleosides
AU2021237718B2 (en) 2020-03-20 2023-09-21 Gilead Sciences, Inc. Prodrugs of 4'-C-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
WO2021202669A2 (en) 2020-04-01 2021-10-07 Reyoung Corporation Nucleoside and nucleotide conjugate compounds and uses thereof
KR20220164784A (en) 2020-04-06 2022-12-13 길리애드 사이언시즈, 인코포레이티드 Inhalation Formulations of 1′-Cyano Substituted Carbanucleoside Analogues
KR20210125298A (en) 2020-04-08 2021-10-18 주식회사 파마코스텍 New process for the preparation of Tenofovir alafenamide hemi-tartrate
CN115605492A (en) 2020-04-21 2023-01-13 配体制药股份有限公司（Us） Nucleotide prodrug compounds
US20210393653A1 (en) 2020-05-29 2021-12-23 Gilead Sciences, Inc. Remdesivir treatment methods
BR112022026321A2 (en) 2020-06-24 2023-01-17 Gilead Sciences Inc 1'-CYAN NUCLEOSIDE ANALOGS AND USES THEREOF
CN115996925A (en) 2020-06-25 2023-04-21 吉利德科学公司 Capsid inhibitors for the treatment of HIV
CN113970612B (en) * 2020-07-22 2023-08-01 北京四环制药有限公司 Method for measuring related substances of propiophenone tenofovir by high performance liquid chromatography
JP2023540225A (en) 2020-08-27 2023-09-22 ギリアード サイエンシーズ， インコーポレイテッド Compounds and methods for the treatment of viral infections
CN112336695B (en) * 2020-09-28 2023-01-03 华北制药华坤河北生物技术有限公司 Propofol fumarate and tenofovir tablet, preparation method thereof and detection method of related substances
JP2023549188A (en) 2020-11-11 2023-11-22 ギリアード サイエンシーズ， インコーポレイテッド Method for identifying HIV patients susceptible to treatment with gp120 CD4 binding site-directed antibodies
US11667656B2 (en) 2021-01-27 2023-06-06 Apotex Inc. Crystalline forms of Tenofovir alafenamide
CN113214322B (en) * 2021-04-30 2022-10-25 山东立新制药有限公司 Green and environment-friendly preparation method of tenofovir
WO2022251594A1 (en) * 2021-05-27 2022-12-01 Antios Therapeutics, Inc. Pharmacokinetics and dose-related improvments in subjects treated with phosphoramidate clevudine prodrugs
WO2023102523A1 (en) 2021-12-03 2023-06-08 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
US20230203071A1 (en) 2021-12-03 2023-06-29 Zhimin Du Therapeutic compounds for hiv virus infection
TW202337439A (en) 2021-12-03 2023-10-01 美商基利科學股份有限公司 Therapeutic compounds for hiv virus infection
CN114369120A (en) * 2022-01-28 2022-04-19 石家庄龙泽制药股份有限公司 Preparation method of key intermediate of prophenoltenofovir
TW202400172A (en) 2022-04-06 2024-01-01 美商基利科學股份有限公司 Bridged tricyclic carbamoylpyridone compounds and uses thereof
US20240034724A1 (en) 2022-07-01 2024-02-01 Gilead Sciences, Inc. Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection
WO2024044477A1 (en) 2022-08-26 2024-02-29 Gilead Sciences, Inc. Dosing and scheduling regimen for broadly neutralizing antibodies

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0481214A1 (en) * 1990-09-14 1992-04-22 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
WO1996037503A1 (en) * 1995-05-26 1996-11-28 Genta Incorporated Compositions and methods for the synthesis of organophosphorus derivatives
US5977089A (en) * 1996-07-26 1999-11-02 Gilead Sciences, Inc. Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CS233665B1 (en) 1983-01-06 1985-03-14 Antonin Holy Processing of isomere o-phosphonylmethylderivative of anantiomere racemic vicinal diene
CS263951B1 (en) 1985-04-25 1989-05-12 Antonin Holy 9-(phosponylmethoxyalkyl)adenines and method of their preparation
CS263952B1 (en) 1985-04-25 1989-05-12 Holy Antonin Remedy with antiviral effect
CS264222B1 (en) 1986-07-18 1989-06-13 Holy Antonin N-phosphonylmethoxyalkylderivatives of bases of pytimidine and purine and method of use them
US5650510A (en) 1986-11-18 1997-07-22 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiviral phosphonomethoxyalkylene purine and pyrimidine derivatives
US5057301A (en) 1988-04-06 1991-10-15 Neorx Corporation Modified cellular substrates used as linkers for increased cell retention of diagnostic and therapeutic agents
US5053215A (en) * 1988-05-26 1991-10-01 University Of Florida NMR-assayable ligand-labelled trifluorothymidine containing composition and method for diagnosis of HSV infection
US5744600A (en) 1988-11-14 1998-04-28 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Phosphonomethoxy carbocyclic nucleosides and nucleotides
US5688778A (en) 1989-05-15 1997-11-18 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Nucleoside analogs
JP2648516B2 (en) 1989-07-27 1997-09-03 ダイセル化学工業株式会社 Separation of stereoisomers
US5624898A (en) * 1989-12-05 1997-04-29 Ramsey Foundation Method for administering neurologic agents to the brain
JP2925753B2 (en) 1990-02-23 1999-07-28 ダイセル化学工業株式会社 Optical isomer separation method
US5302585A (en) 1990-04-20 1994-04-12 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Use of chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents
PT97407B (en) * 1990-04-20 1998-08-31 Rega Stichting METHOD FOR THE PREPARATION OF (R) -9- {2- (PHOSPHO-METHOXY) -PROPYL} -GUANINE
SK280313B6 (en) 1990-04-24 1999-11-08 �Stav Organick� Chemie A Biochemie Av �R N-(3-fluoro-2-phosphonylmethoxypropyl) derivatives of purine and pyrimidine heterocyclic bases, process for their preparation and their use
US5627165A (en) * 1990-06-13 1997-05-06 Drug Innovation & Design, Inc. Phosphorous prodrugs and therapeutic delivery systems using same
US5177064A (en) 1990-07-13 1993-01-05 University Of Florida Targeted drug delivery via phosphonate derivatives
CS387190A3 (en) 1990-08-06 1992-03-18 Ustav Organicke Chemie A Bioch (2r)-2-/di(2-propyl)phosphonylmethoxy/-3-p-toluenesulfonyloxy -1- trimethylacetoxypropane and process for preparing thereof
DE69132276T2 (en) 1990-08-10 2001-03-01 Acad Of Science Czech Republic METHOD FOR PRODUCING NUCLEOTIDES
US5827819A (en) * 1990-11-01 1998-10-27 Oregon Health Sciences University Covalent polar lipid conjugates with neurologically active compounds for targeting
US5208221A (en) * 1990-11-29 1993-05-04 Bristol-Myers Squibb Company Antiviral (phosphonomethoxy) methoxy purine/pyrimidine derivatives
CZ284678B6 (en) 1991-05-20 1999-01-13 Ústav Organické Chemie A Biochemie Avčr Di(2-propyl)esters of 1-fluoro-2-phosphonomethoxy-3-p-toluenesulfonyloxypropanes, process of their preparation and use
US5498752A (en) 1991-08-22 1996-03-12 Daicel Chemical Industries, Ltd. Process for recovering optical isomers and solvent, process for using solvent by circulation and process for reusing optical isomers in optical resolution
JP3010816B2 (en) 1991-08-22 2000-02-21 ダイセル化学工業株式会社 Method for recovering optical isomer and solvent in optical resolution, method for recycling solvent, and method for reusing optical isomer
EP0630381B1 (en) 1991-10-11 1997-04-09 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiviral acyclic phosphonomethoxyalkyl substituted, alkenyl and alkynyl purine and pyrimidine derivatives
US6057305A (en) 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
IL106998A0 (en) * 1992-09-17 1993-12-28 Univ Florida Brain-enhanced delivery of neuroactive peptides by sequential metabolism
US6413949B1 (en) * 1995-06-07 2002-07-02 D-Pharm, Ltd. Prodrugs with enhanced penetration into cells
US5798340A (en) * 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
KR100386685B1 (en) * 1993-09-17 2003-12-31 길리애드 사이언시즈, 인코포레이티드 Nucleotide Homolog
JP4086314B2 (en) 1993-09-17 2008-05-14 ギリアード サイエンシーズ， インコーポレイテッド Nucleotide analogs
US5656745A (en) * 1993-09-17 1997-08-12 Gilead Sciences, Inc. Nucleotide analogs
GB9505025D0 (en) 1995-03-13 1995-05-03 Medical Res Council Chemical compounds
US5977061A (en) 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
AU1427097A (en) 1995-12-29 1997-07-28 Gilead Sciences, Inc. Nucleotide analogs
US5717095A (en) * 1995-12-29 1998-02-10 Gilead Sciences, Inc. Nucleotide analogs
US5874577A (en) * 1996-04-03 1999-02-23 Medichem Research, Inc. Method for the preparing 9-12-(Diethoxyphosphonomethoxy)ethyl!adenine and analogues thereof
JP4033494B2 (en) * 1996-07-26 2008-01-16 ギリヤド サイエンシーズ， インコーポレイテッド Nucleotide analogs
US5739314A (en) 1997-04-25 1998-04-14 Hybridon, Inc. Method for synthesizing 2'-O-substituted pyrimidine nucleosides
US5935946A (en) 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
JP4173202B2 (en) * 1997-07-25 2008-10-29 ギリアード サイエンシーズ，インコーポレイテッド Nucleotide analog compositions and synthesis methods
AU747163B2 (en) 1997-07-25 2002-05-09 Gilead Sciences, Inc. Nucleotide analog compositions
WO1999030727A1 (en) * 1997-12-17 1999-06-24 Enzon, Inc. Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents
CN1192102C (en) * 1998-01-23 2005-03-09 新生物生物公司 Enzyme catalyzed therapeutic agents
US6169078B1 (en) * 1998-05-12 2001-01-02 University Of Florida Materials and methods for the intracellular delivery of substances
JP2002518521A (en) * 1998-06-20 2002-06-25 ワシントン・ユニバーシティ Membrane permeable peptide complexes for medical image analysis, diagnosis and therapy
US6169879B1 (en) * 1998-09-16 2001-01-02 Webtv Networks, Inc. System and method of interconnecting and using components of home entertainment system
GB9821058D0 (en) † 1998-09-28 1998-11-18 Univ Cardiff Chemical compound
TWI230618B (en) * 1998-12-15 2005-04-11 Gilead Sciences Inc Pharmaceutical compositions of 9-[2-[[bis[(pivaloyloxy)methyl]phosphono]methoxy]ethyl]adenine and tablets or capsules containing the same
HUP0105476A3 (en) † 1999-02-12 2002-08-28 Univ Cardiff Phosphoramidate, and mono-, di-, and tri-phosphate esters of (1r, cis)-4-(6-amino-9h-purin-9-yl)-2-cyclopentene-1-methanol as antiviral agents, process for preparation of the compounds and pharmaceutical compositions containing the same
CN1291994C (en) * 2000-07-21 2006-12-27 吉里德科学公司 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
US6960648B2 (en) * 2000-10-13 2005-11-01 Universite De Lausanne Intracellular delivery of biological effectors
US20020119433A1 (en) * 2000-12-15 2002-08-29 Callender Thomas J. Process and system for creating and administering interview or test

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0481214A1 (en) * 1990-09-14 1992-04-22 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
WO1996037503A1 (en) * 1995-05-26 1996-11-28 Genta Incorporated Compositions and methods for the synthesis of organophosphorus derivatives
US5977089A (en) * 1996-07-26 1999-11-02 Gilead Sciences, Inc. Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
H. CHAPMAN ET AL.: "Practical synthesis, separation, and stereochemical assignment of the PMPA pro-drug GS-7340", NUCLEOSIDES, NUCLEOTIDES & NUCLEIC ACIDS, vol. 20, 2001, pages 621 - 628, XP002202043 *
SIDDIQUI A Q ET AL: "DESIGN AND SYNTHESIS OF LIPOPHILIC PHOSPHORAMIDATE D4T-MP PRODRUGS EXPRESSING HIGH POTENCY AGAINST HIV IN CELL CULTRURE: STRUCTURAL DETERMINANTS FOR IN VITRO ACTIVITY AND QSAR", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 20, 1999, pages 4122 - 4128, XP000999173, ISSN: 0022-2623 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8871785B2 (en) 2003-04-25 2014-10-28 Gilead Sciences, Inc. Antiviral phosphonate analogs
US9579332B2 (en) 2004-07-27 2017-02-28 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds
US9585906B2 (en) 2007-03-30 2017-03-07 Gilead Pharmasset Llc Nucleoside phosphoramidate prodrugs
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV
US11845755B2 (en) 2022-03-02 2023-12-19 Gilead Sciences, Inc. Compounds and methods for treatment of viral infections
US11851438B2 (en) 2022-03-02 2023-12-26 Gilead Sciences, Inc. 1′-cyano nucleoside analogs and methods for treatment of viral infections

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