CN1291994C - 核苷酸膦酸酯类似物前药及其筛选和制备方法 - Google Patents

核苷酸膦酸酯类似物前药及其筛选和制备方法 Download PDF

Info

Publication number
CN1291994C
CN1291994C CNB018131611A CN01813161A CN1291994C CN 1291994 C CN1291994 C CN 1291994C CN B018131611 A CNB018131611 A CN B018131611A CN 01813161 A CN01813161 A CN 01813161A CN 1291994 C CN1291994 C CN 1291994C
Authority
CN
China
Prior art keywords
amino
tautomer
salt
methyl
free base
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
CNB018131611A
Other languages
English (en)
Chinese (zh)
Other versions
CN1443189A (zh
Inventor
M·W·贝克尔
H·H·查普曼
T·西拉
E·J·埃森伯格
何公欣
M·R·柯南
W·A·李
E·J·普里斯博
J·C·罗洛夫
M·L·斯帕拉西诺
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Sciences Inc
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
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=CN1291994(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of CN1443189A publication Critical patent/CN1443189A/zh
Application granted granted Critical
Publication of CN1291994C publication Critical patent/CN1291994C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biophysics (AREA)
  • General Engineering & Computer Science (AREA)
  • General Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Food Science & Technology (AREA)
  • Pathology (AREA)
CNB018131611A 2000-07-21 2001-07-20 核苷酸膦酸酯类似物前药及其筛选和制备方法 Expired - Lifetime CN1291994C (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22002100P 2000-07-21 2000-07-21
US60/220,021 2000-07-21
PCT/US2001/023104 WO2002008241A2 (en) 2000-07-21 2001-07-20 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CNB2004100978453A Division CN100402539C (zh) 2000-07-21 2001-07-20 核苷酸膦酸酯类似物前药及其筛选和制备方法

Publications (2)

Publication Number Publication Date
CN1443189A CN1443189A (zh) 2003-09-17
CN1291994C true CN1291994C (zh) 2006-12-27

Family

ID=22821718

Family Applications (2)

Application Number Title Priority Date Filing Date
CNB2004100978453A Expired - Lifetime CN100402539C (zh) 2000-07-21 2001-07-20 核苷酸膦酸酯类似物前药及其筛选和制备方法
CNB018131611A Expired - Lifetime CN1291994C (zh) 2000-07-21 2001-07-20 核苷酸膦酸酯类似物前药及其筛选和制备方法

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CNB2004100978453A Expired - Lifetime CN100402539C (zh) 2000-07-21 2001-07-20 核苷酸膦酸酯类似物前药及其筛选和制备方法

Country Status (37)

Country Link
US (10) US20040018150A1 (OSRAM)
EP (3) EP1301519B2 (OSRAM)
JP (4) JP4651264B2 (OSRAM)
KR (2) KR100767432B1 (OSRAM)
CN (2) CN100402539C (OSRAM)
AP (1) AP1466A (OSRAM)
AU (3) AU2001282941C1 (OSRAM)
BE (1) BE2016C018I2 (OSRAM)
BG (1) BG66037B1 (OSRAM)
BR (1) BRPI0112646B8 (OSRAM)
CA (3) CA2725819C (OSRAM)
CY (2) CY2016008I2 (OSRAM)
CZ (2) CZ304734B6 (OSRAM)
DK (2) DK2682397T3 (OSRAM)
EA (1) EA004926B1 (OSRAM)
EE (1) EE05366B1 (OSRAM)
ES (2) ES2627903T3 (OSRAM)
FR (1) FR16C0013I2 (OSRAM)
HK (1) HK1243711A1 (OSRAM)
HR (2) HRP20160074B1 (OSRAM)
HU (2) HU230960B1 (OSRAM)
IL (1) IL153658A0 (OSRAM)
IS (1) IS2985B (OSRAM)
LT (2) LT2682397T (OSRAM)
LU (1) LU93029I2 (OSRAM)
MX (1) MXPA03000587A (OSRAM)
NL (1) NL300803I2 (OSRAM)
NO (6) NO336718B1 (OSRAM)
NZ (3) NZ535408A (OSRAM)
OA (1) OA12393A (OSRAM)
PL (1) PL213214B1 (OSRAM)
PT (2) PT2682397T (OSRAM)
SI (2) SI1301519T1 (OSRAM)
TR (1) TR200300055T2 (OSRAM)
UA (1) UA75889C2 (OSRAM)
WO (1) WO2002008241A2 (OSRAM)
ZA (1) ZA200210271B (OSRAM)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104558036A (zh) * 2014-12-11 2015-04-29 杭州和泽医药科技有限公司 一种替诺福韦艾拉酚胺半反丁烯二酸盐晶型及其制备方法
US10065958B2 (en) 2010-07-22 2018-09-04 Gilead Sciences, Inc. Methods and compounds for treating Paramyxoviridae virus infections

Families Citing this family (237)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ535408A (en) * 2000-07-21 2006-09-29 Gilead Sciences Inc Method for selecting prodrugs of phosphonate nucleotide analogues
US7388002B2 (en) * 2001-11-14 2008-06-17 Biocryst Pharmaceuticals, Inc. Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
WO2003087298A2 (en) * 2001-11-14 2003-10-23 Biocryst Pharmaceuticals, Inc. Nucleosides preparation thereof and use as inhibitors of rna viral polymerases
MXPA04010527A (es) * 2002-04-26 2004-12-13 Gilead Sciences Inc Acumulacion celular de analogos de fosfonato de los compuestos inhibidores de la proteasa del virus de inmunodeficiencia humana (vih).
US20050239054A1 (en) * 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
CA2485702C (en) 2002-05-13 2011-07-19 Metabasis Therapeutics, Inc. Novel phosphonic acid based prodrugs of pmea and its analogues
WO2004064845A1 (en) * 2003-01-14 2004-08-05 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
WO2005002626A2 (en) * 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US7452901B2 (en) * 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
WO2004096287A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
US7429565B2 (en) * 2003-04-25 2008-09-30 Gilead Sciences, Inc. Antiviral phosphonate analogs
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
WO2004096285A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
KR20060022647A (ko) 2003-04-25 2006-03-10 길리애드 사이언시즈, 인코포레이티드 키나아제 억제 포스포네이트 유사체
WO2005044308A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
EP1678322A2 (en) * 2003-10-24 2006-07-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
US7427624B2 (en) 2003-10-24 2008-09-23 Gilead Sciences, Inc. Purine nucleoside phosphorylase inhibitory phosphonate compounds
US20050153990A1 (en) * 2003-12-22 2005-07-14 Watkins William J. Phosphonate substituted kinase inhibitors
BRPI0418031A (pt) * 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
NZ547907A (en) * 2003-12-22 2010-07-30 Gilead Sciences Inc 4'-Substituted carbovir-and abacavir-derivatives as well as related compounds with HIV and HCV antiviral activity
CN1950383B (zh) * 2003-12-30 2010-06-09 吉里德科学公司 用于治疗病毒性疾病的膦酸酯、单膦酸酰胺化物、双膦酸酰胺化物
WO2005072748A1 (en) * 2004-01-21 2005-08-11 Gilead Sciences, Inc. Use of adefovir or tenofovir for inhibiting mmtv-like viruses involved in breast cancer and primary biliary cirrhosis
US8411105B1 (en) 2004-05-14 2013-04-02 Nvidia Corporation Method and system for computing pixel parameters
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
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
MXPA06014013A (es) 2004-06-08 2007-03-15 Metabasis Therapeutics Inc Sintesis mediada por acidos de lewis de esteres ciclicos.
ES2720618T3 (es) * 2004-07-27 2019-07-23 Gilead Sciences Inc Análogos de fosfonato de compuestos de inhibidores de VIH
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
US8642577B2 (en) 2005-04-08 2014-02-04 Chimerix, Inc. Compounds, compositions and methods for the treatment of poxvirus infections
CN100359315C (zh) * 2005-05-26 2008-01-02 林维宣 兽药残留能力验证样品及制备方法
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 (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
US8076303B2 (en) 2005-12-13 2011-12-13 Spring Bank Pharmaceuticals, Inc. Nucleotide and oligonucleotide prodrugs
CN100396689C (zh) * 2006-03-07 2008-06-25 中国医学科学院医药生物技术研究所 一组具有抑制hiv-1/hbv病毒复制活性的替诺福韦单酯化合物
CN101442994B (zh) 2006-05-16 2013-03-06 吉里德科学公司 用于治疗恶性血液病的方法和组合物
ES2532502T3 (es) * 2006-07-12 2015-03-27 Mylan Laboratories Limited Proceso para la preparación de tenofovir
US7951789B2 (en) 2006-12-28 2011-05-31 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
US8105489B2 (en) * 2007-06-26 2012-01-31 The University Of Wyoming Research Corporation 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
JP5562255B2 (ja) * 2008-01-25 2014-07-30 キメリクス，インコーポレイテッド ウイルス感染を治療する方法
TWI444384B (zh) 2008-02-20 2014-07-11 Gilead Sciences Inc 核苷酸類似物及其在治療惡性腫瘤上的用途
CA2722165C (en) * 2008-04-25 2016-01-19 Cipla Limited Crystalline form of tenofovir disoproxil and a process for its preparation
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
AU2009277172B2 (en) * 2008-07-02 2014-05-29 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
KR101642527B1 (ko) 2008-07-08 2016-07-25 길리애드 사이언시즈, 인코포레이티드 Ｈｉｖ 억제제 화합물의 염
NZ617066A (en) 2008-12-23 2015-02-27 Gilead Pharmasset Llc Nucleoside analogs
AU2009329872B2 (en) 2008-12-23 2016-07-07 Gilead Pharmasset Llc Synthesis of purine nucleosides
NZ593648A (en) 2008-12-23 2013-09-27 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI576352B (zh) 2009-05-20 2017-04-01 基利法瑪席特有限責任公司 核苷磷醯胺
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
US8614200B2 (en) 2009-07-21 2013-12-24 Chimerix, Inc. Compounds, compositions and methods for treating ocular conditions
WO2011035250A1 (en) 2009-09-21 2011-03-24 Gilead Sciences, Inc. Processes and intermediates for the preparation of 1'-substituted carba-nucleoside analogs
ES2629165T3 (es) 2010-02-12 2017-08-07 Chimerix, Inc. Métodos de tratamiento de una infección vírica
PL3290428T3 (pl) 2010-03-31 2022-02-07 Gilead Pharmasset Llc Tabletka zawierająca krystaliczny (S)-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-diokso-3,4-dihydropirymidyn-1(2H)-ylo)-4-fluoro-3-hydroksy-4-metylotetrahydrofuran-2-ylo)metoksy)(fenoksy)fosforylo)amino)propanian izopropylu
ES2644990T3 (es) 2010-03-31 2017-12-01 Gilead Pharmasset Llc Síntesis estereoselectiva de principios activos que contienen fósforo
CA2795054A1 (en) 2010-04-01 2011-10-06 Idenix Pharmaceuticals, Inc. 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
US9090642B2 (en) * 2010-07-19 2015-07-28 Gilead Sciences, Inc. Methods for the preparation of diasteromerically pure phosphoramidate prodrugs
PT3042910T (pt) 2010-11-30 2019-04-16 Gilead Pharmasset Llc 2'-espiro-nucleósidos para utilização na terapia da hepatite c
CN103338754A (zh) 2010-12-10 2013-10-02 西格玛制药实验有限责任公司 口服活性核苷酸类似物或口服活性核苷酸类似物前药的高度稳定组合物
ZA201103820B (en) 2010-12-13 2012-01-25 Laurus Labs Private Ltd Process for the preparation of tenofovir
EP2691409B1 (en) 2011-03-31 2018-02-21 Idenix Pharmaceuticals LLC. Compounds and pharmaceutical compositions for the treatment of viral infections
US9550803B2 (en) 2011-05-06 2017-01-24 University Of Southern California Method to improve antiviral activity of nucleotide analogue drugs
JP5951757B2 (ja) * 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 抗ｈｉｖ剤を調製するためのプロセスおよび中間体
AP3639A (en) * 2011-08-16 2016-03-13 Gilead Sciences Inc Tenofovir alafenamide hemifumarate
AU2014271320B2 (en) * 2011-08-16 2017-02-23 Gilead Sciences, Inc. Tenofovir alafenamide hemifumarate
WO2013040492A2 (en) 2011-09-16 2013-03-21 Gilead Sciences, Inc. Methods for treating hcv
TWI689513B (zh) * 2011-10-07 2020-04-01 美商基利科學股份有限公司 抗病毒核苷酸類似物的製備方法
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
ES2874774T3 (es) 2011-12-22 2021-11-05 Geron Corp Análogos de guanina como sustratos de telomerasa y afectores de la longitud de los telómeros
US20150105350A1 (en) * 2012-02-03 2015-04-16 Gilead Sciences, Inc. Combination therapy comprising tenofovir alafenamide hemifumarate and cobicistat for use in the treatment of viral infections
WO2013115916A1 (en) 2012-02-03 2013-08-08 Gilead Sciences, Inc. Combination therapy comprising gs-7340 and cobicistat for use in the treatment of viral infections
CN107312039B (zh) * 2012-08-30 2019-06-25 江苏豪森药业集团有限公司 一种替诺福韦前药的制备方法
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)
KR102186030B1 (ko) 2012-10-29 2020-12-03 시플라 리미티드 항 바이러스성 포스포네이트 유사체 및 이의 제조를 위한 방법
CN102899327B (zh) * 2012-11-06 2014-06-11 清华大学深圳研究生院 一种抗病毒的小核酸及其温度敏感型凝胶制剂与应用
KR20150082613A (ko) * 2012-11-16 2015-07-15 머크 샤프 앤드 돔 코포레이션 인간 포스파티딜이노시톨 3-키나제 델타의 퓨린 억제제
CN103848869B (zh) * 2012-12-04 2016-12-21 上海医药工业研究院 制备替诺福韦的方法
CN103848868B (zh) * 2012-12-04 2017-04-12 蚌埠丰原涂山制药有限公司 制备替诺福韦的方法
EP2950786B1 (en) 2013-01-31 2019-11-27 Gilead Pharmasset LLC Combination formulation of two antiviral compounds
CN104072539B (zh) * 2013-03-25 2017-03-29 安徽贝克联合制药有限公司 替诺福韦双(4‑乙酰氨基苯酚氧基)酯及其制备方法和其应用
WO2014187314A1 (zh) * 2013-05-21 2014-11-27 成都先导药物开发有限公司 一种药物靶标捕获方法
WO2014195724A1 (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
NZ716840A (en) 2013-08-27 2017-06-30 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
WO2015079455A2 (en) * 2013-11-27 2015-06-04 Laurus Labs Private Limited A recycling process for preparing tenofovir alafenamide diastereomers
IN2014MU00118A (OSRAM) * 2014-01-14 2015-08-28 Mylan Lab Ltd
TWI660965B (zh) * 2014-01-15 2019-06-01 美商基利科學股份有限公司 泰諾福韋之固體形式
CN104804042B (zh) * 2014-01-24 2018-01-19 齐鲁制药有限公司 核苷酸膦酸酯类化合物、其药物组合物、制备方法及用途
WO2015120057A1 (en) 2014-02-05 2015-08-13 Gilead Sciences, Inc. Pharmaceutical combinations against co-infection with hiv and tuberculosis
EP3105238A4 (en) 2014-02-13 2017-11-08 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
CN105814068B (zh) * 2014-02-27 2017-08-04 四川海思科制药有限公司 一种取代的氨基磷酸酯类衍生物、其制备方法及其应用
CN105001262B (zh) * 2014-04-18 2017-09-01 四川海思科制药有限公司 芳基取代的磷酰胺类衍生物及其在医学上的应用
CN105531281B (zh) * 2014-04-21 2017-12-15 四川海思科制药有限公司 一种核苷类似物及其中间体的制备方法
CN105085571A (zh) * 2014-05-20 2015-11-25 四川海思科制药有限公司 替诺福韦艾拉酚胺复合物及其制备方法和用途
WO2015197006A1 (zh) * 2014-06-25 2015-12-30 四川海思科制药有限公司 一种取代的氨基酸硫酯类化合物、其组合物及应用
JP2017520545A (ja) 2014-07-02 2017-07-27 リガンド・ファーマシューティカルズ・インコーポレイテッド プロドラッグ化合物およびそれらの使用
CN106795188B (zh) 2014-09-15 2021-02-09 加利福尼亚大学董事会 核苷酸类似物
KR101703258B1 (ko) 2014-12-30 2017-02-06 한미정밀화학주식회사 고순도의 (r)-9-[2-(포스포노메톡시)프로필]아데닌의 제조방법
KR101703257B1 (ko) 2014-09-30 2017-02-06 한미정밀화학주식회사 고순도의 (r)-9-[2-(포스포노메톡시)프로필]아데닌의 제조방법
CN106687467A (zh) * 2014-09-30 2017-05-17 韩美精密化学株式会社 高纯度（r）‑9‑[2‑（磷酰甲氧基）丙基]腺嘌呤的制备方法
US11311545B2 (en) 2014-10-09 2022-04-26 Board Of Regents Of The University Of Nebraska Compositions and methods for the delivery of therapeutics
TWI740546B (zh) 2014-10-29 2021-09-21 美商基利科學股份有限公司 製備核糖苷的方法
CN105646584B (zh) * 2014-11-12 2018-09-28 四川海思科制药有限公司 替诺福韦艾拉酚胺富马酸盐晶型及其制备方法和用途
BR112017014085A2 (pt) 2015-01-03 2018-01-09 Mylan Laboratories Ltd processos para a preparação de hemifumarato de tenofovir alafenamida amorfo e uma pré-mistura do mesmo
WO2016187160A1 (en) * 2015-05-16 2016-11-24 Godx, Inc. Point of need testing device and methods of use thereof
CN106188139B (zh) 2015-05-29 2020-02-18 江苏天士力帝益药业有限公司 替诺福韦单苄酯磷酸酰胺前药、其制备方法及应用
CZ2015384A3 (cs) 2015-06-05 2016-12-14 Zentiva, K.S. Pevné formy Tenofovir alafenamidu
CA2987085A1 (en) * 2015-06-17 2016-12-22 Gilead Sciences, Inc. Co-crystals, salts and solid forms of tenofovir alafenamide
AU2016287500B2 (en) 2015-06-30 2019-05-02 Gilead Sciences, Inc. Pharmaceutical formulations comprising tenofovir and emtricitabine
TN2018000048A1 (en) 2015-08-10 2019-07-08 Merck Sharp & Dohme Antiviral beta-amino acid ester phosphodiamide compounds
TWI620754B (zh) * 2015-08-26 2018-04-11 Method for preparing amino phosphate derivative and preparation method thereof
TWI616452B (zh) * 2015-08-26 2018-03-01 Preparation method of nucleoside analog and intermediate thereof
TWI616453B (zh) * 2015-08-27 2018-03-01 Substituted amino acid thioester compounds, compositions 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
CN114366745A (zh) 2015-09-16 2022-04-19 吉利德科学公司 治疗沙粒病毒科和冠状病毒科病毒感染的方法
EA201890654A1 (ru) 2015-11-09 2018-10-31 Джилид Сайэнс, Инк. Терапевтические композиции для лечения вируса иммунодефицита человека
CN106800573B (zh) * 2015-11-25 2020-03-10 四川海思科制药有限公司 一种核苷酸膦酸酯一水合物及其制备方法和在医药上的应用
WO2017100108A1 (en) 2015-12-10 2017-06-15 Merck Sharp & Dohme Corp. Antiviral phosphodiamide prodrugs of tenofovir
CN106866737B (zh) * 2015-12-11 2020-11-20 南京圣和药物研发有限公司 膦酸衍生物及其应用
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
EP3411378B1 (en) 2016-02-02 2020-03-25 Sandoz AG Crystalline forms of tenofovir alafenamide monofumarate
WO2017133517A1 (zh) * 2016-02-03 2017-08-10 四川海思科制药有限公司 一种磷酰胺衍生物及制备方法和用途
CN108350007B (zh) * 2016-03-01 2020-04-10 深圳市塔吉瑞生物医药有限公司 一种取代的腺嘌呤化合物及其药物组合物
CN107179355B (zh) * 2016-03-11 2021-08-10 广东东阳光药业有限公司 一种分离检测替诺福韦艾拉酚胺及其有关物质的方法
CZ2016156A3 (cs) 2016-03-17 2017-09-27 Zentiva, K.S. Způsob přípravy diastereomerně čistého Tenofoviru Alafenamidu nebo jeho solí
CN107226826A (zh) * 2016-03-25 2017-10-03 江苏奥赛康药业股份有限公司 替诺福韦艾拉酚胺富马酸盐化合物及其药物组合物
WO2017211325A1 (zh) * 2016-06-05 2017-12-14 上海诚妙医药科技有限公司 富马酸替诺福韦艾拉酚胺盐的新晶型、制备方法及其用途
CN107698621A (zh) * 2016-06-20 2018-02-16 杭州和泽医药科技有限公司 一种腺嘌呤衍生物的膦酸酯前药及其在医药上的应用
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
TWI853404B (zh) 2016-08-19 2024-08-21 美商基利科學股份有限公司 治療性化合物
CN106317116A (zh) * 2016-08-19 2017-01-11 张红利 磷酰胺核苷类化合物及其药学上可接受的盐与应用、药物组合物
WO2018039157A1 (en) 2016-08-25 2018-03-01 Merck Sharp & Dohme Corp. Antiviral prodrugs of tenofovir
CN106380484A (zh) * 2016-08-29 2017-02-08 杭州百诚医药科技股份有限公司 一种替诺福韦艾拉酚胺的新晶型及其制备方法
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
WO2018080903A1 (en) 2016-10-26 2018-05-03 Merck Sharp & Dohme Corp. Antiviral aryl-amide phosphodiamide compounds
CN106565785B (zh) * 2016-11-09 2019-11-12 周雨恬 一种具有抗hbv/hiv活性的核苷氨基磷酸酯类化合物及其盐和用途
CN108129514A (zh) * 2016-12-01 2018-06-08 北京美倍他药物研究有限公司 磷酸/膦酸衍生物的单一异构体及其医药用途
BR112019012511A2 (pt) 2016-12-22 2019-11-19 Idenix Pharmaceuticals Llc compostos antivirais de benzil-amina fosfodiamida, composição farmacêutica e uso do composto
US10519159B2 (en) 2016-12-22 2019-12-31 Merck Sharp & Dohme Corp. Antiviral aliphatic ester prodrugs of tenofovir
WO2018115046A1 (en) 2016-12-23 2018-06-28 Sandoz Ag Crystalline solid forms of tenofovir alafenamide
TWI820984B (zh) 2017-01-31 2023-11-01 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
WO2018153977A1 (en) 2017-02-24 2018-08-30 Hexal Ag Stable composition of tenofovir alafenamide
US20190374557A1 (en) * 2017-02-28 2019-12-12 Alexandre Vasilievich Ivachtchenko Cyclobutyl (S)-2-[[[(R)-2-(6-aminopurin-9-yl)-1-methyl-ethoxy]methyl-phenoxy-phosphoryl]amino]-propanoates, and production process and application thereof
RU2659388C1 (ru) 2017-02-28 2018-07-02 Васильевич Иващенко Александр Нуклеотиды, включающие N-[(S)-1-циклобутоксикарбонил]фосфорамидатный фрагмент, их аналоги и их применение
CN106866739B (zh) * 2017-03-10 2018-11-02 华东师范大学 一种(r)-1-(6-氨基-9h-嘌呤-9-基)2-苯酯的制备方法
KR102460968B1 (ko) 2017-03-14 2022-11-01 길리애드 사이언시즈, 인코포레이티드 고양이 코로나바이러스 감염의 치료 방법
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 (zh) * 2017-04-26 2018-11-13 上海医药工业研究院 一种替诺福韦丙酚酰胺盐晶型及其制备方法和用途
CN110636884B (zh) 2017-05-01 2022-10-04 吉利德科学公司 新结晶形式
KR102379965B1 (ko) * 2017-05-19 2022-03-29 주식회사 종근당 테노포비르의 효율적인 제조방법
CN107266499B (zh) * 2017-06-05 2019-07-02 珠海优润医药科技有限公司 一种抗病毒化合物及其制备方法
CN111587107B (zh) 2017-06-30 2023-03-31 希普拉有限公司 药物组合物
TW201919648A (zh) 2017-07-11 2019-06-01 美商基利科學股份有限公司 用於治療病毒感染之含rna聚合酶抑制劑與環糊精的組合物
WO2019021319A1 (en) 2017-07-27 2019-01-31 Cipla Limited PHARMACEUTICAL COMPOSITIONS
WO2019027920A1 (en) 2017-08-01 2019-02-07 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) FOR THE TREATMENT OF VIRAL INFECTIONS
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
CN107655987B (zh) * 2017-09-08 2020-11-03 厦门蔚扬药业有限公司 一种替诺福韦艾拉酚胺及其异构体的hplc检测方法
CN107522743A (zh) * 2017-09-30 2017-12-29 深圳科兴生物工程有限公司 一种半富马酸替诺福韦艾拉酚胺工业化连续生产方法
EP3700573A1 (en) 2017-10-24 2020-09-02 Gilead Sciences, Inc. Methods of treating patients co-infected with a virus and tuberculosis
CN109942632B (zh) * 2017-12-20 2021-08-31 上海博志研新药物研究有限公司 替诺福韦艾拉酚胺中间体的制备方法
CN109942633B (zh) * 2017-12-20 2021-08-31 上海新礼泰药业有限公司 替诺福韦艾拉酚胺中间体的制备方法
WO2019130354A1 (en) 2017-12-30 2019-07-04 Cipla Limited Polymorphic forms of (9-[(r)-2-[[(s)-[[(s)-1- (isopropoxycarbonyl)ethyl]amino]phenoxy phosphinyl]methoxy]propyl] adenine and pharmaceutically acceptable salts thereof
AU2019207625A1 (en) 2018-01-09 2020-07-30 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
CN117402189A (zh) * 2018-01-10 2024-01-16 广东集宝医药技术有限公司 氨基磷(膦)酸缩醛和磷(膦)酸缩醛化合物
CA3126348A1 (en) * 2018-01-12 2020-07-18 Board Of Regents Of The University Of Nebraska Antiviral prodrugs and formulations thereof
AU2019221568B2 (en) 2018-02-15 2021-04-22 Gilead Sciences, Inc. Pyridine derivatives and their use for treating HIV infection
TWI823164B (zh) 2018-02-16 2023-11-21 美商基利科學股份有限公司 用於製備有療效化合物之方法及中間物
CN108101943B (zh) * 2018-02-28 2020-11-24 顾世海 一种替诺福韦前药或可药用盐及其在医药上的应用
CA3132832A1 (en) 2018-04-09 2019-10-17 Howard E. Gendelman Antiviral prodrugs and formulations thereof
TWI814350B (zh) 2018-07-16 2023-09-01 美商基利科學股份有限公司 用於治療hiv之蛋白殼抑制劑
WO2020018399A1 (en) 2018-07-19 2020-01-23 Merck Sharp & Dohme Corp. Phosphinic amide prodrugs of tenofovir
CN112996517A (zh) 2018-09-19 2021-06-18 吉利德科学公司 预防hiv的整合酶抑制剂
PL3938047T3 (pl) 2019-03-22 2022-11-07 Gilead Sciences, Inc. Zmostkowane tricykliczne związki karbamoilopirydonowe i ich zastosowanie farmaceutyczne
CA3143349A1 (en) 2019-07-17 2021-01-21 Nucorion Pharmaceuticals, Inc. Cyclic deoxyribonucleotide compounds
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
EP3999067A1 (en) 2019-07-19 2022-05-25 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
US12049474B2 (en) 2019-08-22 2024-07-30 Emory University Nucleoside prodrugs and uses related thereto
WO2021055808A1 (en) * 2019-09-20 2021-03-25 Abbott Rapid Diagnostics International Unlimited Company Antibodies directed against tenofovir and derivatives thereof
EP4065116B1 (en) 2019-11-26 2026-01-21 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
TWI789695B (zh) 2020-01-27 2023-01-11 美商基利科學股份有限公司 治療sars cov-2感染之方法
EP4085062A1 (en) 2020-02-20 2022-11-09 Cipla Limited Novel salts and/or co-crystals of tenofovir alafenamide
JP7554841B2 (ja) 2020-03-12 2024-09-20 ギリアード サイエンシーズ， インコーポレイテッド １’－シアノヌクレオシドを調製する方法
KR20220156884A (ko) 2020-03-20 2022-11-28 길리애드 사이언시즈, 인코포레이티드 4'-c-치환된-2-할로-2'-데옥시아데노신 뉴클레오시드의 프로드러그 및 이의 제조 및 사용 방법
WO2021202669A2 (en) 2020-04-01 2021-10-07 Reyoung Corporation Nucleoside and nucleotide conjugate compounds and uses thereof
KR102906891B1 (ko) 2020-04-06 2026-01-05 길리애드 사이언시즈, 인코포레이티드 1'-시아노 치환된 카르바뉴클레오시드 유사체의 흡입 제형
KR20210125298A (ko) 2020-04-08 2021-10-18 주식회사 파마코스텍 테노포비어 알라펜아미드 헤미타르트레이트의 신규한 제조방법
CN115605492B (zh) 2020-04-21 2025-09-16 配体制药股份有限公司 核苷酸前药化合物
KR20230018473A (ko) 2020-05-29 2023-02-07 길리애드 사이언시즈, 인코포레이티드 렘데시비르 치료 방법
JP2023531524A (ja) 2020-06-24 2023-07-24 ギリアード サイエンシーズ， インコーポレイテッド １’－シアノヌクレオシド類似体及びその使用
TWI858267B (zh) 2020-06-25 2024-10-11 美商基利科學股份有限公司 用於治療hiv之蛋白殼抑制劑
CN113970612B (zh) * 2020-07-22 2023-08-01 北京四环制药有限公司 一种高效液相色谱法测定丙酚替诺福韦有关物质的方法
AU2021331214B2 (en) 2020-08-27 2024-01-04 Gilead Sciences, Inc. Compounds and methods for treatment of viral infections
CN112336695B (zh) * 2020-09-28 2023-01-03 华北制药华坤河北生物技术有限公司 一种富马酸丙酚替诺福韦片剂及其制备方法和有关物质的检测方法
KR20230107288A (ko) 2020-11-11 2023-07-14 길리애드 사이언시즈, 인코포레이티드 gp120 CD4 결합 부위-지향 항체를 이용한 요법에 감수성인 HIV 환자를 식별하는 방법
US11667656B2 (en) 2021-01-27 2023-06-06 Apotex Inc. Crystalline forms of Tenofovir alafenamide
CN113075307B (zh) * 2021-03-08 2025-03-11 瑞阳制药股份有限公司 富马酸丙酚替诺福韦异构体的检测方法
CN113214322B (zh) * 2021-04-30 2022-10-25 山东立新制药有限公司 替诺福韦绿色环保的制备方法
WO2022251594A1 (en) * 2021-05-27 2022-12-01 Antios Therapeutics, Inc. Pharmacokinetics and dose-related improvments in subjects treated with phosphoramidate clevudine prodrugs
CA3237155A1 (en) 2021-12-03 2023-06-08 Zhimin Du Therapeutic compounds for hiv virus infection
AU2022403012B2 (en) 2021-12-03 2026-02-12 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
SI4440702T1 (sl) 2021-12-03 2025-09-30 Gilead Sciences, Inc. Terapevtske spojine za okužbo z virusom hiv
CN114369120A (zh) * 2022-01-28 2022-04-19 石家庄龙泽制药股份有限公司 一种丙酚替诺福韦关键中间体的制备方法
KR20240154647A (ko) 2022-03-02 2024-10-25 길리애드 사이언시즈, 인코포레이티드 바이러스성 감염 치료를 위한 화합물 및 방법
TWI856796B (zh) 2022-04-06 2024-09-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
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
CA3262284A1 (en) 2022-07-21 2024-01-25 Antiva Biosciences, Inc. Pharmaceutical compositions and forms for the treatment of human papillomavirus (HPV) infection and HPV-induced neoplasm
CN119768183A (zh) 2022-08-26 2025-04-04 吉利德科学公司 用于广泛中和抗体的给药和安排方案
WO2024076915A1 (en) 2022-10-04 2024-04-11 Gilead Sciences, Inc. 4'-thionucleoside analogues and their pharmaceutical use
US12357577B1 (en) 2024-02-02 2025-07-15 Gilead Sciences, Inc. Pharmaceutical formulations and uses thereof
AU2024240009A1 (en) 2023-03-17 2025-09-18 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Methods for treatment of age-related macular degeneration
AR132464A1 (es) 2023-04-19 2025-07-02 Gilead Sciences Inc Régimen de dosificación de inhibidor de la cápside
WO2024249592A1 (en) 2023-05-31 2024-12-05 Gilead Sciences, Inc. Quinazolinyl-indazole derivatives as therapeutic compounds for hiv
AU2024281548A1 (en) 2023-05-31 2025-11-13 Gilead Sciences, Inc. Solid forms of compounds useful in the treatment of hiv
WO2025029247A1 (en) 2023-07-28 2025-02-06 Gilead Sciences, Inc. Weekly regimen of lenacapavir for the treatment and prevention of hiv
WO2025042394A1 (en) 2023-08-23 2025-02-27 Gilead Sciences, Inc. Dosing regimen of hiv capsid inhibitor
TW202530226A (zh) 2023-10-11 2025-08-01 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
TW202530227A (zh) 2023-10-11 2025-08-01 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
US20250120989A1 (en) 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
WO2025137245A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
US20250333424A1 (en) 2024-03-01 2025-10-30 Gilead Sciences, Inc. Antiviral compounds
US20250296932A1 (en) 2024-03-01 2025-09-25 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2025184452A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
EP4640214A1 (en) 2024-03-28 2025-10-29 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi A tablet comprising tenofovir alafenamide monofumarate
US20260007683A1 (en) 2024-06-14 2026-01-08 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
CN118652277A (zh) * 2024-08-19 2024-09-17 成都工业学院 一种用于治疗癌症疾病的化合物的制备方法

Family Cites Families (56)

* 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 (ja) 1989-07-27 1997-09-03 ダイセル化学工業株式会社 立体異性体の分離法
US5624898A (en) * 1989-12-05 1997-04-29 Ramsey Foundation Method for administering neurologic agents to the brain
JP2925753B2 (ja) 1990-02-23 1999-07-28 ダイセル化学工業株式会社 光学異性体の分離方法
FI911875L (fi) * 1990-04-20 1991-10-21 Bristol Myers Squibb Co Kirala 2-(fosfonometoxi) propylguaniner som antivirala aemnen.
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
SK280313B6 (sk) 1990-04-24 1999-11-08 �Stav Organick� Chemie A Biochemie Av �R N-(3-fluór-2-fosfonylmetoxypropyl)deriváty purínov
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
KR100221981B1 (ko) 1990-08-10 1999-09-15 안토닌 포레이트 뉴클레오티드의 신규 제조방법
ATE167679T1 (de) 1990-09-14 1998-07-15 Acad Of Science Czech Republic Wirkstoffvorläufer von phosphonaten
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 (cs) 1991-05-20 1999-01-13 Ústav Organické Chemie A Biochemie Avčr Di(2-propyl)estery 1-fluor-2-fosfonomethoxy-3-p -toluensulfonyloxypropanů, způsob jejich přípravy a použití
JP3010816B2 (ja) 1991-08-22 2000-02-21 ダイセル化学工業株式会社 光学分割における光学異性体と溶媒との回収方法、溶媒の循環使用方法、および光学異性体の再利用方法
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
AU661347B2 (en) 1991-10-11 1995-07-20 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
CA2171868A1 (en) * 1993-09-17 1995-03-23 Petr Alexander Method for dosing therapeutic compounds
BR9407510A (pt) 1993-09-17 1997-01-07 Gilead Sciences Inc Análogos de nucleotideo
US5798340A (en) * 1993-09-17 1998-08-25 Gilead Sciences, Inc. 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
DE69629112T2 (de) * 1995-05-26 2004-04-22 Genta Inc., San Diego Verfahren zur synthese von phosphororganischen verbindungen
EP0874858A1 (en) 1995-12-29 1998-11-04 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
WO1998004569A1 (en) 1996-07-26 1998-02-05 Gilead Sciences, Inc. Nucleotide analogs
US5922695A (en) * 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
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
ID28006A (id) 1997-07-25 2001-05-03 Gilead Sciences Inc Komposisi analog nukleotida
SG106657A1 (en) * 1997-07-25 2004-10-29 Gilead Sciences Inc Nycleotide analog composition and sythesis method
WO1999030727A1 (en) * 1997-12-17 1999-06-24 Enzon, Inc. Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents
JP2002500880A (ja) * 1998-01-23 2002-01-15 ニューバイオティックス インコーポレイテッド 酵素に触媒される治療剤
US6169078B1 (en) * 1998-05-12 2001-01-02 University Of Florida Materials and methods for the intracellular delivery of substances
JP2002518521A (ja) * 1998-06-20 2002-06-25 ワシントン・ユニバーシティ 医用画像解析、診断および治療のための膜透過性ペプチド錯体
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
DE60002986T2 (de) † 1999-02-12 2004-05-19 Glaxo Group Ltd., Greenford Phosphoramidat-, mono-, di-, und triphosphatester von (1r, cis)-4-(6-amino-9h-purin-9-yl)-2-cyclopentene-1-methanol als antivirale mittel
NZ535408A (en) * 2000-07-21 2006-09-29 Gilead Sciences Inc Method for selecting prodrugs of phosphonate nucleotide analogues
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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10065958B2 (en) 2010-07-22 2018-09-04 Gilead Sciences, Inc. Methods and compounds for treating Paramyxoviridae virus infections
CN104558036A (zh) * 2014-12-11 2015-04-29 杭州和泽医药科技有限公司 一种替诺福韦艾拉酚胺半反丁烯二酸盐晶型及其制备方法

Also Published As

Publication number Publication date
DK2682397T3 (da) 2017-06-19
CY1119411T1 (el) 2018-03-07
HRP20160074B1 (hr) 2021-09-03
US20050124584A1 (en) 2005-06-09
CN1443189A (zh) 2003-09-17
ES2627903T3 (es) 2017-08-01
SI2682397T1 (sl) 2017-08-31
BR0112646A (pt) 2003-06-24
ES2536972T3 (es) 2015-06-01
JP2010174033A (ja) 2010-08-12
US20050124585A1 (en) 2005-06-09
WO2002008241A3 (en) 2002-08-29
SI1301519T1 (sl) 2015-07-31
US20040018150A1 (en) 2004-01-29
CA2416757A1 (en) 2002-01-31
AU2001282941B2 (en) 2006-04-27
LTC1301519I2 (lt) 2023-02-27
EA200300188A1 (ru) 2003-06-26
FR16C0013I2 (fr) 2016-09-09
NZ536942A (en) 2006-03-31
US20050159392A1 (en) 2005-07-21
HRP20160074A8 (hr) 2016-07-29
IS6689A (is) 2003-01-17
HUS1900027I1 (hu) 2021-03-29
PT2682397T (pt) 2017-05-31
MXPA03000587A (es) 2004-04-05
CA2416757C (en) 2011-02-15
JP5111551B2 (ja) 2013-01-09
BRPI0112646B8 (pt) 2021-05-25
CA2725819C (en) 2015-09-22
AP1466A (en) 2005-09-22
LU93029I2 (fr) 2016-06-14
US20080227754A1 (en) 2008-09-18
CA2893174A1 (en) 2002-01-31
BG66037B1 (bg) 2010-11-30
LTPA2016009I1 (lt) 2016-04-25
BG107572A (bg) 2003-11-28
CZ304886B6 (cs) 2015-01-07
BRPI0112646B1 (pt) 2017-10-17
US20020119443A1 (en) 2002-08-29
NO20150909L (no) 2003-03-20
BE2016C018I2 (OSRAM) 2020-08-20
NO20131717L (no) 2003-03-20
CZ2003413A3 (cs) 2003-12-17
EA004926B1 (ru) 2004-10-28
NO2016006I1 (no) 2016-04-19
KR100767432B1 (ko) 2007-10-17
EP1301519B2 (en) 2021-11-10
NO2023006I1 (no) 2023-02-03
KR20060105807A (ko) 2006-10-11
PL213214B1 (pl) 2013-01-31
OA12393A (en) 2006-04-18
CY2016008I1 (el) 2016-12-14
JP2009062383A (ja) 2009-03-26
HRP20160074A2 (hr) 2016-03-11
DK1301519T4 (da) 2021-12-20
KR100749160B1 (ko) 2007-08-14
NL300803I2 (OSRAM) 2016-06-30
NO2016006I2 (no) 2016-04-19
IS2985B (is) 2017-09-15
NZ535408A (en) 2006-09-29
EP1301519B1 (en) 2015-02-25
IL153658A0 (en) 2003-07-06
NZ523438A (en) 2005-02-25
FR16C0013I1 (fr) 2016-05-27
NO20030270D0 (no) 2003-01-20
CN100402539C (zh) 2008-07-16
CN1706855A (zh) 2005-12-14
HUP0301307A2 (hu) 2003-09-29
US20050009043A1 (en) 2005-01-13
US7803788B2 (en) 2010-09-28
EP1301519A2 (en) 2003-04-16
HRP20030047A2 (en) 2007-08-31
US20050124583A1 (en) 2005-06-09
US20030219727A1 (en) 2003-11-27
TR200300055T2 (tr) 2004-12-21
NO20030270L (no) 2003-03-20
HK1054238A1 (en) 2003-11-21
EE05366B1 (et) 2010-12-15
JP2004504402A (ja) 2004-02-12
EP2682397A1 (en) 2014-01-08
ES2536972T5 (es) 2022-04-06
EP3235823A1 (en) 2017-10-25
EP2682397B1 (en) 2017-04-19
UA75889C2 (uk) 2006-06-15
CZ304734B6 (cs) 2014-09-10
JP5063554B2 (ja) 2012-10-31
JP4651264B2 (ja) 2011-03-16
ZA200210271B (en) 2003-12-31
NO20120466L (no) 2003-03-20
DK1301519T3 (en) 2015-05-26
AP2003002724A0 (en) 2003-06-30
LT2682397T (lt) 2017-06-12
EE200300029A (et) 2004-10-15
AU8294101A (en) 2002-02-05
JP2011140506A (ja) 2011-07-21
HK1243711A1 (en) 2018-07-20
US7390791B2 (en) 2008-06-24
HU230960B1 (hu) 2019-06-28
PT1301519E (pt) 2015-06-11
AU2005225039A1 (en) 2005-11-10
AU2005225039B2 (en) 2008-09-25
AU2001282941C1 (en) 2016-12-22
CY2016008I2 (el) 2016-12-14
US20060024659A1 (en) 2006-02-02
WO2002008241A2 (en) 2002-01-31
HRP20030047B1 (hr) 2016-02-26
HUP0301307A3 (en) 2005-12-28
HUS000494I2 (hu) 2021-03-29
PL360490A1 (en) 2004-09-06
CA2725819A1 (en) 2002-01-31
NO336718B1 (no) 2015-10-26
KR20030022295A (ko) 2003-03-15

Similar Documents

Publication Publication Date Title
CN1291994C (zh) 核苷酸膦酸酯类似物前药及其筛选和制备方法
AU2001282941A1 (en) Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
HK1194074B (en) Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
HK1194074A (en) Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
HK1054238B (en) Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CP01 Change in the name or title of a patent holder
CP01 Change in the name or title of a patent holder

Address after: California, USA

Patentee after: Gilead Sciences Inc.

Address before: American California

Patentee before: Gilead Sciences Inc.

CX01 Expiry of patent term
CX01 Expiry of patent term

Granted publication date: 20061227