JP2016522172A - Ｈｃｖを治療するのに有用な重水素化されたヌクレオシドプロドラッグ - Google Patents

Ｈｃｖを治療するのに有用な重水素化されたヌクレオシドプロドラッグ Download PDF

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JP2016522172A
JP2016522172A JP2016507703A JP2016507703A JP2016522172A JP 2016522172 A JP2016522172 A JP 2016522172A JP 2016507703 A JP2016507703 A JP 2016507703A JP 2016507703 A JP2016507703 A JP 2016507703A JP 2016522172 A JP2016522172 A JP 2016522172A
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alkyl
compound
deuterium
hydrogen
salt according
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JP2016522172A5 (enExample
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ミリンド、デシュパンデ
ジェイソン、アラン、ワイルス
本 彰 宏 橋
本 彰 宏 橋
アビナッシュ、パドケー
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アキリオン ファーマシューティカルズ，インコーポレーテッド
アキリオン ファーマシューティカルズ，インコーポレーテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/005—Sugars; Derivatives thereof; Nucleosides; Nucleotides; Nucleic acids
    • 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
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/22—Amides of acids of phosphorus
    • C07F9/24—Esteramides
    • C07F9/2404—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/2429—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic of arylalkanols
    • 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
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/22—Amides of acids of phosphorus
    • C07F9/24—Esteramides
    • C07F9/2454—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/2458—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic of aliphatic amines
    • 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
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • 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
    • C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
JP2016507703A 2013-04-12 2014-04-14 Ｈｃｖを治療するのに有用な重水素化されたヌクレオシドプロドラッグ Pending JP2016522172A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361811464P 2013-04-12 2013-04-12
US61/811,464 2013-04-12
PCT/US2014/034021 WO2014169280A2 (en) 2013-04-12 2014-04-14 Deuterated nucleoside prodrugs useful for treating hcv

Publications (2)

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JP2016522172A true JP2016522172A (ja) 2016-07-28
JP2016522172A5 JP2016522172A5 (enExample) 2017-06-01

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JP2016507703A Pending JP2016522172A (ja) 2013-04-12 2014-04-14 Ｈｃｖを治療するのに有用な重水素化されたヌクレオシドプロドラッグ
JP2016507702A Ceased JP2016518359A (ja) 2013-04-12 2014-04-14 Ｈｃｖを治療するための高活性のヌクレオシド誘導体

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JP2016507702A Ceased JP2016518359A (ja) 2013-04-12 2014-04-14 Ｈｃｖを治療するための高活性のヌクレオシド誘導体

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US (2) US9447132B2 (enExample)
EP (2) EP2984098A2 (enExample)
JP (2) JP2016522172A (enExample)
KR (2) KR20160002896A (enExample)
CN (2) CN105705511A (enExample)
AU (2) AU2014250762A1 (enExample)
BR (2) BR112015025716A2 (enExample)
CA (2) CA2909270A1 (enExample)
ES (1) ES2623287T3 (enExample)
RU (2) RU2015148006A (enExample)
WO (2) WO2014169280A2 (enExample)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS52954B (sr) 2009-09-21 2014-02-28 Gilead Sciences Inc. Postupci i intermedijeri za proizvodnju 1'-cijanokarbanukleozidnih analoga
AP3269A (en) 2010-07-22 2015-05-31 Gilead Sciences Inc Methods and compounds for treating paramyxoviridaevirus infections
WO2013174962A1 (en) 2012-05-25 2013-11-28 Janssen R&D Ireland Uracyl spirooxetane nucleosides
US10034893B2 (en) 2013-02-01 2018-07-31 Enanta Pharmaceuticals, Inc. 5, 6-D2 uridine nucleoside/tide derivatives
JP6767878B2 (ja) 2014-06-06 2020-10-14 リサーチ トライアングル インスティテュート アペリン受容体（ａｐｊ）アゴニストおよびそれらの使用
LT3160476T (lt) 2014-06-24 2021-04-12 Janssen Biopharma, Inc. Pakeistieji nukleozidai, nukleotidai ir jų analogai, skirti naudoti virusinių infekcijų gydyme
US20160016986A1 (en) * 2014-07-21 2016-01-21 Milind Deshpande Stabilized nucleotides for medical treatment
BR112017001847A2 (pt) * 2014-07-31 2018-02-27 Sandoz Ag processo para a preparação de um composto de fórmula (i), mistura, composição e composto de fórmula (ii)
US10526363B2 (en) 2014-08-15 2020-01-07 Merck Sharp & Dohme Corp. Substituted phosphoramidate compounds and uses thereof
WO2016033164A1 (en) 2014-08-26 2016-03-03 Enanta Pharmaceuticals, Inc. Nucleoside and nucleotide derivatives
WO2016041877A1 (en) * 2014-09-15 2016-03-24 Medivir Ab Methods for the preparation of diastereomerically pure phosphoramidate prodrugs
TWI687432B (zh) * 2014-10-29 2020-03-11 美商基利科學股份有限公司 絲狀病毒科病毒感染之治療
WO2016073756A1 (en) * 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Deuterated nucleoside/tide derivatives
US9732110B2 (en) 2014-12-05 2017-08-15 Enanta Pharmaceuticals, Inc. Nucleoside and nucleotide derivatives
WO2016099982A2 (en) 2014-12-15 2016-06-23 Emory University Phosphoramidates for the treatment of hepatitis b virus
WO2016098123A2 (en) * 2014-12-16 2016-06-23 Laurus Labs Private Ltd A recycling process for preparing (s)-2-[(substituted-phenoxy)-phenoxy- phosphorylamino] propionic acid isopropyl ester diastereomers
MA41441A (fr) * 2014-12-19 2017-12-12 Alios Biopharma Inc Nucléosides substitués, nucléotides et analogues de ceux-ci
LT3236972T (lt) 2014-12-26 2021-11-10 Emory University Antivirusiniai n4-hidroksicitidino dariniai
WO2016134053A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
WO2016134058A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Combinations useful to treat hepatitis c virus
KR102363946B1 (ko) 2015-03-06 2022-02-17 아테아 파마슈티컬즈, 인크. HCV 치료를 위한 β-D-2'-데옥시-2'-α-플루오로-2'-β-C-치환된-2-변형된-N6-치환된 퓨린 뉴클레오티드
CA2997170A1 (en) 2015-09-02 2017-03-09 Abbvie Inc. Anti-viral tetrahydrofurane derivatives
ES2918585T3 (es) 2015-09-16 2022-07-19 Gilead Sciences Inc Métodos para el tratamiento de infecciones por el virus Arenaviridae
WO2017059147A1 (en) * 2015-09-29 2017-04-06 Janssen Pharmaceuticals, Inc. Combination therapy regimen for treatment of hcv
RU2021133849A (ru) 2015-12-09 2022-03-21 Рисерч Трайэнгл Инститьют Улучшенные агонисты апелинового рецептора (apj) и их использование
CN106699828B (zh) * 2016-01-04 2019-05-21 上海长森药业有限公司 氘代HCV NS5b抑制剂核苷酸衍生物及其用途
JP2019525905A (ja) * 2016-06-24 2019-09-12 エモリー ユニバーシティー Ｂ型肝炎ウイルスの治療のためのホスホロアミデート
WO2018013937A1 (en) 2016-07-14 2018-01-18 Atea Pharmaceuticals, Inc. Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection
CN109890831A (zh) * 2016-08-12 2019-06-14 詹森生物制药有限公司 被取代的核苷、核苷酸以及它们的类似物
CN107759632A (zh) * 2016-08-19 2018-03-06 正大天晴药业集团股份有限公司 一种手性磷酸酯的制备方法
EP4088725A1 (en) 2016-09-07 2022-11-16 ATEA Pharmaceuticals, Inc. 2'-substituted-n6-substituted purine nucleotides for the treatment of a virus from the picornaviridae family
CN109790125B (zh) 2016-09-16 2022-07-05 研究三角协会 四氢异喹啉κ阿片拮抗剂
KR102541080B1 (ko) 2016-10-12 2023-06-08 리서치 트라이앵글 인스티튜트 복소환식 아펠린 수용체(apj) 작용제 및 이의 용도
EP3558996A4 (en) 2016-12-21 2020-08-05 Research Triangle Institute, International DIARYLPURINE DERIVATIVES WITH ENHANCED BIOAVAILABILITY
CN108276463A (zh) * 2017-01-06 2018-07-13 米文君 一类新的化合物及其用途
CN110248951B (zh) 2017-02-01 2022-10-28 阿堤亚制药公司 用于治疗丙型肝炎病毒的核苷酸半硫酸盐
US10682368B2 (en) 2017-03-14 2020-06-16 Gilead Sciences, Inc. Methods of treating feline coronavirus infections
CN115403626A (zh) 2017-05-01 2022-11-29 吉利德科学公司 新结晶形式
WO2019014247A1 (en) 2017-07-11 2019-01-17 Gilead Sciences, Inc. COMPOSITIONS COMPRISING POLYMERASE RNA INHIBITOR AND CYCLODEXTRIN FOR THE TREATMENT OF VIRAL INFECTIONS
CN107987105B (zh) * 2017-11-24 2019-10-01 无锡微色谱生物科技有限公司 一种可用于皮肤敷料的h2s给体化合物、海绵敷料和制备方法
KR102139340B1 (ko) 2017-12-01 2020-07-29 주식회사 엘지생활건강 즉시 주름 개선 및 탄력 증진용 화장료 조성물
US11331331B2 (en) 2017-12-07 2022-05-17 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
WO2019200005A1 (en) 2018-04-10 2019-10-17 Atea Pharmaceuticals, Inc. Treatment of hcv infected patients with cirrhosis
CN110835358B (zh) * 2018-08-16 2022-08-05 上海复星星泰医药科技有限公司 一种索磷布韦中间体的制备方法
AU2019326448A1 (en) 2018-08-20 2021-03-11 Duke University Methods and compositions for drugs to treat ophthalmic diseases
CN110221064A (zh) * 2019-05-23 2019-09-10 南京农业大学 猪塞尼卡谷病毒elisa抗体检测方法及应用
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
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
WO2021173713A1 (en) 2020-02-27 2021-09-02 Atea Pharmaceuticals, Inc. Highly active compounds against covid-19
CN111233929B (zh) * 2020-02-28 2023-02-28 成都阿奇生物医药科技有限公司 一种核苷类似物的氘代物及其制备方法和用途
TWI890963B (zh) 2020-03-12 2025-07-21 美商基利科學股份有限公司 1'-氰基核苷之製備方法
JP7482250B2 (ja) 2020-04-06 2024-05-13 ギリアード サイエンシーズ， インコーポレイテッド １’－シアノ置換カルバヌクレオシド類似体の吸入製剤
CN111467363A (zh) * 2020-04-07 2020-07-31 中国科学院深圳先进技术研究院 索非布韦在制备预防和治疗冠状病毒的药物中的应用
TW202203941A (zh) 2020-05-29 2022-02-01 美商基利科學股份有限公司 瑞德西韋之治療方法
KR102911165B1 (ko) 2020-06-24 2026-01-13 길리애드 사이언시즈, 인코포레이티드 1'-시아노 뉴클레오시드 유사체 및 이의 용도
HRP20240733T1 (hr) 2020-08-27 2024-08-30 Gilead Sciences, Inc. Spojevi i postupci za liječenje virusnih infekcija
CA3174073A1 (en) 2021-06-17 2022-12-17 Atea Pharmaceuticals, Inc. Advantageous anti-hcv combination therapy
CN116217632A (zh) * 2021-12-06 2023-06-06 广州谷森制药有限公司 一种氘代胞苷衍生物的制备方法
CR20240363A (es) 2022-03-02 2024-10-25 Gilead Sciences Inc Compuestos y métodos para el tratamiento de infecciones virales.
IL318465A (en) 2022-07-21 2025-03-01 Antiva Biosciences Inc Compositions and dosage forms for the treatment of HPV infection and HPV-induced neoplasia
US12357577B1 (en) 2024-02-02 2025-07-15 Gilead Sciences, Inc. Pharmaceutical formulations and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012040127A1 (en) * 2010-09-22 2012-03-29 Alios Biopharma, Inc. Substituted nucleotide analogs
WO2012142523A2 (en) * 2011-04-13 2012-10-18 Gilead Sciences, Inc. 1'-substituted pyrimidine n-nucleoside analogs for antiviral treatment
JP2012527477A (ja) * 2009-05-20 2012-11-08 ギリアド ファーマセット エルエルシー Ｎ−［（２’ｒ）−２’−デオキシ−２’−フルオロ−２’−メチル−ｐ−フェニル−５’−ウリジリル］−ｌ−アラニン１−メチルエチルエステルおよびその製造のためのプロセス

Family Cites Families (120)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3480613A (en) 1967-07-03 1969-11-25 Merck & Co Inc 2-c or 3-c-alkylribofuranosyl - 1-substituted compounds and the nucleosides thereof
US3792039A (en) 1971-12-27 1974-02-12 Miles Lab Poly 2'-fluoro-2'-deoxyuridylic acid
US5449664A (en) 1988-11-21 1995-09-12 Syntex (U.S.A.) Inc. Antiviral agents
US6423489B1 (en) 1992-09-10 2002-07-23 Isis Pharmaceuticals, Inc. Compositions and methods for treatment of Hepatitis C virus-associated diseases
US6391542B1 (en) 1992-09-10 2002-05-21 Isis Pharmaceuticals, Inc. Compositions and methods for treatment of Hepatitis C virus-associated diseases
US6433159B1 (en) 1992-09-10 2002-08-13 Isis Pharmaceuticals, Inc. Compositions and methods for treatment of Hepatitis C virus associated diseases
US6174868B1 (en) 1992-09-10 2001-01-16 Isis Pharmaceuticals, Inc. Compositions and methods for treatment of hepatitis C virus-associated diseases
DE69330372T2 (de) 1992-09-10 2002-03-14 Isis Pharmaceuticals, Inc. ZUSAMMENSETZUNGEN UND VERFAHREN FüR DIE BEHANDLUNG VON MIT HEPATITIS C VIREN ASSOZIIERTEN KRANKHEITEN
US5656745A (en) 1993-09-17 1997-08-12 Gilead Sciences, Inc. Nucleotide analogs
EP0719273B1 (en) 1993-09-17 2010-11-03 Gilead Sciences, Inc. Nucleotide analogs
US5798340A (en) 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
SI20076A (sl) 1996-10-16 2000-04-30 Icn Pharmaceuticals, Inc. Monociklični L-nukleozidi, analogi in uporaba od teh
US6316612B1 (en) 1997-08-22 2001-11-13 Ribozyme Pharmaceuticals, Inc. Xylofuranosly-containing nucleoside phosphoramidites and polynucleotides
US6054576A (en) 1997-10-02 2000-04-25 Ribozyme Pharmaceuticals, Inc. Deprotection of RNA
US6617438B1 (en) 1997-11-05 2003-09-09 Sirna Therapeutics, Inc. Oligoribonucleotides with enzymatic activity
US6528640B1 (en) 1997-11-05 2003-03-04 Ribozyme Pharmaceuticals, Incorporated Synthetic ribonucleic acids with RNAse activity
US6127535A (en) 1997-11-05 2000-10-03 Ribozyme Pharmaceuticals, Inc. Nucleoside triphosphates and their incorporation into oligonucleotides
US6482932B1 (en) 1997-11-05 2002-11-19 Ribozyme Pharmaceuticals, Incorporated Nucleoside triphosphates and their incorporation into oligonucleotides
US6339151B1 (en) 1998-01-23 2002-01-15 Newbiotics, Inc. Enzyme catalyzed therapeutic agents
US6030957A (en) 1998-06-29 2000-02-29 Wayne Hughes Institute Aryl phosphate derivatives of d4T having anti-HIV activity
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
PL359169A1 (en) 2000-05-26 2004-08-23 Idenix (Cayman) Limited Methods and compositions for treating flaviviruses and pestiviruses
US20030008841A1 (en) 2000-08-30 2003-01-09 Rene Devos Anti-HCV nucleoside derivatives
CN101862345B (zh) 2000-10-18 2014-06-04 吉利德制药有限责任公司 用于治疗病毒感染和异常细胞增殖的修饰核苷类化合物
US8481712B2 (en) 2001-01-22 2013-07-09 Merck Sharp & Dohme Corp. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
EA007491B1 (ru) 2001-01-22 2006-10-27 Мерк Энд Ко., Инк. Производные нуклеозидов в качестве ингибиторов рнк-зависимой рнк вирусной полимеразы
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
AU2002316118A1 (en) 2001-05-16 2002-11-25 Micrologix Biotech, Inc. Nucleic acid-based compounds and methods of use thereof
GB0114286D0 (en) 2001-06-12 2001-08-01 Hoffmann La Roche Nucleoside Derivatives
WO2003062256A1 (en) 2002-01-17 2003-07-31 Ribapharm Inc. 2'-beta-modified-6-substituted adenosine analogs and their use as antiviral agents
CN1646534A (zh) 2002-02-14 2005-07-27 法玛塞特有限公司 修饰的氟化核苷类似物
CA2484921A1 (en) 2002-05-06 2003-11-13 Genelabs Technologies, Inc. Nucleoside derivatives for treating hepatitis c virus infection
AU2003237249A1 (en) 2002-05-24 2003-12-12 Isis Pharmaceuticals, Inc. Oligonucleotides having modified nucleoside units
US7608600B2 (en) 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
CA2489552A1 (en) 2002-06-28 2004-01-08 Idenix (Cayman) Limited 2'-c-methyl-3'-o-l-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
TW200500374A (en) 2002-06-28 2005-01-01 Idenlx Cayman Ltd 2' and 3' -nucleoside produrgs for treating flavivridae infections
NZ537662A (en) 2002-06-28 2007-10-26 Idenix Cayman Ltd 2'-C-methyl-3'-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
WO2004028454A2 (en) 2002-09-24 2004-04-08 Koronis Pharmaceuticals, Incorporated 1, 3, 5-triazines for treatment of viral diseases
ES2470771T3 (es) 2002-12-12 2014-06-24 Idenix Pharmaceuticals, Inc Procedimiento para la producción de nucle�sidos ramificados en 2'
AR043006A1 (es) 2003-02-12 2005-07-13 Merck & Co Inc Proceso para preparar ribonucleosidos ramificados
US20040229839A1 (en) 2003-05-14 2004-11-18 Biocryst Pharmaceuticals, Inc. Substituted nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
WO2004106356A1 (en) 2003-05-27 2004-12-09 Syddansk Universitet Functionalized nucleotide derivatives
PT1633766T (pt) 2003-05-30 2019-06-04 Gilead Pharmasset Llc Análogos de nucleósido fluorado modificado
GB0317009D0 (en) 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
JP2007509939A (ja) 2003-10-27 2007-04-19 ジェネラブズ テクノロジーズ インコーポレーティッド ウイルス感染を治療するためのヌクレオシド化合物
KR100570697B1 (ko) 2004-09-24 2006-04-12 삼성에스디아이 주식회사 연료 전지 시스템 및 이에 사용되는 개질기
WO2006121820A1 (en) 2005-05-05 2006-11-16 Valeant Research & Development Phosphoramidate prodrugs for treatment of viral infection
WO2007027248A2 (en) 2005-05-16 2007-03-08 Valeant Research & Development 3', 5' - cyclic nucleoside analogues for treatment of hcv
WO2006133353A2 (en) 2005-06-08 2006-12-14 The University Of North Carolina At Chapel Hill Methods of facilitating neural cell survival using non-peptide and peptide bdnf neurotrophin mimetics
EP1928475B1 (en) 2005-08-15 2018-05-23 Riboscience LLC Antiviral phosphoramidates of 4'-c-azido-substituted pronucleotides
US7888330B2 (en) 2005-11-09 2011-02-15 Wayne State University Phosphoramidate derivatives of FAU
US8236904B2 (en) 2005-12-28 2012-08-07 Ethicon, Inc. Bioabsorbable polymer compositions exhibiting enhanced crystallization and hydrolysis rates
US7879815B2 (en) 2006-02-14 2011-02-01 Merck Sharp & Dohme Corp. Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
WO2008005542A2 (en) 2006-07-07 2008-01-10 Gilead Sciences, Inc., Antiviral phosphinate compounds
US7906619B2 (en) 2006-07-13 2011-03-15 Achillion Pharmaceuticals, Inc. 4-amino-4-oxobutanoyl peptides as inhibitors of viral replication
GB0623493D0 (en) 2006-11-24 2007-01-03 Univ Cardiff Chemical compounds
EP2120565B1 (en) 2006-12-20 2012-11-28 Merck Sharp & Dohme Corp. Nucleoside cyclic phosphoramidates for the treatment of rna-dependent rna viral infection
AU2007337983A1 (en) 2006-12-22 2008-07-03 Ablynx N.V. Anti-chemokine (CCL2, CCL3, CCL5, CXCL11, CXCL12) single-domain antibodies
US20080261913A1 (en) 2006-12-28 2008-10-23 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of liver disorders
WO2008085508A2 (en) 2007-01-05 2008-07-17 Merck & Co., Inc. Nucleoside aryl phosphoramidates for the treatment of rna-dependent rna viral infection
EP2121719A2 (en) 2007-01-31 2009-11-25 Alios Biopharma, Inc. 2-5a derivatives and their use as anti-cancer, anti-viral and anti-parasitic agents
US8324179B2 (en) 2007-02-09 2012-12-04 Gilead Sciences, Inc. Nucleoside analogs for antiviral treatment
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
EP1980568A1 (de) 2007-04-13 2008-10-15 Eberhard Karls Universität Tübingen Ethinylierte Heterodinucleosidphosphatanaloga, Verfahren zu deren Herstellung und deren Verwendung
GB0709791D0 (en) 2007-05-22 2007-06-27 Angeletti P Ist Richerche Bio Antiviral agents
WO2009058800A2 (en) 2007-10-29 2009-05-07 President And Fellows Of Harvard College Synthesis of nucleosides
US20090318380A1 (en) 2007-11-20 2009-12-24 Pharmasset, Inc. 2',4'-substituted nucleosides as antiviral agents
WO2009086192A1 (en) 2007-12-21 2009-07-09 Alios Biopharma, Inc. Biodegradable phosphate protected nucleotide derivatives and their use as cancer, anti viral and anti parasitic agents
US20090181921A1 (en) 2007-12-21 2009-07-16 Alios Biopharma Inc. 2-5a analogs and their methods of use
WO2009129120A2 (en) 2008-04-15 2009-10-22 Rfs Pharma, Llc Nucleoside derivatives for treatment of caliciviridae infections, including norovirus infections
US20100003217A1 (en) 2008-07-02 2010-01-07 Erika Cretton-Scott Compounds and Pharmaceutical Compositions for the Treatment of Viral Infections
US8212021B2 (en) 2008-08-08 2012-07-03 Scinopharm Taiwan, Ltd. Process for making 5-azacytosine nucleosides and their derivatives
GB0815968D0 (en) 2008-09-03 2008-10-08 Angeletti P Ist Richerche Bio Antiviral agents
US8163707B2 (en) 2008-09-15 2012-04-24 Enanta Pharmaceuticals, Inc. 4′-allene-substituted nucleoside derivatives
PA8852101A1 (es) 2008-12-08 2010-07-27 Medivir Ab Nucleótidos uracil ciclopropílicos
NZ592705A (en) 2008-12-10 2013-02-22 Achillion Pharmaceuticals Inc 4-amino-4-oxobutanoyl peptide cyclic analogues, inhibitors of viral replication
NZ592668A (en) 2008-12-10 2013-12-20 Achillion Pharmaceuticals Inc New 4-amino-4-oxobutanoyl peptides as inhibitors of viral replication
JP2012514657A (ja) 2009-01-09 2012-06-28 ユニバーシテイ・カレツジ・オブ・カーデイフ・コンサルタンツ・リミテツド ウィルス感染を治療するためのグアノシンヌクレオシド化合物のホスホルアミダート誘導体
BRPI1005401A2 (pt) 2009-02-06 2019-04-02 Rfs Pharma, Llc pro-farmácos de purina nucleosídeo monofosfato para o tratamento de câncer e infecções virais
WO2010108140A1 (en) 2009-03-20 2010-09-23 Alios Biopharma, Inc. Substituted nucleoside and nucleotide analogs
WO2010108135A1 (en) 2009-03-20 2010-09-23 Alios Biopharma, Inc. Protected nucleotide analogs
JO3027B1 (ar) 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TW201107342A (en) 2009-05-20 2011-03-01 Chimerix Inc Compounds, compositions and methods for treating viral infection
WO2011097607A1 (en) 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
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
WO2011123668A2 (en) 2010-03-31 2011-10-06 Pharmasset, Inc. Stereoselective synthesis of phosphorus containing actives
EP2552203B1 (en) 2010-04-01 2017-03-22 Idenix Pharmaceuticals LLC. Compounds and pharmaceutical compositions for the treatment of viral infections
US9090642B2 (en) * 2010-07-19 2015-07-28 Gilead Sciences, Inc. Methods for the preparation of diasteromerically pure phosphoramidate prodrugs
WO2012016994A1 (en) 2010-08-04 2012-02-09 Herbert Schott Bone-targeting bisphosphonate duplex drugs
US20120070411A1 (en) 2010-09-22 2012-03-22 Alios Biopharma, Inc. Substituted nucleotide analogs
EP2619215B1 (en) 2010-09-22 2018-09-05 Alios Biopharma, Inc. Azido nucleosides and nucleotide analogs
AR083221A1 (es) 2010-09-29 2013-02-06 Univ Nac Quilmes Proceso para producir dialquilfosfotriesteres de nucleosidos mediante transesterificacion enzimatica y desproteccion de los mismos para producir nucleosidos monofosfato
US9006209B2 (en) 2010-11-10 2015-04-14 Janssen Products, Lp Uracyl spirooxetane nucleoside phosphoramidates
EP2646453A1 (en) 2010-11-30 2013-10-09 Gilead Pharmasset LLC Compounds
EP2655392B1 (en) 2010-12-22 2018-04-18 Alios Biopharma, Inc. Cyclic nucleotide analogs
WO2012092484A2 (en) 2010-12-29 2012-07-05 Inhibitex, Inc. Substituted purine nucleosides, phosphoroamidate and phosphorodiamidate derivatives for treatment of viral infections
US9156874B2 (en) 2011-01-03 2015-10-13 Nanjing Molecular Research, Inc. Double-liver-targeting phosphoramidate and phosphonoamidate prodrugs
CN103403014B (zh) 2011-01-03 2016-07-06 河南美泰宝生物制药有限公司 O-(经取代的苯甲基)氨基磷酸酯化合物及其治疗用途
US9085599B2 (en) 2011-03-16 2015-07-21 Enanta Pharmaceuticals, Inc. 2′allene-substituted nucleoside derivatives
CA2843324A1 (en) 2011-03-31 2012-11-15 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
EP2697242B1 (en) 2011-04-13 2018-10-03 Merck Sharp & Dohme Corp. 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
JP2014515023A (ja) 2011-04-13 2014-06-26 メルク・シャープ・アンド・ドーム・コーポレーション ２’−置換ヌクレオシド誘導体およびウイルス疾患の処置のためのその使用方法
CN103687866A (zh) 2011-05-19 2014-03-26 Rfs制药公司 用于治疗病毒性感染的嘌呤单磷酸酯前药
EA029099B1 (ru) 2011-05-27 2018-02-28 Ачиллион Фармасьютикалз, Инк. Замещенные циклофаны для использования при лечении инфекции вгс
KR20140064765A (ko) 2011-06-30 2014-05-28 스텔라 에이피에스 Hcv 조합 치료
US9416154B2 (en) 2011-07-13 2016-08-16 Merck Sharp & Dohme Corp. 5′-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
EP2731433A4 (en) 2011-07-13 2014-12-31 Merck Sharp & Dohme 5'-SUBSTITUTED NUCLEOSIDE ANALOGA AND METHOD FOR THEIR USE FOR THE TREATMENT OF VIRUS DISEASES
WO2013024155A1 (en) 2011-08-17 2013-02-21 Inserm (Institut National De La Sante Et De La Recherche Medicale) Combinations of anti-hcv-entry factor antibodies and direct acting antivirals for the treatment and the prevention of hcv infection
AU2012298750A1 (en) 2011-08-24 2014-03-13 Glaxosmithkline Llc Combination treatments for Hepatitis C
US9403863B2 (en) 2011-09-12 2016-08-02 Idenix Pharmaceuticals Llc Substituted carbonyloxymethylphosphoramidate compounds and pharmaceutical compositions for the treatment of viral infections
JP2014526474A (ja) 2011-09-12 2014-10-06 アイディニックス ファーマシューティカルズ インコーポレイテッド ウイルス感染の治療のための化合物および薬学的組成物
EP2755689A1 (en) 2011-09-16 2014-07-23 AbbVie Inc. Methods for treating hcv
WO2013044030A1 (en) 2011-09-23 2013-03-28 Enanta Pharmaceuticals, Inc. 2'-chloroacetylenyl substituted nucleoside derivatives
US8507460B2 (en) 2011-10-14 2013-08-13 Idenix Pharmaceuticals, Inc. Substituted 3′,5′-cyclic phosphates of purine nucleotide compounds and pharmaceutical compositions for the treatment of viral infections
WO2013066991A1 (en) 2011-10-31 2013-05-10 Inhibitex, Inc. Crystalline solvates of nucleoside phosphoroamidates, their stereoselective preparation, novel intermediates thereof, and their use in the treatment of viral disease
US20130244966A1 (en) 2011-12-12 2013-09-19 Catabasis Pharmaceuticals, Inc. Fatty acid antiviral conjugates and their uses
US20130172240A1 (en) 2011-12-28 2013-07-04 Abbvie Inc. Methods for treating hcv
CA2857339C (en) 2011-12-29 2015-11-17 Abbvie Inc. Solid compositions comprising an hcv inhibitor
WO2013133927A1 (en) 2012-02-13 2013-09-12 Idenix Pharmaceuticals, Inc. Pharmaceutical compositions of 2'-c-methyl-guanosine, 5'-[2-[(3-hydroxy-2,2-dimethyl-1-oxopropyl)thio]ethyl n-(phenylmethyl)phosphoramidate]

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012527477A (ja) * 2009-05-20 2012-11-08 ギリアド ファーマセット エルエルシー Ｎ−［（２’ｒ）−２’−デオキシ−２’−フルオロ−２’−メチル−ｐ−フェニル−５’−ウリジリル］−ｌ−アラニン１−メチルエチルエステルおよびその製造のためのプロセス
WO2012040127A1 (en) * 2010-09-22 2012-03-29 Alios Biopharma, Inc. Substituted nucleotide analogs
WO2012142523A2 (en) * 2011-04-13 2012-10-18 Gilead Sciences, Inc. 1'-substituted pyrimidine n-nucleoside analogs for antiviral treatment

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