TW444020B - Nucleotide analogs - Google Patents

Nucleotide analogs Download PDF

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Publication number
TW444020B
TW444020B TW086110757A TW86110757A TW444020B TW 444020 B TW444020 B TW 444020B TW 086110757 A TW086110757 A TW 086110757A TW 86110757 A TW86110757 A TW 86110757A TW 444020 B TW444020 B TW 444020B
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TW
Taiwan
Prior art keywords
alkyl
independently
alkenyl
alkynyl
aryl
Prior art date
Application number
TW086110757A
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English (en)
Inventor
Murty N Arimilli
Kenneth C Cundy
Joseph P Dougherty
Reza Oliyai
Choung Un Kim
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Gilead Sciences Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26696272&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW444020(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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Publication of TW444020B publication Critical patent/TW444020B/zh

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    • 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
    • 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
    • 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
    • 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
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Description

444020 A8 B8 C8 六、申請專利範圍
與L-CHR2-0-C(0)-0R /反應後回收式（1)化合物，其中B是 鳥糞嘌呤-9-基，腺嘌呤-9-基，2,6-二胺基嘌呤-9-基，2-胺基 嘌玲-9-基或其1-去氮，3-去氮，或8-氮基類似物，或b是 胞嘧啶-1-基； R1 是氫，-CH3, -CH2〇H, -CH2F，-CH = CH2, -CH2N3 或 R1 與R8連結形成-CH2-;及 R8 是氫，-CHR2-0-C(0)-0R > 或 R8 與 R1 連結形成 _CH2_; R2是H.CVCu烷基，芳基，烯基，炔基，烯芳基，炔芳 基，烷芳基，芳炔基，芳烯基或芳烷基，其係未經取代或 經鹵基，疊氮基，硝基或〇113(113爲Ci-Cu烷基）取代； R /分別是H，G-Cu烷基，芳基，烯基，炔基，烯芳基， 炔芳基，烷芳基，芳炔基，芳烯基或芳烷基，其係未經取 代或經鹵基，疊氮基，硝基或OR3取代，惟至少一個R-不 是Η ;及 L是離去基。 18.如申請專利範圍第17項之方法，該方法包括用至少 約1.0當量之l-chr2-o-c(o)-〇r/進行反應。 i 9.如申請專利範圍第17項之方法，該方法包括在有機 鹼存在下，於有機溶劑中及反應溫度約4-lOOt：進行反應約 4-72小時。 本紙張尺度適用中國國家梯準（CNS ) A4规格（210X 297公着）-4- (請先聞靖背面之注意事項再填寫本頁) 訂 Ψ. 經濟部智慧財產局員工消費合作社印製 444020 A6 B8 C8 D8 六、申請專利範圍 20. 如申請專利範圍第17項之方法 形成鹽類後沈澱回收。 21. 如申請專利範圍第20項之方法 酸、磷酸、乳酸或檸檬酸。 22.—種具有下式之化合物 其中式（1)化合物 其中該鹽類得自硫
〇 〇、/ 3 CH2〆 c 、CH3 •〇-CH2^C c -ch3 0 \h. (請先閲请背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 本纸張尺度適用中國國家揉準（CNS ) A4規格（210X297公釐）-5 -
TW086110757A 1996-07-26 1997-08-21 Nucleotide analogs TW444020B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2270896P 1996-07-26 1996-07-26
US68683896A 1996-07-26 1996-07-26

Publications (1)

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TW444020B true TW444020B (en) 2001-07-01

Family

ID=26696272

Family Applications (2)

Application Number Title Priority Date Filing Date
TW089123708A TW470748B (en) 1996-07-26 1997-08-21 Nucleotide analogs
TW086110757A TW444020B (en) 1996-07-26 1997-08-21 Nucleotide analogs

Family Applications Before (1)

Application Number Title Priority Date Filing Date
TW089123708A TW470748B (en) 1996-07-26 1997-08-21 Nucleotide analogs

Country Status (4)

Country Link
JP (6) JP4033494B2 (zh)
CA (1) CA2261619C (zh)
TW (2) TW470748B (zh)
WO (1) WO1998004569A1 (zh)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4033494B2 (ja) * 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 ヌクレオチドアナログ
EP1243593B1 (en) * 1997-07-25 2005-09-21 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
PT1256584E (pt) * 1997-07-25 2004-12-31 Gilead Sciences Inc Processo para a preparacao de adefovir-dipivoxil
BR9811045A (pt) * 1997-07-25 2000-08-22 Gilead Sciences Inc Composição de análogo de nucleotìdeo e processo de sìntese
CA2335617C (en) * 1998-06-24 2009-12-15 Emory University Use of 3'-azido-2',3'-dideoxyuridine in combination with further anti-hiv drugs for the manufacture of a medicament for the treatment of hiv
AU2001282941C1 (en) * 2000-07-21 2016-12-22 Gilead Sciences, Inc. Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
BR0309557A (pt) 2002-04-26 2005-03-01 Gilead Sciences Inc Inibidores da transcriptase reversa não nucleosìdeos
ATE398455T1 (de) 2003-01-14 2008-07-15 Gilead Sciences Inc Zusammensetzungen und verfahren zur antiviralen kombinationstherapie
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
US7427636B2 (en) 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
EA014685B1 (ru) 2003-04-25 2010-12-30 Джилид Сайэнс, Инк. Фосфонатсодержащие антивирусные соединения (варианты) и фармацевтическая композиция на их основе
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer 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
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
AU2004233897A1 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
WO2004096285A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
CN1805966B (zh) 2003-06-16 2013-03-13 捷克科学院有机化学和生物化学研究所 作为抗病毒核苷酸类似物的含膦酸酯基团的嘧啶化合物
EP1678321A1 (en) 2003-10-24 2006-07-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
US7432273B2 (en) 2003-10-24 2008-10-07 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
US7427624B2 (en) 2003-10-24 2008-09-23 Gilead Sciences, Inc. Purine nucleoside phosphorylase inhibitory phosphonate compounds
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
MXPA06007095A (es) * 2003-12-22 2006-09-04 Gilead Sciences Inc Conjugados de fosfonato inhibidores de cinasa.
UA88313C2 (ru) 2004-07-27 2009-10-12 Гилиад Сайенсиз, Инк. Фосфонатные аналоги соединений ингибиторов вич
US20100216822A1 (en) * 2005-06-13 2010-08-26 Brightgene Bio-Medical Technology Co., Ltd. Nucleotide Analogue Prodrug and the Preparation Thereof
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
CN101940571A (zh) 2007-04-13 2011-01-12 南方研究所 抗血管生成剂和使用方法
US20090270352A1 (en) * 2007-05-22 2009-10-29 Ultimorphix Technologies B.V. Tenofovir Disoproxil Hemi-Fumaric Acid Co-Crystal
WO2009064174A1 (en) * 2007-11-14 2009-05-22 Ultimorphix Technologies B.V. Polymorphic form of tenofovir disoproxil fumarate, method for its preparation and use
JP5757860B2 (ja) * 2008-04-25 2015-08-05 シプラ・リミテッド 結晶形態のテノホビルジソプロキシル及びその製造方法
EA018308B1 (ru) 2008-07-08 2013-07-30 Джилид Сайэнс, Инк. Соли соединений ингибиторов вич
CN102093422B (zh) 2009-12-10 2015-02-25 中国人民解放军军事医学科学院毒物药物研究所 无环核苷膦酸酯衍生物及其医药用途
US20140073607A1 (en) * 2011-05-10 2014-03-13 Okapi Sciences Nv Compounds for use in the treatment of feline retroviral infections
US8754065B2 (en) 2011-08-16 2014-06-17 Gilead Sciences, Inc. Tenofovir alafenamide hemifumarate
CN103626802A (zh) * 2012-08-23 2014-03-12 重庆药友制药有限责任公司 一种制备替诺福韦的新方法
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
US9227990B2 (en) 2012-10-29 2016-01-05 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
EP2860184B1 (en) 2013-10-09 2018-08-29 Zentiva, k.s. Dihydrogenphosphate salt of Tenofovir disoproxil
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
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
PL3661937T3 (pl) 2017-08-01 2021-12-20 Gilead Sciences, Inc. Formy krystaliczne ((s)-((((2r,5r)-5-(6-amino-9h-puryn-9-ylo)-4-fluoro-2,5-dihydrofuran-2-ylo)oksy)metylo)(fenoksy)fosforylo)-l-alaninianu etylu (gs-9131) do leczenia zakażeń wirusowych
CN107805202A (zh) * 2017-12-01 2018-03-16 内蒙古圣氏化学股份有限公司 一种氯甲基异丙基碳酸酯连续化反应装置及方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL84477A (en) * 1986-11-18 1995-12-08 Bristol Myers Squibb Co History of Phosphonomethoxyalkylene Purinopyrimidine and Pharmaceutical Preparations Containing Them
EP0481214B1 (en) * 1990-09-14 1998-06-24 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
GB9026164D0 (en) * 1990-12-01 1991-01-16 Beecham Group Plc Pharmaceuticals
AU691527B2 (en) * 1993-09-17 1998-05-21 Gilead Sciences, Inc. Nucleotide analogs
JP4033494B2 (ja) * 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 ヌクレオチドアナログ

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Publication number Publication date
WO1998004569A1 (en) 1998-02-05
CA2261619C (en) 2006-05-23
JP2015164934A (ja) 2015-09-17
CA2261619A1 (en) 1998-02-05
JP4033494B2 (ja) 2008-01-16
JP2017031212A (ja) 2017-02-09
JP2007297406A (ja) 2007-11-15
JP2000515866A (ja) 2000-11-28
TW470748B (en) 2002-01-01
JP2014159450A (ja) 2014-09-04
JP2011016847A (ja) 2011-01-27

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