KR101115210B1 - 신규 시타라빈 모노포스페이트 전구약물 - Google Patents

신규 시타라빈 모노포스페이트 전구약물 Download PDF

Info

Publication number
KR101115210B1
KR101115210B1 KR1020057007626A KR20057007626A KR101115210B1 KR 101115210 B1 KR101115210 B1 KR 101115210B1 KR 1020057007626 A KR1020057007626 A KR 1020057007626A KR 20057007626 A KR20057007626 A KR 20057007626A KR 101115210 B1 KR101115210 B1 KR 101115210B1
Authority
KR
South Korea
Prior art keywords
compound
formula iii
liver
pharmaceutical composition
cytarabine
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 - Fee Related
Application number
KR1020057007626A
Other languages
English (en)
Korean (ko)
Other versions
KR20050083879A (ko
Inventor
세르쥐 아쉬. 보이에르
마크 디. 에리온
Original Assignee
메타베이시스 테라퓨틱스, 인크.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 메타베이시스 테라퓨틱스, 인크. filed Critical 메타베이시스 테라퓨틱스, 인크.
Publication of KR20050083879A publication Critical patent/KR20050083879A/ko
Application granted granted Critical
Publication of KR101115210B1 publication Critical patent/KR101115210B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

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
    • 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
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65742—Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
KR1020057007626A 2002-10-31 2003-10-31 신규 시타라빈 모노포스페이트 전구약물 Expired - Fee Related KR101115210B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US42321102P 2002-10-31 2002-10-31
US42325902P 2002-10-31 2002-10-31
US60/423,211 2002-10-31
US60/423,259 2002-10-31
PCT/US2003/034690 WO2004041837A1 (en) 2002-10-31 2003-10-31 Novel cytarabine monophosphate prodrugs

Publications (2)

Publication Number Publication Date
KR20050083879A KR20050083879A (ko) 2005-08-26
KR101115210B1 true KR101115210B1 (ko) 2012-04-12

Family

ID=32314479

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020057007605A Expired - Fee Related KR101026294B1 (ko) 2002-10-31 2003-10-31 1,3-프로판-1-아릴 디올의 신규 시클릭 포스페이트디에스테르 및 프로드럭 제조에서의 이들의 용도
KR1020057007626A Expired - Fee Related KR101115210B1 (ko) 2002-10-31 2003-10-31 신규 시타라빈 모노포스페이트 전구약물

Family Applications Before (1)

Application Number Title Priority Date Filing Date
KR1020057007605A Expired - Fee Related KR101026294B1 (ko) 2002-10-31 2003-10-31 1,3-프로판-1-아릴 디올의 신규 시클릭 포스페이트디에스테르 및 프로드럭 제조에서의 이들의 용도

Country Status (13)

Country Link
US (4) US7148349B2 (enExample)
EP (2) EP1556393B1 (enExample)
JP (2) JP4689274B2 (enExample)
KR (2) KR101026294B1 (enExample)
AT (1) ATE442375T1 (enExample)
AU (2) AU2003286816B2 (enExample)
BR (2) BR0315795A (enExample)
CA (2) CA2503729C (enExample)
DE (1) DE60329211D1 (enExample)
IL (2) IL167984A (enExample)
MX (2) MXPA05004504A (enExample)
PL (2) PL376474A1 (enExample)
WO (2) WO2004041834A2 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
JP4476811B2 (ja) * 2002-05-13 2010-06-09 メタバシス・セラピューティクス・インコーポレイテッド Ｐｍｅａおよびそのアナログの新規ホスホン酸系プロドラッグ
JP4332496B2 (ja) 2002-05-13 2009-09-16 メタバシス・セラピューティクス・インコーポレイテッド Ｐｍｅａおよびｐｍｐａ環生成合成
JP4689274B2 (ja) * 2002-10-31 2011-05-25 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 新規なシタラビン・モノホスフェートプロドラッグ
US20050182252A1 (en) * 2004-02-13 2005-08-18 Reddy K. R. Novel 2'-C-methyl nucleoside derivatives
MXPA06014013A (es) 2004-06-08 2007-03-15 Metabasis Therapeutics Inc Sintesis mediada por acidos de lewis de esteres ciclicos.
BRPI0615157A2 (pt) * 2005-08-12 2016-09-13 Merck & Co Inc composto, composição farmacêutica, métodos para inibir a replicação viral em um paciente humano, e para tratar uma infecção viral em um paciente humano, e, uso de um composto
US20070241502A1 (en) * 2006-04-14 2007-10-18 Campbell Darrell C Poker game and apparatus for play thereof
US7584968B2 (en) * 2006-04-14 2009-09-08 Seven Generations, Inc. Poker game and apparatus for play thereof
WO2009073506A2 (en) * 2007-11-29 2009-06-11 Metabasis Therapeutics Inc. Nucleoside prodrugs and uses thereof
AR069740A1 (es) * 2007-11-29 2010-02-17 Metabasis Therapeutics Inc Compuestos nucleosidos antivirales
CA2975841C (en) 2008-04-30 2021-05-25 Siemens Medical Solutions Usa, Inc. Substrate based pet imaging agents
CN101787064B (zh) * 2009-01-23 2013-03-13 高峰 阿糖胞苷衍生物及其在抗癌抗肿瘤中的用途
US20130059952A1 (en) * 2010-01-15 2013-03-07 Basf Se Phospho-substituted alkoxyamine compounds
WO2011113174A1 (zh) * 2010-03-15 2011-09-22 Gao Feng 阿糖胞苷衍生物及其在抗癌抗肿瘤中的用途
RU2732440C2 (ru) * 2013-06-24 2020-09-16 Кэнбас Ко., Лтд. Пептиды и пептидомиметики для комбинированного применения и лечения в субпопуляциях пациентов с раковыми заболеваниями
GB201317166D0 (en) * 2013-09-27 2013-11-06 Astex Therapeutics Ltd Pharmaceutical compounds
WO2015123352A1 (en) 2014-02-13 2015-08-20 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
WO2016003812A1 (en) 2014-07-02 2016-01-07 Ligand Pharmaceuticals, Inc. Prodrug compounds and uses therof
WO2017024310A1 (en) 2015-08-06 2017-02-09 Chimerix, Inc. Pyrrolopyrimidine nucleosides and analogs thereof useful as antiviral agents
US12064445B2 (en) 2015-12-03 2024-08-20 Biosight Ltd. Cytarabine conjugates for cancer therapy
JP2018535987A (ja) * 2015-12-03 2018-12-06 バイオサイト リミテッド 癌療法のためのコンジュゲートの塩
BR112018011177A2 (pt) 2015-12-03 2018-11-21 Biosight Ltd conjugados de citarabina para terapia de câncer
US12071450B2 (en) 2015-12-03 2024-08-27 Biosight Ltd. Salts of conjugates for cancer therapy
JP6775591B2 (ja) * 2016-09-20 2020-10-28 株式会社島津製作所 両親媒性ブロックポリマーを用いた薬剤内包分子集合体
WO2019060692A1 (en) 2017-09-21 2019-03-28 Chimerix, Inc. MORPHIC FORMS OF 4-AMINO-7- (3,4-DIHYDROXY-5- (HYDROXYMETHYL) -ETRAHYDROFURAN-2-YL) -2-METHYL-7H-PYRROLO [2,3-D] PYRIMIDINE-5-CARBOXAMIDE AND THEIR USES
CN109956985A (zh) * 2017-12-22 2019-07-02 浙江柏拉阿图医药科技有限公司 肝递送阿糖胞苷前体药物核苷环磷酸酯化合物及应用
RU2020126177A (ru) 2018-01-09 2022-02-10 Лиганд Фармасьютикалз, Инк. Ацетальные соединения и их терапевтическое применение

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL99688C (enExample) * 1956-12-20
US3116282A (en) 1960-04-27 1963-12-31 Upjohn Co Pyrimidine nucleosides and process
US3328388A (en) 1964-09-02 1967-06-27 Merck & Co Inc Arabinofuranosyl pyrimidines and methods of preparing same
US4440740A (en) 1982-04-26 1984-04-03 Merck & Co., Inc. α-Keto aldehydes as enhancing agents of gastro-intestinal drug absorption
US4579849A (en) 1984-04-06 1986-04-01 Merck & Co., Inc. N-alkylguanine acyclonucleosides as antiviral agents
FR2562543B1 (fr) * 1984-04-10 1987-09-25 Elf Aquitaine Nouveaux phosphonites cycliques, leur preparation et applications
US4749694A (en) * 1984-04-26 1988-06-07 Merck & Co., Inc. Novel lysine esters used as absorption
US4537772A (en) * 1984-05-02 1985-08-27 Merck & Co., Inc. Enhancing absorption of drugs from gastrointestinal tract using acylcarnitines
NL8403224A (nl) 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
US4729989A (en) * 1985-06-28 1988-03-08 Merck & Co., Inc. Enhancement of absorption of drugs from gastrointestinal tract using choline ester salts
US4822773A (en) * 1985-06-28 1989-04-18 Merck & Co., Inc. Enhancement of absorption of drugs from gastrointestinal tract using choline ester salts
US4973579A (en) * 1985-06-28 1990-11-27 Merck & Co., Inc. Enhancment of absorption of drugs from gastrointestinal tract using choline ester salts
US4847298A (en) * 1985-08-16 1989-07-11 Merck & Co., Inc. Acylcarnitines as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal compartments
US4963556A (en) * 1985-08-16 1990-10-16 Merck & Co., Inc. Choline esters as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal cavities
US4963525A (en) * 1985-08-16 1990-10-16 Merck & Co., Inc. Acylcarnitines as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal compartments
US4692441A (en) * 1985-08-16 1987-09-08 Merck & Co., Inc. Chorine esters as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal cavities
US4731360A (en) 1985-08-16 1988-03-15 Merck & Co., Inc. Acylcarnitines as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal compartments
US5159067A (en) 1987-01-28 1992-10-27 University Of Georgia Research Foundation Inc. 5'-Diphosphohexose nucleoside pharmaceutical compositions
US5077280A (en) * 1988-04-12 1991-12-31 Brown University Research Foundation Treatment of viral infections
EP0338372A3 (en) 1988-04-22 1991-10-09 American Cyanamid Company Solubilized pro-drugs
ATE128623T1 (de) 1988-08-02 1995-10-15 Nissan Chemical Ind Ltd Mittel zur verbesserung von arzneimitteleffekten für antitumormittel.
US5658889A (en) * 1989-01-24 1997-08-19 Gensia Pharmaceuticals, Inc. Method and compounds for aica riboside delivery and for lowering blood glucose
US5118672A (en) * 1989-07-10 1992-06-02 University Of Georgia Research Foundation 5'-diphosphohexose nucleoside pharmaceutical compositions
JP3347723B2 (ja) 1990-06-13 2002-11-20 グラツィエル，アーノルド 含リンプロドラッグ
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
WO1993016388A1 (en) 1992-02-13 1993-08-19 The Uab Research Foundation Method of detecting and monitoring levels of 3'-amino-3'-deoxythymidine in body fluids and antibodies for same
GB2266527A (en) 1992-03-17 1993-11-03 Merck & Co Inc Substituted azetidinones useful in the treatment of leukemia
GB2266525A (en) 1992-03-17 1993-11-03 Merck & Co Inc Substituted cephalosporin sulfone compositions useful in the treatment of leukemia
JP4117901B2 (ja) 1993-05-21 2008-07-16 アメリカ合衆国 デオキシヌクレオチド合成の阻害剤を使用することによって逆転写酵素依存ウイルスの複製を阻害する新規な方法
DE69426904T2 (de) 1993-06-29 2001-10-11 Mitsubishi Chemical Corp., Tokio/Tokyo Phosphonat-Nukleotid Ester-Derivate
US5567689A (en) 1993-08-13 1996-10-22 The Uab Research Foundation Methods for increasing uridine levels with L-nucleosides
US20020120130A1 (en) 1993-09-10 2002-08-29 Gilles Gosselin 2' or 3' -deoxy and 2', 3' -dideoxy-beta-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti- viral agents
FR2709754B1 (fr) 1993-09-10 1995-12-01 Centre Nat Rech Scient Composés 2' ou 3'-déoxy- et 2', 3'-didéoxy-beta-L-pentofuranonucléosides, procédé de préparation et application thérapeutique, notamment anti-virale.
WO1995007086A1 (en) 1993-09-10 1995-03-16 Emory University Nucleosides with anti-hepatitis b virus activity
CA2171743C (en) 1993-09-17 2007-11-20 Norbert W. Bischofberger Nucleotide analogs
US5437772A (en) 1993-11-01 1995-08-01 The Electrosynthesis Co., Inc. Portable lead detector
US5866679A (en) * 1994-06-28 1999-02-02 Merck & Co., Inc. Peptides
US5599686A (en) 1994-06-28 1997-02-04 Merck & Co., Inc. Peptides
US6143864A (en) 1994-06-28 2000-11-07 Merck & Co., Inc. Peptides
DE69520360T2 (de) 1994-07-04 2001-08-09 Takeda Chemical Industries, Ltd. Phosphonsäure verbindungen imre herstellung und verwendung
US5665713A (en) 1995-04-12 1997-09-09 Procter & Gamble Company Pharmaceutical composition for inhibiting the growth of viruses and cancers
AU722214B2 (en) * 1995-06-07 2000-07-27 Centre National De La Recherche Scientifique (Cnrs) Nucleosides with anti-hepatitis B virus activity
WO1997003679A1 (en) 1995-07-17 1997-02-06 Cephalon, Inc. Phosphorous-containing cysteine and serine protease inhibitors
US5750493A (en) 1995-08-30 1998-05-12 Raymond F. Schinazi Method to improve the biological and antiviral activity of protease inhibitors
RU2111970C1 (ru) 1996-06-25 1998-05-27 Иван Игоревич Федоров 3'-оксимино-2',3'-дидезоксинуклеозиды
US6177404B1 (en) 1996-10-15 2001-01-23 Merck & Co., Inc. Conjugates useful in the treatment of benign prostatic hyperplasia
US5948750A (en) 1996-10-30 1999-09-07 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
WO1998039342A1 (en) 1997-03-07 1998-09-11 Metabasis Therapeutics, Inc. Novel indole and azaindole inhibitors of fructose-1,6-bisphosphatase
AU6452098A (en) * 1997-03-07 1998-09-22 Metabasis Therapeutics, Inc. Novel purine inhibitors of fructose-1,6-bisphosphatase
ZA981936B (en) * 1997-03-07 1999-09-06 Metabasis Therapeutics Inc Novel benzimidazole inhibitors of fructose 1,6-bisphosphatase.
US6130504A (en) 1997-07-11 2000-10-10 Sharp Kabushiki Kaisha Plasma addressing display device and method for producing the same
US6391305B1 (en) 1997-09-10 2002-05-21 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
US20020115596A1 (en) 1997-10-27 2002-08-22 Merk & Co., Inc. Conjugates useful in the treatment of prostate cancer
WO1999045016A2 (en) * 1998-03-06 1999-09-10 Metabasis Therapeutics, Inc. Novel prodrugs for phosphorus-containing compounds
AU4716299A (en) 1998-06-24 2000-01-10 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
IT1305313B1 (it) 1998-07-17 2001-05-04 Colla Paolo 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1.
DE69929060T2 (de) 1998-08-10 2006-08-31 Idenix (Cayman) Ltd. Beta-l-2'-deoxynukleoside für die behandlung von hepatitis b virus
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
DE69910045T2 (de) * 1998-09-09 2004-04-22 Metabasis Therapeutics Inc., San Diego Neue heteroaromatische fructose 1,6-bisphosphatase inhibitoren
KR100618028B1 (ko) 1998-11-05 2006-08-30 쌍트르 나쉬오날 드 라 르쉐르스 쉬앙티피끄 항-ｂ형 간염 활성을 가진 뉴클레오시드
US6407077B1 (en) * 1998-11-05 2002-06-18 Emory University β-L nucleosides for the treatment of HIV infection
EP1165570B9 (en) 1999-03-05 2007-02-21 Metabasis Therapeutics, Inc. Novel phosphorus-containing prodrugs
WO2001018013A1 (en) * 1999-09-08 2001-03-15 Metabasis Therapeutics, Inc. Prodrugs for liver specific drug delivery
EP1253921A4 (en) 2000-01-28 2004-10-13 Merck & Co Inc TREATMENT AND PROPHYLAXIS OF PROSTATE CANCER WITH COX-2 SELECTIVE INHIBITORS
WO2001060365A1 (en) * 2000-02-17 2001-08-23 Merck & Co., Inc. Treatment or prevention of prostate cancer with a cox-2 selective inhibiting drug
MY164523A (en) * 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
YU92202A (sh) * 2000-05-26 2006-01-16 Idenix (Cayman) Limited Metode i smeše za lečenje flavi virusa i pesti virusa
DE60105424T2 (de) * 2000-05-26 2005-09-22 Idenix (Cayman) Ltd. Methoden zur behandlung von delta hepatitis virus infektionen mit beta-l-2' deoxy-nucleosiden
US6875751B2 (en) * 2000-06-15 2005-04-05 Idenix Pharmaceuticals, Inc. 3′-prodrugs of 2′-deoxy-β-L-nucleosides
BR0115474A (pt) 2000-11-17 2006-01-31 Idenix Cayman Ltd Composição e método para inibição da transmissão de hiv que usam 6-benzil-4-oxopirimidinas substituìdas aplicada por via tópica
CN1267446C (zh) * 2001-01-22 2006-08-02 默克公司 作为依赖于rna的rna病毒聚合酶的抑制剂的核苷衍生物
AR035857A1 (es) * 2001-04-11 2004-07-21 Novirio Pharmaceuticals Ltd Fenilindoles; sus composiciones farmaceuticas y sus usos
US20030232760A1 (en) 2001-09-21 2003-12-18 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
JP2005504087A (ja) 2001-09-28 2005-02-10 イデニクス（ケイマン）リミテツド ４’が修飾されたヌクレオシドを使用するｃ型肝炎ウイルス治療のための方法および組成物
WO2003026675A1 (en) 2001-09-28 2003-04-03 Idenix (Cayman) Limited Methods and compositions for treating flaviviruses and pestiviruses using 4'-modified nucleoside
JP4332496B2 (ja) 2002-05-13 2009-09-16 メタバシス・セラピューティクス・インコーポレイテッド Ｐｍｅａおよびｐｍｐａ環生成合成
JP4476811B2 (ja) 2002-05-13 2010-06-09 メタバシス・セラピューティクス・インコーポレイテッド Ｐｍｅａおよびそのアナログの新規ホスホン酸系プロドラッグ
PT1523489E (pt) 2002-06-28 2014-06-24 Centre Nat Rech Scient Profármacos de nucleósido modificado em 2' e 3' para tratamento de infecções por flaviridae
KR20050055630A (ko) 2002-06-28 2005-06-13 이데닉스 (케이만) 리미티드 플라비비리다에 감염 치료를 위한 1'-, 2'- 및 3'-변형된뉴클레오시드 유도체
AU2003248748A1 (en) 2002-06-28 2004-01-19 Idenix (Cayman) Limited 2'-c-methyl-3'-o-l-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
JP4689274B2 (ja) 2002-10-31 2011-05-25 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 新規なシタラビン・モノホスフェートプロドラッグ

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds

Also Published As

Publication number Publication date
AU2003287389B2 (en) 2010-08-12
JP5046219B2 (ja) 2012-10-10
US20040092476A1 (en) 2004-05-13
CA2503729A1 (en) 2004-05-21
PL376474A1 (en) 2005-12-27
IL167990A (en) 2010-12-30
BR0315806A (pt) 2005-09-13
WO2004041834A2 (en) 2004-05-21
US20070037774A1 (en) 2007-02-15
US7553826B2 (en) 2009-06-30
JP4689274B2 (ja) 2011-05-25
KR101026294B1 (ko) 2011-03-31
CA2503729C (en) 2012-09-18
CA2503730A1 (en) 2004-05-21
WO2004041837A1 (en) 2004-05-21
JP2006504791A (ja) 2006-02-09
ATE442375T1 (de) 2009-09-15
CA2503730C (en) 2011-10-18
WO2004041834A3 (en) 2004-07-01
US7151092B2 (en) 2006-12-19
US7148349B2 (en) 2006-12-12
MXPA05004504A (es) 2005-08-16
EP1556398A1 (en) 2005-07-27
IL167984A (en) 2011-09-27
US20040192651A1 (en) 2004-09-30
AU2003286816A1 (en) 2004-06-07
EP1556393B1 (en) 2013-12-25
AU2003286816B2 (en) 2010-08-19
PL376327A1 (en) 2005-12-27
KR20050072776A (ko) 2005-07-12
US7498320B2 (en) 2009-03-03
PL212929B1 (pl) 2012-12-31
BR0315795A (pt) 2005-09-13
EP1556398B1 (en) 2009-09-09
AU2003287389A1 (en) 2004-06-07
KR20050083879A (ko) 2005-08-26
DE60329211D1 (de) 2009-10-22
EP1556393A2 (en) 2005-07-27
MXPA05004503A (es) 2005-08-16
JP2006507308A (ja) 2006-03-02
US20070021388A1 (en) 2007-01-25

Similar Documents

Publication Publication Date Title
KR101115210B1 (ko) 신규 시타라빈 모노포스페이트 전구약물
EP3186244B1 (en) Dioxolane analogues of uridine for the treatment of cancer
CN109553651B (zh) 4’-硫代核苷的新型化合物及其制备方法、药物组合物和应用
LU100724B1 (en) 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
JP2007522237A (ja) 新規２’−ｃ−メチルヌクレオシド誘導体
WO2015101183A1 (zh) 尿嘧啶核苷酸类似物及其制备方法和应用
CN113939526A (zh) 环状磷酸酯化合物
JPH09504541A (ja) ５‐フルオロウラシル誘導体
CN111655710B (zh) 吉西他滨含磷前药
EP3730508A1 (en) Liver specific delivery-based gemcitabine prodrug nucleoside cyclic phosphate compound, and application thereof
ZA200503252B (en) Novel cytarabine monophosphate prodrugs
KR102776475B1 (ko) 아민, 아미드 및 페놀 전달에 유용한 프로드러그 플랫폼
EP3730504B1 (en) Cytarabine prodrug nucleoside cyclic phosphate compound based on liver-specific delivery and use
EP4151646A1 (en) 5-fluorouracil derivatives as prodrugs for cancer treatment
US11173174B2 (en) DNMT inhibitor as solid tumor therapeutic drug
HUP0302882A2 (hu) Javított specificitás betegségek kezelésében
TWI695841B (zh) 治療癌症之前藥

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

A201 Request for examination
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20150116

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

FPAY Annual fee payment

Payment date: 20160104

Year of fee payment: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

P22-X000 Classification modified

St.27 status event code: A-4-4-P10-P22-nap-X000

FPAY Annual fee payment

Payment date: 20170102

Year of fee payment: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

FPAY Annual fee payment

Payment date: 20180103

Year of fee payment: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

P22-X000 Classification modified

St.27 status event code: A-4-4-P10-P22-nap-X000

FPAY Annual fee payment

Payment date: 20190116

Year of fee payment: 8

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 8

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

FPAY Annual fee payment

Payment date: 20200115

Year of fee payment: 9

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 9

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 10

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 11

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20230204

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20230204