JP2007520452A - ホスホネート誘導体としてのイノシン一リン酸デヒドロゲナーゼインヒビター - Google Patents

ホスホネート誘導体としてのイノシン一リン酸デヒドロゲナーゼインヒビター Download PDF

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Publication number
JP2007520452A
JP2007520452A JP2006536844A JP2006536844A JP2007520452A JP 2007520452 A JP2007520452 A JP 2007520452A JP 2006536844 A JP2006536844 A JP 2006536844A JP 2006536844 A JP2006536844 A JP 2006536844A JP 2007520452 A JP2007520452 A JP 2007520452A
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JP
Japan
Prior art keywords
compound
compound according
methyl
ethyl
following formula
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.)
Withdrawn
Application number
JP2006536844A
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English (en)
Japanese (ja)
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JP2007520452A5 (enExample
Inventor
イソップ チョー，
トールステン エー． キルシュベルク，
ウィル ワトキンス，
マリア ファーディス，
リー エス． チョン，
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
Priority claimed from PCT/US2004/013063 external-priority patent/WO2004096286A2/en
Priority claimed from PCT/US2004/013064 external-priority patent/WO2004096287A2/en
Priority claimed from PCT/US2004/013143 external-priority patent/WO2004096236A2/en
Priority claimed from PCT/US2004/013121 external-priority patent/WO2004096235A2/en
Priority claimed from PCT/US2004/013198 external-priority patent/WO2004100960A2/en
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of JP2007520452A publication Critical patent/JP2007520452A/ja
Publication of JP2007520452A5 publication Critical patent/JP2007520452A5/ja
Withdrawn legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
    • C07F9/65517—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2006536844A 2003-10-24 2004-10-25 ホスホネート誘導体としてのイノシン一リン酸デヒドロゲナーゼインヒビター Withdrawn JP2007520452A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US51425803P 2003-10-24 2003-10-24
PCT/US2004/013063 WO2004096286A2 (en) 2003-04-25 2004-04-26 Antiviral phosphonate analogs
PCT/US2004/013064 WO2004096287A2 (en) 2003-04-25 2004-04-26 Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
PCT/US2004/013143 WO2004096236A2 (en) 2003-04-25 2004-04-26 Immunomodulator phosphonate conjugates
PCT/US2004/013121 WO2004096235A2 (en) 2003-04-25 2004-04-26 Anti-cancer phosphonate analogs
PCT/US2004/013198 WO2004100960A2 (en) 2003-04-25 2004-04-26 Anti-inflammatory phosphonate compounds
PCT/US2004/035136 WO2005039552A2 (en) 2003-10-24 2004-10-25 Inosine monophosphate dehydrogenase inhibitors as phosphonate derivatives

Publications (2)

Publication Number Publication Date
JP2007520452A true JP2007520452A (ja) 2007-07-26
JP2007520452A5 JP2007520452A5 (enExample) 2007-12-06

Family

ID=38344791

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2006536844A Withdrawn JP2007520452A (ja) 2003-10-24 2004-10-25 ホスホネート誘導体としてのイノシン一リン酸デヒドロゲナーゼインヒビター

Country Status (7)

Country Link
US (1) US20070027116A1 (enExample)
EP (1) EP1680129A2 (enExample)
JP (1) JP2007520452A (enExample)
CN (1) CN101410120A (enExample)
AU (1) AU2004283710A1 (enExample)
CA (1) CA2542967A1 (enExample)
WO (1) WO2005039552A2 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5069463B2 (ja) 2003-04-25 2012-11-07 ギリアード サイエンシーズ， インコーポレイテッド 抗ウイルス性ホスホネート類似物
EP1740564A2 (en) 2004-04-26 2007-01-10 Teva Gyógyszergyár Zártköruen Muködo Részvenytarsaság Process for preparation of mycophenolic acid and ester derivatives thereof
ES2720618T3 (es) 2004-07-27 2019-07-23 Gilead Sciences Inc Análogos de fosfonato de compuestos de inhibidores de VIH
WO2007014352A2 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
DE102005057924A1 (de) * 2005-12-05 2007-06-06 Merck Patent Gmbh Pyridazinonderivate
NZ590075A (en) 2008-07-08 2012-12-21 Gilead Sciences Inc citrate, malonate and succinate salts of the HIV inhibitor ethyl N-[(S)({ [(2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl]oxy} methyl)phenoxyphosphinoyl]-L-alaninate
WO2010064146A2 (en) 2008-12-02 2010-06-10 Chiralgen, Ltd. Method for the synthesis of phosphorus atom modified nucleic acids
AP2011005929A0 (en) * 2009-03-20 2011-10-31 Alios Biopharma Inc Substituted nucleoside and nucleotide analogs.
US8816077B2 (en) 2009-04-17 2014-08-26 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
WO2010120386A1 (en) 2009-04-17 2010-10-21 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
CA2767253A1 (en) 2009-07-06 2011-01-13 Ontorii, Inc. Novel nucleic acid prodrugs and methods of use thereof
SG188497A1 (en) 2010-09-22 2013-05-31 Alios Biopharma Inc Substituted nucleotide analogs
WO2012039448A1 (ja) 2010-09-24 2012-03-29 株式会社キラルジェン 不斉補助基
CN103796657B (zh) 2011-07-19 2017-07-11 波涛生命科学有限公司 合成官能化核酸的方法
EP2794630A4 (en) 2011-12-22 2015-04-01 Alios Biopharma Inc SUBSTITUTED PHOSPHORTHIOAT NUCLEOTIDE ANALOGUE
WO2013142124A1 (en) 2012-03-21 2013-09-26 Vertex Pharmaceuticals Incorporated Solid forms of a thiophosphoramidate nucleotide prodrug
HK1203356A1 (en) 2012-03-22 2015-10-30 艾丽奥斯生物制药有限公司 Pharmaceutical combinations comprising a thionucleotide analog
WO2014010250A1 (en) 2012-07-13 2014-01-16 Chiralgen, Ltd. Asymmetric auxiliary group
KR20230152178A (ko) 2014-01-16 2023-11-02 웨이브 라이프 사이언시스 리미티드 키랄 디자인
CN118286245A (zh) 2014-12-26 2024-07-05 埃莫里大学 N4-羟基胞苷和衍生物及与其相关的抗病毒用途
CN106565769B (zh) * 2016-11-12 2018-12-04 北京汇康博源医药科技有限公司 恩替卡韦中间体的合成工艺
PT3661937T (pt) 2017-08-01 2021-09-24 Gilead Sciences Inc Formas cristalinas de ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-il)-4-fluoro-2,5-dihidrofurano-2-il)oxi)metil)(fenoxi)fosforil)-l-alaninato de etil (gs-9131) para tratamento de infeções virais
RS66222B1 (sr) 2017-12-07 2024-12-31 Univ Emory N4-hidroksicitidin i derivati i antivirusne upotrebe povezane sa njim
CN110726801A (zh) * 2019-10-31 2020-01-24 山东泰星新材料股份有限公司 一种监测烷基次膦酸反应状态的方法
IT202100005777A1 (it) 2021-03-11 2022-09-11 Hippocrates Res S R L Composizione per l’uso nel trattamento dell’occhio secco

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5631370A (en) * 1988-01-20 1997-05-20 Regents Of The University Of Minnesota Optically-active isomers of dideoxycarbocyclic nucleosides
US5177064A (en) * 1990-07-13 1993-01-05 University Of Florida Targeted drug delivery via phosphonate derivatives
US5610294A (en) * 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5654286A (en) * 1993-05-12 1997-08-05 Hostetler; Karl Y. Nucleotides for topical treatment of psoriasis, and methods for using same
WO1995002582A1 (en) * 1993-07-14 1995-01-26 Ciba-Geigy Ag Cyclic hydrazine compounds
US5446137B1 (en) * 1993-12-09 1998-10-06 Behringwerke Ag Oligonucleotides containing 4'-substituted nucleotides
US5493030A (en) * 1994-02-18 1996-02-20 Syntex (U.S.A.) Inc. 5-substituted derivatives of mycophenolic acid
US5854227A (en) * 1994-03-04 1998-12-29 Hartmann; John F. Therapeutic derivatives of diphosphonates
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5750493A (en) * 1995-08-30 1998-05-12 Raymond F. Schinazi Method to improve the biological and antiviral activity of protease inhibitors
US5914332A (en) * 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
US5874577A (en) * 1996-04-03 1999-02-23 Medichem Research, Inc. Method for the preparing 9-12-(Diethoxyphosphonomethoxy)ethyl!adenine and analogues thereof
CA2261619C (en) * 1996-07-26 2006-05-23 Gilead Sciences, Inc. Nucleotide analogs
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
US6174888B1 (en) * 1998-05-28 2001-01-16 Novartis Ag 2-amino-7-(1-substituted-2-hydroxyethyl)-3,5-dihydropyrrolo[3,2-D]pyrimidin-4-ones
TNSN00027A1 (fr) * 1999-02-12 2005-11-10 Vertex Pharma Inhibiteurs de l'aspartyle protease
US6258831B1 (en) * 1999-03-31 2001-07-10 The Procter & Gamble Company Viral treatment
US6608027B1 (en) * 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
MXPA02000294A (es) * 1999-06-25 2002-06-21 Vertex Pharma Profarmacos de carbamatos inhibidores de impdh.
KR20020093824A (ko) * 2000-02-29 2002-12-16 미쯔비시 웰 파마 가부시키가이샤 포스포네이트 뉴클레오티드 화합물
WO2002008241A2 (en) * 2000-07-21 2002-01-31 Gilead Sciences, Inc. Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
KR20020097384A (ko) * 2001-06-20 2002-12-31 미쯔비시 도꾜 세이야꾸 가부시끼가이샤 기존의 약제에 내성변이를 가지는 바이러스에 유효한 약제
EP1509537B9 (en) * 2002-04-26 2007-11-14 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such
MXPA05008736A (es) * 2003-02-19 2005-10-05 Univ Yale Analogos de nucleosido antivirales y metodos para tratar infecciones virales, especialmente infecciones por vih.

Also Published As

Publication number Publication date
US20070027116A1 (en) 2007-02-01
CA2542967A1 (en) 2005-05-06
WO2005039552A2 (en) 2005-05-06
EP1680129A2 (en) 2006-07-19
CN101410120A (zh) 2009-04-15
AU2004283710A1 (en) 2005-05-06
WO2005039552A3 (en) 2005-06-09

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