CN102304150B - 作为hiv抑制剂的磷酸-吲哚 - Google Patents

作为hiv抑制剂的磷酸-吲哚 Download PDF

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Publication number
CN102304150B
CN102304150B CN201110185299.9A CN201110185299A CN102304150B CN 102304150 B CN102304150 B CN 102304150B CN 201110185299 A CN201110185299 A CN 201110185299A CN 102304150 B CN102304150 B CN 102304150B
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China
Prior art keywords
alkyl
hiv
independently
aryl
optionally substituted
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Expired - Fee Related
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CN201110185299.9A
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English (en)
Chinese (zh)
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CN102304150A (zh
Inventor
理查德·斯托勒
西里尔·多森
弗兰西斯-雷内·亚历山大
阿琳·罗兰
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Idenix Pharmaceuticals LLC
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Idenix Pharmaceuticals LLC
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Application filed by Idenix Pharmaceuticals LLC filed Critical Idenix Pharmaceuticals LLC
Publication of CN102304150A publication Critical patent/CN102304150A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic 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
    • C07F9/65586Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • C07F9/5728Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic 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
    • C07F9/65583Heterocyclic 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 each of the hetero rings containing nitrogen as ring hetero atom

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  • 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
CN201110185299.9A 2004-09-17 2005-09-16 作为hiv抑制剂的磷酸-吲哚 Expired - Fee Related CN102304150B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US61106104P 2004-09-17 2004-09-17
US60/611,061 2004-09-17
US71144505P 2005-08-25 2005-08-25
US60/711,445 2005-08-25
US71156505P 2005-08-26 2005-08-26
US60/711,565 2005-08-26

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2005800392187A Division CN101084231B (zh) 2004-09-17 2005-09-16 作为hiv抑制剂的磷酸-吲哚

Publications (2)

Publication Number Publication Date
CN102304150A CN102304150A (zh) 2012-01-04
CN102304150B true CN102304150B (zh) 2014-06-18

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ID=36407947

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CN201110185299.9A Expired - Fee Related CN102304150B (zh) 2004-09-17 2005-09-16 作为hiv抑制剂的磷酸-吲哚

Country Status (24)

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US (2) US7534809B2 (cg-RX-API-DMAC7.html)
EP (3) EP2256124A1 (cg-RX-API-DMAC7.html)
JP (1) JP5031569B2 (cg-RX-API-DMAC7.html)
KR (1) KR101242962B1 (cg-RX-API-DMAC7.html)
CN (1) CN102304150B (cg-RX-API-DMAC7.html)
AT (2) ATE414092T1 (cg-RX-API-DMAC7.html)
AU (1) AU2005305609B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0515344A (cg-RX-API-DMAC7.html)
CA (1) CA2583409C (cg-RX-API-DMAC7.html)
CY (1) CY1109440T1 (cg-RX-API-DMAC7.html)
DE (2) DE602005011031D1 (cg-RX-API-DMAC7.html)
DK (1) DK1799696T3 (cg-RX-API-DMAC7.html)
ES (1) ES2320252T3 (cg-RX-API-DMAC7.html)
HR (1) HRP20090086T3 (cg-RX-API-DMAC7.html)
IL (1) IL181909A0 (cg-RX-API-DMAC7.html)
MX (1) MX2007003040A (cg-RX-API-DMAC7.html)
NO (1) NO20071871L (cg-RX-API-DMAC7.html)
NZ (1) NZ554232A (cg-RX-API-DMAC7.html)
PL (1) PL1799696T3 (cg-RX-API-DMAC7.html)
PT (1) PT1799696E (cg-RX-API-DMAC7.html)
RS (1) RS50981B (cg-RX-API-DMAC7.html)
SG (1) SG155939A1 (cg-RX-API-DMAC7.html)
SI (1) SI1799696T1 (cg-RX-API-DMAC7.html)
WO (1) WO2006054182A2 (cg-RX-API-DMAC7.html)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0515344A (pt) 2004-09-17 2008-07-15 Idenix Pharmaceuticals Inc composto, composição farmacêutica, e, usos de uma quantidade eficaz de um composto 3-fosfoindol ou sal, pró-droga, estereoisÈmero, tautÈmero, n-óxido ou amina quaternária farmaceuticamente aceitável do mesmo e de uma quantidade de tratamento eficaz anti-hiv de um composto de 3-fosfoindol ou sal, pró-droga, estereo-isÈmero, tautÈmero, n-óxido ou amina quaternária farmaceuticamente aceitável do mesmo
JP2010504978A (ja) 2006-09-29 2010-02-18 アイデニクス ファーマシューティカルズ,インコーポレーテッド Hiv阻害剤としての鏡像異性的に純粋なホスホインドール
CA2665007A1 (en) * 2006-10-06 2008-05-08 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
JP5167350B2 (ja) 2007-05-30 2013-03-21 エフ.ホフマン−ラ ロシュ アーゲー 非ヌクレオシド系逆転写酵素阻害剤
TW200946541A (en) * 2008-03-27 2009-11-16 Idenix Pharmaceuticals Inc Solid forms of an anti-HIV phosphoindole compound
TW200944537A (en) * 2008-04-03 2009-11-01 Idenix Pharmaceuticals Inc Formulations comprising a phosphoindole compound and one or more second active agents
WO2010090976A1 (en) * 2009-02-03 2010-08-12 Idenix Pharmaceuticals, Inc. Phosphinate ruthenium complexes
JP5690286B2 (ja) * 2009-03-04 2015-03-25 イデニク プハルマセウティカルス,インコーポレイテッド ホスホチオフェン及びホスホチアゾールhcvポリメラーゼ阻害剤
LT3494972T (lt) 2010-01-27 2024-03-12 Viiv Healthcare Company Dolutegraviro ir lamivudino kompozicija živ infekcijai gydyti
CN103275126B (zh) * 2013-05-28 2016-03-23 兰州大学 一种立体选择性合成3-位膦酰化吲哚的方法
ITMI20131218A1 (it) * 2013-07-19 2015-01-20 Need Pharma Srl Nuovi ureido derivati di acidi naftalensolfonici
US11795239B2 (en) * 2017-10-13 2023-10-24 Orasure Technologies, Inc. Products and methods for monitoring adherence to nucleoside reverse transcriptase inhibitor therapy

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US4866084A (en) 1987-07-17 1989-09-12 Harbor Branch Oceanographic Institution, Inc. Topsentin compounds effective against viruses and certain tumors
US5527819A (en) * 1991-09-06 1996-06-18 Merck & Co., Inc. Inhibitors of HIV reverse transcriptase
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BRPI0515344A (pt) * 2004-09-17 2008-07-15 Idenix Pharmaceuticals Inc composto, composição farmacêutica, e, usos de uma quantidade eficaz de um composto 3-fosfoindol ou sal, pró-droga, estereoisÈmero, tautÈmero, n-óxido ou amina quaternária farmaceuticamente aceitável do mesmo e de uma quantidade de tratamento eficaz anti-hiv de um composto de 3-fosfoindol ou sal, pró-droga, estereo-isÈmero, tautÈmero, n-óxido ou amina quaternária farmaceuticamente aceitável do mesmo
JP2010504978A (ja) * 2006-09-29 2010-02-18 アイデニクス ファーマシューティカルズ,インコーポレーテッド Hiv阻害剤としての鏡像異性的に純粋なホスホインドール

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EP1961757A1 (en) 2008-08-27
HRP20090086T3 (en) 2009-03-31
US8044091B2 (en) 2011-10-25
US20060074054A1 (en) 2006-04-06
EP1961757B1 (en) 2010-09-01
BRPI0515344A (pt) 2008-07-15
MX2007003040A (es) 2007-08-02
NO20071871L (no) 2007-05-15
CA2583409A1 (en) 2006-05-26
ES2320252T3 (es) 2009-05-20
KR101242962B1 (ko) 2013-03-13
JP2008515782A (ja) 2008-05-15
HK1100142A1 (en) 2007-09-07
DK1799696T3 (da) 2009-03-09
AU2005305609A1 (en) 2006-05-26
SG155939A1 (en) 2009-10-29
EP2256124A1 (en) 2010-12-01
ATE479693T1 (de) 2010-09-15
SI1799696T1 (sl) 2009-04-30
ATE414092T1 (de) 2008-11-15
EP1799696A2 (en) 2007-06-27
IL181909A0 (en) 2007-07-04
DE602005023360D1 (de) 2010-10-14
CN102304150A (zh) 2012-01-04
JP5031569B2 (ja) 2012-09-19
WO2006054182A2 (en) 2006-05-26
NZ554232A (en) 2010-09-30
AU2005305609B2 (en) 2011-10-06
KR20070063545A (ko) 2007-06-19
WO2006054182A3 (en) 2007-03-01
CA2583409C (en) 2014-06-17
DE602005011031D1 (en) 2008-12-24
WO2006054182A9 (en) 2006-08-17
CY1109440T1 (el) 2014-08-13
US7534809B2 (en) 2009-05-19
PL1799696T3 (pl) 2009-04-30
RS50981B (sr) 2010-10-31
EP1799696B1 (en) 2008-11-12
US20090163444A1 (en) 2009-06-25
PT1799696E (pt) 2009-02-16

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