JP2007532665A - Ｈｉｖインテグラーゼ阻害剤化合物のホスホネート類似物 - Google Patents

Ｈｉｖインテグラーゼ阻害剤化合物のホスホネート類似物 Download PDF

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Publication number
JP2007532665A
JP2007532665A JP2007508496A JP2007508496A JP2007532665A JP 2007532665 A JP2007532665 A JP 2007532665A JP 2007508496 A JP2007508496 A JP 2007508496A JP 2007508496 A JP2007508496 A JP 2007508496A JP 2007532665 A JP2007532665 A JP 2007532665A
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Prior art keywords
substituted
formula
compound
hiv integrase
integrase inhibitor
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JP2007532665A5 (https=
Inventor
ツェンホン アール． カイ，
シャオウー チェン，
マリア ファーディス，
サルマン ワイ． ジャブリ，
ハオルン ジン，
チョウン ユー． キム，
サヌエル イー． メトボ，
マイケル アール． ミッシュ，
リチャード エム． パスター，
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Publication of JP2007532665A5 publication Critical patent/JP2007532665A5/ja
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    • 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
    • A61K31/66—Phosphorus compounds
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • C07F9/6561—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
JP2007508496A 2004-04-14 2005-04-11 Ｈｉｖインテグラーゼ阻害剤化合物のホスホネート類似物 Pending JP2007532665A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US56267804P 2004-04-14 2004-04-14
PCT/US2005/012520 WO2005117904A2 (en) 2004-04-14 2005-04-11 Phosphonate analogs of hiv integrase inhibitor compounds

Publications (2)

Publication Number Publication Date
JP2007532665A true JP2007532665A (ja) 2007-11-15
JP2007532665A5 JP2007532665A5 (https=) 2008-06-19

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JP2007508496A Pending JP2007532665A (ja) 2004-04-14 2005-04-11 Ｈｉｖインテグラーゼ阻害剤化合物のホスホネート類似物

Country Status (13)

Country Link
US (2) US20080076738A1 (https=)
EP (1) EP1742642B1 (https=)
JP (1) JP2007532665A (https=)
AT (1) ATE411030T1 (https=)
AU (1) AU2005249363A1 (https=)
CA (1) CA2562713A1 (https=)
DE (1) DE602005010413D1 (https=)
DK (1) DK1742642T3 (https=)
ES (1) ES2315922T3 (https=)
PL (1) PL1742642T3 (https=)
PT (1) PT1742642E (https=)
SI (1) SI1742642T1 (https=)
WO (1) WO2005117904A2 (https=)

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JP2009502964A (ja) * 2005-07-27 2009-01-29 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖを阻害するための抗ウイルス性ホスホン酸結合体
JP2013536873A (ja) * 2010-09-06 2013-09-26 グアンジョウ インスティテュート オブ バイオメディスン アンド ヘルス，チャイニーズ アカデミー オブ サイエンスィズ アミド化合物

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WO2004035577A2 (en) * 2002-10-16 2004-04-29 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
AR057023A1 (es) * 2005-05-16 2007-11-14 Gilead Sciences Inc Compuestos heterociclicos con propiedades inhibidoras de hiv-integrasa
WO2006122403A1 (en) 2005-05-19 2006-11-23 Merck Frosst Canada Ltd. Quinoline derivatives as ep4 antagonists
CA2642321A1 (en) * 2006-02-20 2007-08-30 Alembic Limited An improved process for the preparation of biphosphonic derivatives
AU2007254190A1 (en) 2006-05-16 2007-11-29 Gilead Sciences, Inc. Integrase inhibitors
WO2009026206A1 (en) * 2007-08-21 2009-02-26 University Of Toledo Method for synthesizing xanthohumol
US20090291921A1 (en) * 2007-11-20 2009-11-26 Gilead Sciences, Inc. Integrase inhibitors
WO2010011814A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
ES2448766T3 (es) * 2008-07-25 2014-03-17 Viiv Healthcare Company Profármacos de dolutegravir
WO2010011815A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
KR101733625B1 (ko) 2008-12-11 2017-05-10 시오노기세야쿠 가부시키가이샤 카르바모일피리돈 ｈｉｖ 인테그라제 억제제 및 중간체의 합성
TWI518084B (zh) 2009-03-26 2016-01-21 鹽野義製藥股份有限公司 哌喃酮與吡啶酮衍生物之製造方法
LT3494972T (lt) * 2010-01-27 2024-03-12 Viiv Healthcare Company Dolutegraviro ir lamivudino kompozicija živ infekcijai gydyti
TWI582097B (zh) 2010-03-23 2017-05-11 Ｖｉｉｖ醫療保健公司 製備胺甲醯吡啶酮衍生物及中間體之方法
US20120142701A1 (en) * 2010-05-28 2012-06-07 The University Of Hong Kong Compounds and methods for the treatment of proliferative diseases
CA2830027C (en) 2011-03-31 2016-04-26 Pfizer Inc. Novel bicyclic pyridinones
KR101365849B1 (ko) * 2012-03-28 2014-02-24 경동제약 주식회사 솔리페나신 또는 그의 염의 제조방법 및 이에 사용되는 신규 중간체
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
JP7381190B2 (ja) 2014-12-26 2023-11-15 エモリー・ユニバーシテイ Ｎ４－ヒドロキシシチジン及び誘導体並びにそれに関連する抗ウイルス用途
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PT3706762T (pt) 2017-12-07 2024-12-05 Univ Emory N4-hidroxicitidina e derivados e utilizações antivirais relacionadas com os mesmos
WO2019113523A1 (en) 2017-12-08 2019-06-13 Ashok Bajji Compounds and therapeutic uses thereof
CN111484529A (zh) * 2019-01-28 2020-08-04 奥锐特药业股份有限公司 一种合成替诺福韦单苯酯的方法
CN112946154B (zh) * 2021-02-05 2022-10-25 石家庄四药有限公司 他汀类药物起始物料及其对映异构体的hplc检测方法

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009502964A (ja) * 2005-07-27 2009-01-29 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖを阻害するための抗ウイルス性ホスホン酸結合体
JP2013536873A (ja) * 2010-09-06 2013-09-26 グアンジョウ インスティテュート オブ バイオメディスン アンド ヘルス，チャイニーズ アカデミー オブ サイエンスィズ アミド化合物
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Publication number Publication date
US20060116356A1 (en) 2006-06-01
WO2005117904A2 (en) 2005-12-15
DK1742642T3 (da) 2009-02-16
WO2005117904A3 (en) 2006-07-27
DE602005010413D1 (de) 2008-11-27
CA2562713A1 (en) 2005-12-15
US20080076738A1 (en) 2008-03-27
EP1742642B1 (en) 2008-10-15
ATE411030T1 (de) 2008-10-15
EP1742642A2 (en) 2007-01-17
SI1742642T1 (sl) 2009-04-30
PL1742642T3 (pl) 2009-06-30
HK1099235A1 (en) 2007-08-10
PT1742642E (pt) 2009-01-23
ES2315922T3 (es) 2009-04-01
AU2005249363A1 (en) 2005-12-15

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