CA2562713A1 - Phosphonate analogs of hiv integrase inhibitor compounds - Google Patents

Phosphonate analogs of hiv integrase inhibitor compounds Download PDF

Info

Publication number
CA2562713A1
CA2562713A1 CA002562713A CA2562713A CA2562713A1 CA 2562713 A1 CA2562713 A1 CA 2562713A1 CA 002562713 A CA002562713 A CA 002562713A CA 2562713 A CA2562713 A CA 2562713A CA 2562713 A1 CA2562713 A1 CA 2562713A1
Authority
CA
Canada
Prior art keywords
substituted
formula
hiv integrase
integrase inhibitor
inhibitor compound
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.)
Abandoned
Application number
CA002562713A
Other languages
English (en)
French (fr)
Inventor
Zhenhong R. Cai
Xiaowu Chen
Maria Fardis
Salman Y. Jabri
Haolun Jin
Choung U. Kim
Samuel E. Metobo
Michael R. Mish
Richard M. Pastor
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
Individual
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 Individual filed Critical Individual
Publication of CA2562713A1 publication Critical patent/CA2562713A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
CA002562713A 2004-04-14 2005-04-11 Phosphonate analogs of hiv integrase inhibitor compounds Abandoned CA2562713A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US56267804P 2004-04-14 2004-04-14
US60/562,678 2004-04-14
PCT/US2005/012520 WO2005117904A2 (en) 2004-04-14 2005-04-11 Phosphonate analogs of hiv integrase inhibitor compounds

Publications (1)

Publication Number Publication Date
CA2562713A1 true CA2562713A1 (en) 2005-12-15

Family

ID=35276373

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002562713A Abandoned CA2562713A1 (en) 2004-04-14 2005-04-11 Phosphonate analogs of hiv integrase inhibitor compounds

Country Status (13)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003301439A1 (en) * 2002-10-16 2004-05-04 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
EP1888581A2 (en) * 2005-05-16 2008-02-20 Gilead Sciences, Inc. Hiv-integrase inhibitor compounds
EP1885722B1 (en) 2005-05-19 2011-11-16 Merck Canada Inc. Quinoline derivatives as ep4 antagonists
WO2007014352A2 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
EP1987046A1 (en) * 2006-02-20 2008-11-05 Alembic Limited An improved process for the preparation of biphosphonic derivatives
CA2651579A1 (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
WO2009067541A2 (en) * 2007-11-20 2009-05-28 Gilead Sciences, Inc. Integrase inhibitors
KR101700267B1 (ko) * 2008-07-25 2017-01-26 비이브 헬쓰케어 컴퍼니 화합물
US8217034B2 (en) * 2008-07-25 2012-07-10 Shionogi & Co., Ltd. Chemical compounds
WO2010011815A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
CA2744019C (en) 2008-12-11 2017-03-14 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
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
PT3494972T (pt) * 2010-01-27 2024-02-12 Viiv Healthcare Co Combinações de dolutegravir e lamivudina para o tratamento de infeção pelo hiv
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
US9238643B2 (en) 2010-09-06 2016-01-19 Guangzhou Institutes Of Biomedicine And Health, Chinese Academy Of Sciences Amide compounds
ES2602794T3 (es) 2011-03-31 2017-02-22 Pfizer Inc Piridinonas bicíclicas novedosas
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
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
WO2016125048A1 (en) 2015-02-03 2016-08-11 Pfizer Inc. Novel cyclopropabenzofuranyl pyridopyrazinediones
US11331331B2 (en) 2017-12-07 2022-05-17 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
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

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH385846A (de) * 1960-03-31 1964-12-31 Geigy Ag J R Verfahren zur Herstellung von neuen 7-Acyl-8-hydroxy-chinolinen und ihre Verwendung als Fungizide und Bakterizide im Pflanzen- und Materialschutz
US4816570A (en) * 1982-11-30 1989-03-28 The Board Of Regents Of The University Of Texas System Biologically reversible phosphate and phosphonate protective groups
US4968788A (en) * 1986-04-04 1990-11-06 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective gruops
ES2118069T3 (es) * 1990-09-14 1998-09-16 Acad Of Science Czech Republic Profarmacos de fosfonatos.
US5883255A (en) * 1990-10-31 1999-03-16 Smithkline Beecham Corporation Substituted indolizino 1,2-b!quinolinones
EP0498722B1 (fr) * 1991-02-07 1997-07-30 Roussel Uclaf Dérivés bicycliques azotés, leur procédé de préparation, les intermédiaires obtenus, leur application comme médicaments et les compositions pharmaceutiques les renfermant
EP0520573A1 (en) * 1991-06-27 1992-12-30 Glaxo Inc. Cyclic imide derivatives
US5639881A (en) * 1991-11-08 1997-06-17 Arizona Board Of Regents Acting On Behalf Of Arizona State University Synthesis and elucidation of pyrimido (4,5-Q) quinazoline derivatives
TW304945B (enExample) * 1992-06-27 1997-05-11 Hoechst Ag
US5798340A (en) * 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
PT736020E (pt) * 1993-12-17 2000-10-31 Procter & Gamble Compostos 6-(2-imidazolinilamino)quinolina uteis como alfa-2 adrenoceptor agonistas
US5538988A (en) * 1994-04-26 1996-07-23 Martinez; Gregory R. Benzocycloalkylazolethione derivatives
DE19613591A1 (de) * 1996-04-04 1997-10-09 Hoechst Ag Substituierte-Chinolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung
US5854275A (en) * 1996-05-16 1998-12-29 Pfizer Inc. Cyclic imide derivatives
AU4172197A (en) * 1996-09-10 1998-04-02 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
DE19738005A1 (de) * 1997-08-30 1999-03-04 Bayer Ag Verwendung von substituierten 1,1-Bisphosphonaten
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
MXPA00012248A (es) * 1998-06-10 2003-04-25 Arena Pharm Inc Incrementadores de acetilcolina.
WO2000000475A1 (en) * 1998-06-30 2000-01-06 Du Pont Pharmaceuticals Company Substituted quinolin-2(1h)-ones useful as hiv reverse transcriptase inhibitors
US6187907B1 (en) * 1998-08-31 2001-02-13 James Chen Triple helix coil template having a biologically active ligand
AU3118200A (en) * 1998-12-14 2000-07-03 Merck & Co., Inc. Hiv integrase inhibitors
US6245806B1 (en) * 1999-08-03 2001-06-12 Merck & Co., Inc. HIV integrase inhibitors
WO2001027309A1 (en) * 1999-10-13 2001-04-19 Merck & Co., Inc. Hiv integrase inhibitors
PE20011349A1 (es) * 2000-06-16 2002-01-19 Upjohn Co 1-aril-4-oxo-1,4-dihidro-3-quinolincarboxamidas como agentes antivirales
US6525049B2 (en) * 2000-07-05 2003-02-25 Pharmacia & Upjohn Company Pyrroloquinolones as antiviral agents
AR036256A1 (es) * 2001-08-17 2004-08-25 Merck & Co Inc Sal sodica de un inhibidor de integrasa del vih, procesos para su preparacion, composiciones farmaceuticas que lo contienen y su uso para la manufactura de un medicamento
JP4942915B2 (ja) * 2002-04-26 2012-05-30 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積
AU2003301439A1 (en) * 2002-10-16 2004-05-04 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds

Also Published As

Publication number Publication date
WO2005117904A3 (en) 2006-07-27
PT1742642E (pt) 2009-01-23
WO2005117904A2 (en) 2005-12-15
JP2007532665A (ja) 2007-11-15
ES2315922T3 (es) 2009-04-01
US20060116356A1 (en) 2006-06-01
DE602005010413D1 (de) 2008-11-27
US20080076738A1 (en) 2008-03-27
DK1742642T3 (da) 2009-02-16
EP1742642A2 (en) 2007-01-17
AU2005249363A1 (en) 2005-12-15
HK1099235A1 (en) 2007-08-10
PL1742642T3 (pl) 2009-06-30
ATE411030T1 (de) 2008-10-15
EP1742642B1 (en) 2008-10-15
SI1742642T1 (sl) 2009-04-30

Similar Documents

Publication Publication Date Title
CA2562713A1 (en) Phosphonate analogs of hiv integrase inhibitor compounds
DE60315023T2 (de) Anreicherung in der zelle an phosphonat analoga von hiv protease inhibitor verbindungen und die verbindungen selbst
AU2005330489B2 (en) Nucleoside phosphonate conjugates as anti HIV agents
JP2005523912A5 (enExample)
AU2004260789B2 (en) Nucleobase phosphonate analogs for antiviral treatment
AU2011224011A1 (en) Phosphonate analogs of HIV inhibitor compounds

Legal Events

Date Code Title Description
FZDE Discontinued