AU2005249363A1 - Phosphonate analogs of HIV integrase inhibitor compounds - Google Patents

Phosphonate analogs of HIV integrase inhibitor compounds Download PDF

Info

Publication number
AU2005249363A1
AU2005249363A1 AU2005249363A AU2005249363A AU2005249363A1 AU 2005249363 A1 AU2005249363 A1 AU 2005249363A1 AU 2005249363 A AU2005249363 A AU 2005249363A AU 2005249363 A AU2005249363 A AU 2005249363A AU 2005249363 A1 AU2005249363 A1 AU 2005249363A1
Authority
AU
Australia
Prior art keywords
substituted
formula
pct
hiv integrase
integrase inhibitor
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
AU2005249363A
Other languages
English (en)
Inventor
Zhenhong R. Cai
Xiaowu Chen
Maria Fardis
Salman Y. Jabri
Haolun Jin
Choung U. Kim
Sanuel 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
MICHAEL MISH
SALMAN JABRI
SANUEL METOBO
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
Application filed by MICHAEL MISH, SALMAN JABRI, SANUEL METOBO, Gilead Sciences Inc filed Critical MICHAEL MISH
Publication of AU2005249363A1 publication Critical patent/AU2005249363A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/662Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/665Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/548Phosphates or phosphonates, e.g. bone-seeking
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed 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
    • C07F9/6561Heterocyclic 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

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)
  • 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)
AU2005249363A 2004-04-14 2005-04-11 Phosphonate analogs of HIV integrase inhibitor compounds Abandoned AU2005249363A1 (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
AU2005249363A1 true AU2005249363A1 (en) 2005-12-15

Family

ID=35276373

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005249363A Abandoned AU2005249363A1 (en) 2004-04-14 2005-04-11 Phosphonate analogs of HIV integrase inhibitor compounds

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=)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040157804A1 (en) * 2002-10-16 2004-08-12 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
TW200716632A (en) * 2005-05-16 2007-05-01 Gilead Sciences Inc Integrase inhibitor compounds
US8013159B2 (en) 2005-05-19 2011-09-06 Merck Canada Inc. Quinoline derivatives as EP4 antagonists
CA2616314A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
WO2007096896A1 (en) * 2006-02-20 2007-08-30 Alembic Limited An improved process for the preparation of biphosphonic derivatives
NZ572367A (en) * 2006-05-16 2011-09-30 Gilead Sciences Inc Fused cyclic compounds as 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
WO2010011815A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
EP2320909B8 (en) 2008-07-25 2016-03-30 VIIV Healthcare Company Chemical compounds
SI2320908T1 (sl) * 2008-07-25 2014-05-30 Viiv Healthcare Company Predzdravila dolutegravirja
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
PE20121524A1 (es) * 2010-01-27 2012-12-03 Viiv Healthcare Co Combinaciones de compuestos que comprenden inhibidores de la integrasa de vih y otros agentes terapeuticos
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
GB2497476B (en) * 2010-09-06 2018-01-10 Guangzhou Inst Biomed & Health Amide Compounds
EP2691393B1 (en) 2011-03-31 2016-09-14 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
DK3236972T3 (en) 2014-12-26 2021-10-04 Univ Emory Antivirale N4-hydroxycytidin-derivativer
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
JP6804790B1 (ja) 2017-12-07 2020-12-23 エモリー ユニバーシティー N4−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途
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
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
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 (https=) * 1992-06-27 1997-05-11 Hoechst Ag
US5798340A (en) * 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
HU217841B (hu) * 1993-12-17 2000-04-28 The Procter & Gamble Co. 6-[(2-Imidazolidinilidén)-amino]-kinolin-származékok és ezeket tartalmazó gyógyszerkészítmények
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
EP0927164A1 (en) * 1996-09-10 1999-07-07 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
IL139254A0 (en) * 1998-06-10 2001-11-25 Arena Pharm Inc Acetylcholine enhancers
AU4719799A (en) * 1998-06-30 2000-01-17 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
AU2003231765B9 (en) * 2002-04-26 2010-01-28 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such
US20040157804A1 (en) * 2002-10-16 2004-08-12 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds

Also Published As

Publication number Publication date
CA2562713A1 (en) 2005-12-15
DK1742642T3 (da) 2009-02-16
JP2007532665A (ja) 2007-11-15
US20060116356A1 (en) 2006-06-01
ATE411030T1 (de) 2008-10-15
HK1099235A1 (en) 2007-08-10
WO2005117904A2 (en) 2005-12-15
DE602005010413D1 (de) 2008-11-27
ES2315922T3 (es) 2009-04-01
US20080076738A1 (en) 2008-03-27
WO2005117904A3 (en) 2006-07-27
EP1742642B1 (en) 2008-10-15
SI1742642T1 (sl) 2009-04-30
PT1742642E (pt) 2009-01-23
PL1742642T3 (pl) 2009-06-30
EP1742642A2 (en) 2007-01-17

Similar Documents

Publication Publication Date Title
AU2005249363A1 (en) Phosphonate analogs of HIV integrase inhibitor compounds
US7253180B2 (en) Pre-organized tricyclic 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
JP2006514099A5 (https=)
US8008287B2 (en) Integrase inhibitors
US20070072831A1 (en) Integrase inhibitor compounds
AU2004274493A1 (en) Aza-quinolinol phosphonate integrase inhibitor compounds
AU2004260789B2 (en) Nucleobase phosphonate analogs for antiviral treatment
WO2009067541A2 (en) Integrase inhibitors
AU2005206511A1 (en) Pyrimidyl phosphonate antiviral compounds and methods of use
US20060217410A1 (en) Pre-organized tricyclic integrase inhibitor compounds
AU2011224011A1 (en) Phosphonate analogs of HIV inhibitor compounds
HK1099235B (en) Phosphonate analogs of hiv integrase inhibitor compounds

Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application