CA2501881A1 - Pre-organized tricyclic integrase inhibitor compounds - Google Patents

Pre-organized tricyclic integrase inhibitor compounds Download PDF

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Publication number
CA2501881A1
CA2501881A1 CA002501881A CA2501881A CA2501881A1 CA 2501881 A1 CA2501881 A1 CA 2501881A1 CA 002501881 A CA002501881 A CA 002501881A CA 2501881 A CA2501881 A CA 2501881A CA 2501881 A1 CA2501881 A1 CA 2501881A1
Authority
CA
Canada
Prior art keywords
compound
substituted
phosphonate
aryl
heteroaryl
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
CA002501881A
Other languages
English (en)
French (fr)
Inventor
James M. Chen
Xiaowu Chen
Maria Fardis
Haolun Jin
Choung U. Kim
Laura N. Schacherer
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 CA2501881A1 publication Critical patent/CA2501881A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/404—2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA002501881A 2002-10-16 2003-10-16 Pre-organized tricyclic integrase inhibitor compounds Abandoned CA2501881A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US41896302P 2002-10-16 2002-10-16
US60/418,963 2002-10-16
US47878303P 2003-06-16 2003-06-16
US60/478,783 2003-06-16
PCT/US2003/032666 WO2004035576A2 (en) 2002-10-16 2003-10-16 Pre-organized tricyclic integrase inhibitor compounds

Publications (1)

Publication Number Publication Date
CA2501881A1 true CA2501881A1 (en) 2004-04-29

Family

ID=32110203

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002501881A Abandoned CA2501881A1 (en) 2002-10-16 2003-10-16 Pre-organized tricyclic integrase inhibitor compounds

Country Status (19)

Country Link
US (3) US20040157804A1 (enExample)
EP (1) EP1558613A2 (enExample)
JP (1) JP2006514099A (enExample)
KR (1) KR20050087787A (enExample)
CN (1) CN100374438C (enExample)
AP (1) AP1858A (enExample)
AU (2) AU2003301439A1 (enExample)
BR (1) BR0315405A (enExample)
CA (1) CA2501881A1 (enExample)
EA (1) EA011399B1 (enExample)
HR (1) HRP20050431A2 (enExample)
IS (1) IS7845A (enExample)
MX (1) MXPA05003950A (enExample)
NO (1) NO20052378L (enExample)
NZ (1) NZ539264A (enExample)
OA (1) OA13079A (enExample)
PL (1) PL377966A1 (enExample)
UA (1) UA79830C2 (enExample)
WO (2) WO2004035577A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102917590A (zh) * 2010-03-29 2013-02-06 肿瘤疗法科学股份有限公司 三环化合物及含有所述化合物的pbk抑制剂

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1183025B1 (en) * 1999-05-19 2009-01-14 PainCeptor Pharma Corp. Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders
CA2522990A1 (en) * 2003-04-28 2004-11-11 Tibotec Pharmaceuticals Ltd. Hiv integrase inhibitors
US20070185007A1 (en) * 2003-09-19 2007-08-09 Haolun Jin Aza-quinolinol phosphonate integrase inhibitor compounds
AU2004297274B2 (en) * 2003-12-08 2009-09-10 The Research Foundation Of State University Of New York Site selectively tagged and templated molecularly imprinted polymers for sensor applications
EP1694686A1 (en) 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
JP4682153B2 (ja) * 2004-01-07 2011-05-11 ザ リサーチ ファウンデイション オブ ステイト ユニバーシティー オブ ニューヨーク 集積されたエミッションサイトを有するタンパク質インプリントポリマー
DE602005010413D1 (de) * 2004-04-14 2008-11-27 Zhenhong R Cai Phosphonatanaloga von hiv-integrasehemmerverbindungen
US7538112B2 (en) * 2004-05-07 2009-05-26 Merck & Co., Inc. HIV integrase inhibitors
US7476666B2 (en) 2004-06-09 2009-01-13 Merck & Co., Inc. HIV integrase inhibitors
EP1778669A2 (en) 2004-08-18 2007-05-02 Takeda San Diego, Inc. Kinase inhibitors
US7745459B2 (en) 2004-09-21 2010-06-29 Japan Tobacco Inc. Quinolizinone compound and use thereof as HIV integrase inhibitor
ATE479687T1 (de) 2004-10-15 2010-09-15 Takeda Pharmaceutical Kinaseinhibitoren
TW200716632A (en) * 2005-05-16 2007-05-01 Gilead Sciences Inc Integrase inhibitor compounds
AU2006246930C1 (en) 2005-05-19 2012-01-19 Merck Canada Inc. Quinoline derivatives as EP4 antagonists
AU2006272521A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of HIV
WO2007019130A2 (en) * 2005-08-04 2007-02-15 Smithkline Beecham Corporation Hiv integrase inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP1973908A2 (en) * 2005-12-21 2008-10-01 Gilead Sciences, Inc. Processes and intermediates useful for preparing integrase inhibitor compounds
EA018544B1 (ru) 2005-12-30 2013-08-30 Джилид Сайэнс, Инк. Способ лечения ретровирусной инфекции
US20090233964A1 (en) * 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
NZ572367A (en) 2006-05-16 2011-09-30 Gilead Sciences Inc Fused cyclic compounds as integrase inhibitors
JP2010505962A (ja) 2006-10-09 2010-02-25 武田薬品工業株式会社 キナーゼ阻害剤
WO2009067541A2 (en) * 2007-11-20 2009-05-28 Gilead Sciences, Inc. Integrase inhibitors
CN105055432A (zh) 2008-01-25 2015-11-18 奇默里克斯公司 治疗病毒感染的方法
SG192550A1 (en) 2008-07-25 2013-08-30 Viiv Healthcare Co Chemical compounds
BRPI0916649A2 (pt) * 2008-07-28 2015-08-04 Polymedix Inc E The Trustees Of The University Of Pennsylvania Composto, composição, uso de um composto, e, método para exterminar ou inibir o crescimento de uma espécie de plasmodium.
EP2376080B1 (en) 2008-12-11 2017-09-13 Shionogi&Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
EP2376453B1 (en) 2008-12-11 2019-11-20 VIIV Healthcare Company Intermediates for carbamoylpyridone hiv integrase inhibitors
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
EP2270021A1 (en) * 2009-06-18 2011-01-05 Centre National de la Recherche Scientifique Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability
WO2011011483A1 (en) * 2009-07-22 2011-01-27 Glaxosmithkline Llc Chemical compounds
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
JP5745869B2 (ja) * 2010-01-22 2015-07-08 富山化学工業株式会社 アルアルキル基を有する複素環化合物
ES2629165T3 (es) 2010-02-12 2017-08-07 Chimerix, Inc. Métodos de tratamiento de una infección vírica
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
RU2567385C2 (ru) 2010-04-02 2015-11-10 ЯНССЕН Ар ЭНД Ди АЙРЛЭНД Макроциклические ингибиторы интегразы
ES2602794T3 (es) 2011-03-31 2017-02-22 Pfizer Inc Piridinonas bicíclicas novedosas
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
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
US10260089B2 (en) 2012-10-29 2019-04-16 The Research Foundation Of The State University Of New York Compositions and methods for recognition of RNA using triple helical peptide nucleic acids
LT3236972T (lt) 2014-12-26 2021-11-10 Emory University Antivirusiniai n4-hidroksicitidino dariniai
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
CN104803905B (zh) * 2015-04-17 2017-10-10 复旦大学 一种合成异吲哚啉‑1‑酮衍生物的方法
WO2017133517A1 (zh) * 2016-02-03 2017-08-10 四川海思科制药有限公司 一种磷酰胺衍生物及制备方法和用途
CN109305990B (zh) * 2017-07-28 2021-02-26 四川海思科制药有限公司 一种磷酸衍生物及制备方法和用途
CN109305989B (zh) * 2017-07-28 2021-02-26 四川海思科制药有限公司 一种磷酰胺衍生物及制备方法和用途
LT3706762T (lt) 2017-12-07 2024-12-27 Emory University N4-hidroksicitidinas ir jo dariniai bei susiję naudojimo prieš virusus būdai

Family Cites Families (32)

* 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
JP3347723B2 (ja) 1990-06-13 2002-11-20 グラツィエル，アーノルド 含リンプロドラッグ
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
DK0498722T3 (da) * 1991-02-07 1998-03-09 Roussel Uclaf Nye bicycliske nitrogenforbindelser substitueret med en benzylgruppe, fremgangsmåde til deres fremstilling, de opnåede nye intermediærer, deres anvendelse som lægemidler og de pharmaceutiske præparater som de indgår i
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
US5538988A (en) * 1994-04-26 1996-07-23 Martinez; Gregory R. Benzocycloalkylazolethione derivatives
US5854275A (en) * 1996-05-16 1998-12-29 Pfizer Inc. Cyclic imide derivatives
US6310211B1 (en) * 1996-09-10 2001-10-30 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
WO1999007701A1 (en) * 1997-08-05 1999-02-18 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
EP1083897A4 (en) 1998-06-03 2003-01-02 Merck & Co Inc HIV INTEGRASE INHIBITORS
AU4225499A (en) 1998-06-03 1999-12-20 Merck & Co., Inc. Hiv integrase inhibitors
US6218402B1 (en) * 1998-06-10 2001-04-17 Arena Pharmaceuticals, Inc. Acetylcholine enhancers
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
NZ512184A (en) 1998-12-25 2003-08-29 Shionogi & Co Aromatic heterocycle compounds having HIV integrase inhibiting activities
CN1367784A (zh) 1999-06-02 2002-09-04 盐野义制药株式会社 新的取代丙烯酮衍生物的制备方法
AU5880600A (en) 1999-06-25 2001-01-31 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
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
DE60128936T2 (de) * 2000-10-12 2008-04-10 Merck & Co, Inc. Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
AU2002230392A1 (en) 2000-10-12 2002-05-15 Merck & Co., Inc. AZA-and polyaza-naphthalenyl ketones useful as HIV integrase inhibitors
JP2004517860A (ja) 2000-10-12 2004-06-17 メルク　エンド　カムパニー　インコーポレーテッド Ｈｉｖインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類
NZ525088A (en) * 2000-10-12 2004-11-26 Merck & Co Inc Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
WO2002030970A2 (en) * 2000-10-13 2002-04-18 Bayer Aktiengesellschaft Human histone deacetylase gene
US6518767B1 (en) * 2000-10-19 2003-02-11 Schweitzer Engineering Laboratories, Inc. Line differential protection system for a power transmission line
DE602005010413D1 (de) * 2004-04-14 2008-11-27 Zhenhong R Cai Phosphonatanaloga von hiv-integrasehemmerverbindungen

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102917590A (zh) * 2010-03-29 2013-02-06 肿瘤疗法科学股份有限公司 三环化合物及含有所述化合物的pbk抑制剂
CN102917590B (zh) * 2010-03-29 2016-02-17 肿瘤疗法科学股份有限公司 三环化合物及含有所述化合物的pbk抑制剂

Also Published As

Publication number Publication date
AP1858A (en) 2008-06-30
NO20052378D0 (no) 2005-05-13
EA200500660A1 (ru) 2005-10-27
WO2004035577A2 (en) 2004-04-29
WO2004035576A3 (en) 2004-06-24
EP1558613A2 (en) 2005-08-03
AU2003301439A8 (en) 2004-05-04
OA13079A (en) 2006-11-10
US7253180B2 (en) 2007-08-07
AU2003301306A1 (en) 2004-05-04
NZ539264A (en) 2007-08-31
CN100374438C (zh) 2008-03-12
PL377966A1 (pl) 2006-02-20
US20040157804A1 (en) 2004-08-12
IS7845A (is) 2005-05-13
JP2006514099A (ja) 2006-04-27
BR0315405A (pt) 2005-08-09
AU2003301439A1 (en) 2004-05-04
WO2004035577A3 (en) 2004-07-29
NO20052378L (no) 2005-07-18
WO2004035576A2 (en) 2004-04-29
HRP20050431A2 (en) 2005-10-31
EA011399B1 (ru) 2009-02-27
US20040167124A1 (en) 2004-08-26
US20090029939A1 (en) 2009-01-29
AP2005003279A0 (en) 2005-06-30
UA79830C2 (en) 2007-07-25
KR20050087787A (ko) 2005-08-31
CN1726212A (zh) 2006-01-25
MXPA05003950A (es) 2005-06-17

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued