AU2003267098B2 - Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors - Google Patents

Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors Download PDF

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Publication number
AU2003267098B2
AU2003267098B2 AU2003267098A AU2003267098A AU2003267098B2 AU 2003267098 B2 AU2003267098 B2 AU 2003267098B2 AU 2003267098 A AU2003267098 A AU 2003267098A AU 2003267098 A AU2003267098 A AU 2003267098A AU 2003267098 B2 AU2003267098 B2 AU 2003267098B2
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AU
Australia
Prior art keywords
alkyl
rarb
haloalkyl
dihydroxy
dione
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.)
Ceased
Application number
AU2003267098A
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English (en)
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AU2003267098A1 (en
Inventor
Thorsten E. Fisher
Boyoung Kim
H. Marie Langford
Terry A. Lyle
Kyle A. Robinson
John S. Wai
Peter D. Williams
Linghang Zhuang
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Merck and Co Inc
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Merck and Co Inc
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Publication date
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU2003267098A1 publication Critical patent/AU2003267098A1/en
Application granted granted Critical
Publication of AU2003267098B2 publication Critical patent/AU2003267098B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • 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
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2003267098A 2002-09-11 2003-09-10 Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors Ceased AU2003267098B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40974102P 2002-09-11 2002-09-11
US60/409,741 2002-09-11
PCT/US2003/028366 WO2004024078A2 (en) 2002-09-11 2003-09-10 Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
AU2003267098A1 AU2003267098A1 (en) 2004-04-30
AU2003267098B2 true AU2003267098B2 (en) 2008-11-20

Family

ID=31993997

Family Applications (1)

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AU2003267098A Ceased AU2003267098B2 (en) 2002-09-11 2003-09-10 Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors

Country Status (6)

Country Link
US (1) US7517532B2 (enExample)
EP (1) EP1549315A4 (enExample)
JP (1) JP2006506352A (enExample)
AU (1) AU2003267098B2 (enExample)
CA (1) CA2498111A1 (enExample)
WO (1) WO2004024078A2 (enExample)

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KR101678563B1 (ko) 2008-12-11 2016-11-22 비이브 헬쓰케어 컴퍼니 카르바모일피리돈 hiv 인테그라제 억제제를 위한 제조방법 및 중간체
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TWI738321B (zh) 2014-12-23 2021-09-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
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SI3346995T1 (sl) 2015-11-09 2019-11-29 Gilead Sciences Inc Terapevtski sestavek za zdravljenje virusa človeške imunske pomanjkljivosti
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Also Published As

Publication number Publication date
US7517532B2 (en) 2009-04-14
US20060024330A1 (en) 2006-02-02
EP1549315A2 (en) 2005-07-06
EP1549315A4 (en) 2007-05-23
JP2006506352A (ja) 2006-02-23
CA2498111A1 (en) 2004-03-25
WO2004024078A3 (en) 2004-05-13
AU2003267098A1 (en) 2004-04-30
WO2004024078A2 (en) 2004-03-25

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired