CN101014571A - 用作hiv整合酶抑制剂的n－苄基－3,4－二羟基吡啶－2－羧酰胺类和n－苄基－2,3－二羟基吡啶－4－羧酰胺类化合物 - Google Patents

用作hiv整合酶抑制剂的n－苄基－3,4－二羟基吡啶－2－羧酰胺类和n－苄基－2,3－二羟基吡啶－4－羧酰胺类化合物 Download PDF

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Publication number
CN101014571A
CN101014571A CNA2005800033860A CN200580003386A CN101014571A CN 101014571 A CN101014571 A CN 101014571A CN A2005800033860 A CNA2005800033860 A CN A2005800033860A CN 200580003386 A CN200580003386 A CN 200580003386A CN 101014571 A CN101014571 A CN 101014571A
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China
Prior art keywords
alkyl
ring
fluorobenzyl
compound
dihydroxy
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Pending
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CNA2005800033860A
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English (en)
Chinese (zh)
Inventor
P·琼斯
P·D·威廉斯
M·M·莫里塞特
M·S·扩
J·P·瓦卡
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Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
Merck and Co Inc
Original Assignee
Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
Merck and Co Inc
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Application filed by Istituto di Ricerche di Biologia Molecolare P Angeletti SpA, Merck and Co Inc filed Critical Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
Publication of CN101014571A publication Critical patent/CN101014571A/zh
Pending legal-status Critical Current

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    • 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
    • C07D213/60—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 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
    • 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
    • C07D213/60—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 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen atoms
    • 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
    • C07D213/60—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 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNA2005800033860A 2004-01-30 2005-01-26 用作hiv整合酶抑制剂的n－苄基－3,4－二羟基吡啶－2－羧酰胺类和n－苄基－2,3－二羟基吡啶－4－羧酰胺类化合物 Pending CN101014571A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US54053804P 2004-01-30 2004-01-30
US60/540,538 2004-01-30

Publications (1)

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CN101014571A true CN101014571A (zh) 2007-08-08

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CNA2005800033860A Pending CN101014571A (zh) 2004-01-30 2005-01-26 用作hiv整合酶抑制剂的n－苄基－3,4－二羟基吡啶－2－羧酰胺类和n－苄基－2,3－二羟基吡啶－4－羧酰胺类化合物

Country Status (7)

Country Link
US (1) US20070155744A1 (enExample)
EP (1) EP1713773A4 (enExample)
JP (1) JP2007519735A (enExample)
CN (1) CN101014571A (enExample)
AU (1) AU2005211349A1 (enExample)
CA (1) CA2554120A1 (enExample)
WO (1) WO2005074513A2 (enExample)

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* Cited by examiner, † Cited by third party
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CN104903294A (zh) * 2013-01-08 2015-09-09 萨维拉制药有限公司 吡啶酮衍生物及其在治疗、改善或预防病毒疾病中的用途
CN106397311A (zh) * 2016-08-31 2017-02-15 安徽省鸿鑫生物科技有限公司 一种1‑[5‑(苯基甲氧基)‑2‑吡啶]‑乙酮的制备方法

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AU2006306355A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. HIV integrase inhibitors
JP5178738B2 (ja) * 2006-12-20 2013-04-10 メルク・シャープ・アンド・ドーム・コーポレーション 新規なｊｎｋ阻害剤
RS54010B1 (sr) 2009-11-06 2015-10-30 Aerpio Therapeutics Inc. Inhibitori prolil hidroksilaze
BR112012021659A2 (pt) 2010-03-04 2018-01-30 Merck Sharp & Dohme composto, composição farmacêutica, método para tratar e/ou prevenir distúrbios e doenças.
EP2760839B1 (en) * 2011-09-30 2015-11-25 Bristol-Myers Squibb Company Pyridinedione carboxamide inhibitors of endothelial lipase
WO2013048930A1 (en) 2011-09-30 2013-04-04 Bristol-Myers Squibb Company Pyridinedione carboxamide inhibitors of endothelial lipase
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
US9206128B2 (en) * 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
AP2014007805A0 (en) 2011-12-28 2014-07-31 Cytokinetics Inc The Regents Of The University Of California Substituted benzaldehyde compounds and methods fortheir use in increasing tissue oxygenation
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US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
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US9573938B2 (en) 2012-09-11 2017-02-21 Rutgers, The State University Of New Jersey Therapeutic hydroxypyridinones, hydroxypyrimidinones and hydroxypyridazinones
DK3067358T3 (da) 2012-12-21 2019-11-04 Gilead Sciences Inc Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse
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US8952171B2 (en) 2013-03-15 2015-02-10 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
PL3019503T3 (pl) 2013-07-12 2018-01-31 Gilead Sciences Inc Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv
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Cited By (2)

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Publication number Priority date Publication date Assignee Title
CN104903294A (zh) * 2013-01-08 2015-09-09 萨维拉制药有限公司 吡啶酮衍生物及其在治疗、改善或预防病毒疾病中的用途
CN106397311A (zh) * 2016-08-31 2017-02-15 安徽省鸿鑫生物科技有限公司 一种1‑[5‑(苯基甲氧基)‑2‑吡啶]‑乙酮的制备方法

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WO2005074513A2 (en) 2005-08-18
JP2007519735A (ja) 2007-07-19
WO2005074513A3 (en) 2005-09-29
CA2554120A1 (en) 2005-08-18
EP1713773A4 (en) 2009-09-23
US20070155744A1 (en) 2007-07-05
AU2005211349A1 (en) 2005-08-18

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