JP5221544B2 - インテグラーゼ阻害剤を調製するためのプロセスおよび中間体 - Google Patents

インテグラーゼ阻害剤を調製するためのプロセスおよび中間体 Download PDF

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JP5221544B2
JP5221544B2 JP2009528433A JP2009528433A JP5221544B2 JP 5221544 B2 JP5221544 B2 JP 5221544B2 JP 2009528433 A JP2009528433 A JP 2009528433A JP 2009528433 A JP2009528433 A JP 2009528433A JP 5221544 B2 JP5221544 B2 JP 5221544B2
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compound
formula
salt
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chloride
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JP2010503694A5 (enExample
JP2010503694A (ja
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エリック ダウディー，
シー チェン，
スティーブン ファイファー，
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ギリアード サイエンシーズ， インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/21—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
    • C07C65/24—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
    • C—CHEMISTRY; METALLURGY
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    • C07C65/21—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
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    • C07C63/00—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings
    • C07C63/68—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings containing halogen
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
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    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/04—Formation of amino groups in compounds containing carboxyl groups
    • C07C227/10—Formation of amino groups in compounds containing carboxyl groups with simultaneously increasing the number of carbon atoms in the carbon skeleton
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    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
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    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
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    • C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
    • C07C41/01—Preparation of ethers
    • C07C41/18—Preparation of ethers by reactions not forming ether-oxygen bonds
    • C07C41/28—Preparation of ethers by reactions not forming ether-oxygen bonds from acetals, e.g. by dealcoholysis
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    • C07C41/18—Preparation of ethers by reactions not forming ether-oxygen bonds
    • C07C41/30—Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
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    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/225—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
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    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
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    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
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    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
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    • C07C67/00—Preparation of carboxylic acid esters
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    • C07C67/333—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
    • C07C67/343—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings 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
    • C07D233/70—One oxygen atom
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    • C07F1/00—Compounds containing elements of Groups 1 or 11 of the Periodic Table
    • C07F1/02—Lithium compounds

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  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Materials Engineering (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
JP2009528433A 2006-09-12 2007-09-11 インテグラーゼ阻害剤を調製するためのプロセスおよび中間体 Expired - Fee Related JP5221544B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US84402006P 2006-09-12 2006-09-12
US60/844,020 2006-09-12
US90536507P 2007-03-07 2007-03-07
US60/905,365 2007-03-07
PCT/US2007/078157 WO2008033836A2 (en) 2006-09-12 2007-09-11 Process and intermediates for preparing integrase inhibitors

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JP2012230583A Division JP2013047248A (ja) 2006-09-12 2012-10-18 インテグラーゼ阻害剤を調製するためのプロセスおよび中間体

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JP2010503694A JP2010503694A (ja) 2010-02-04
JP2010503694A5 JP2010503694A5 (enExample) 2012-06-28
JP5221544B2 true JP5221544B2 (ja) 2013-06-26

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JP2012230583A Withdrawn JP2013047248A (ja) 2006-09-12 2012-10-18 インテグラーゼ阻害剤を調製するためのプロセスおよび中間体

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US (3) US7825252B2 (enExample)
EP (2) EP2069280B1 (enExample)
JP (2) JP5221544B2 (enExample)
KR (2) KR101565169B1 (enExample)
CN (4) CN105503721A (enExample)
AP (1) AP3004A (enExample)
AR (1) AR063710A1 (enExample)
AU (1) AU2007296555B2 (enExample)
BR (1) BRPI0716752A2 (enExample)
CA (1) CA2661943C (enExample)
EA (1) EA022099B1 (enExample)
ES (1) ES2536923T3 (enExample)
HK (2) HK1221454A1 (enExample)
HR (1) HRP20090213B1 (enExample)
IL (2) IL197527A (enExample)
MX (1) MX2009002689A (enExample)
NO (1) NO342907B1 (enExample)
NZ (1) NZ575542A (enExample)
PT (1) PT2069280E (enExample)
SG (2) SG174787A1 (enExample)
TW (1) TWI411602B (enExample)
WO (1) WO2008033836A2 (enExample)
ZA (1) ZA200901576B (enExample)

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TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
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US20110160458A1 (en) 2011-06-30
HRP20090213B1 (hr) 2016-12-02
HK1223370A1 (zh) 2017-07-28
EP2644587A2 (en) 2013-10-02
HK1221454A1 (zh) 2017-06-02
HRP20090213A2 (hr) 2009-06-30
EP2069280B1 (en) 2015-03-25
CA2661943A1 (en) 2008-03-20
IL197527A0 (en) 2009-12-24
HK1130466A1 (en) 2009-12-31
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BRPI0716752A2 (pt) 2013-09-17
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WO2008033836A2 (en) 2008-03-20
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US7825252B2 (en) 2010-11-02
CN101516819A (zh) 2009-08-26
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EA022099B1 (ru) 2015-11-30
NO20091415L (no) 2009-06-11
CN102766098B (zh) 2016-03-30
ZA200901576B (en) 2010-02-24
IL220311A0 (en) 2012-07-31
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US8796459B2 (en) 2014-08-05
JP2013047248A (ja) 2013-03-07
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EP2069280A2 (en) 2009-06-17
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ES2536923T3 (es) 2015-05-29
AU2007296555A1 (en) 2008-03-20
KR20090059153A (ko) 2009-06-10
SG174787A1 (en) 2011-10-28
PT2069280E (pt) 2015-06-08
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NZ575542A (en) 2012-03-30
EA200900441A1 (ru) 2009-06-30
AP2009004831A0 (en) 2009-04-30
CN102766098A (zh) 2012-11-07
AR063710A1 (es) 2009-02-11
IL220311A (en) 2014-02-27
IL197527A (en) 2013-08-29
CN105315154A (zh) 2016-02-10
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US20080125594A1 (en) 2008-05-29
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