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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formula
salt
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chloride
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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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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00Compounds 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
    • C07C65/21Compounds 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
    • C07C65/24Compounds 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
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    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/16Heterocyclic 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • C07D233/60Heterocyclic 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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    • C07D233/66Heterocyclic 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
    • C07D233/70One oxygen atom
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    • C07F1/00Compounds containing elements of Groups 1 or 11 of the Periodic Table
    • C07F1/02Lithium compounds

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  • 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)

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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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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) EP2644587A3 (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)
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PT (1) PT2069280E (enExample)
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Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60329318D1 (de) * 2002-11-20 2009-10-29 Japan Tobacco Inc 4-oxochinolinverbindungen und deren verwendung als hiv-integrase-inhibitoren
JP4676536B2 (ja) * 2005-12-30 2011-04-27 ギリアド サイエンシズ, インコーポレイテッド Hivインテグラーゼ阻害剤の薬物動態の改善方法
CN101437801B (zh) 2006-03-06 2013-02-06 日本烟草产业株式会社 制备4-氧代喹啉化合物的方法
KR101023635B1 (ko) 2006-03-06 2011-03-22 니뽄 다바코 산교 가부시키가이샤 4-옥소퀴놀린 화합물 제조 방법
EP2644587A3 (en) * 2006-09-12 2013-10-23 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
NZ582086A (en) * 2007-06-29 2012-07-27 Gilead Sciences Inc Therapeutic compositions and the use thereof
AP2490A (en) * 2007-06-29 2012-10-04 Gilead Sciences Inc Therapeutic compositions and the use thereof
AR068403A1 (es) * 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
EP4556010A3 (en) 2011-11-30 2025-07-23 Emory University Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
CN102603499A (zh) * 2012-03-01 2012-07-25 南京药石药物研发有限公司 1-溴-4-氟-5-异丙基-2-甲氧基苯的合成方法
CN102746143A (zh) * 2012-07-24 2012-10-24 上海灏翔生物科技有限公司 L-薄荷羧酸的一种高立体选择性合成方法
CA2878699C (en) 2012-08-03 2018-09-11 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
CZ304984B6 (cs) * 2012-10-12 2015-03-11 Zentiva, K.S. Zlepšený způsob výroby a nové intermediáty syntézy elvitegraviru
CZ304983B6 (cs) * 2012-10-12 2015-03-11 Zentiva, K.S. Způsob výroby a nové intermediáty syntézy elvitegraviru
NZ709260A (en) 2012-12-21 2016-07-29 Gilead Sciences Inc Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
CZ307255B6 (cs) * 2013-07-11 2018-05-02 Zentiva, K.S. Nový způsob přípravy elvitegraviru
NO2865735T3 (enExample) 2013-07-12 2018-07-21
ES2859102T3 (es) 2013-07-12 2021-10-01 Gilead Sciences Inc Compuestos de carbamoilpiridona policíclica y su uso para el tratamiento de infecciones por VIH
NO2717902T3 (enExample) 2014-06-20 2018-06-23
TWI677489B (zh) 2014-06-20 2019-11-21 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
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI695003B (zh) 2014-12-23 2020-06-01 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
SI3466490T1 (sl) 2015-04-02 2020-12-31 Gilead Sciences, Inc. Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba
CN112661698A (zh) * 2021-01-14 2021-04-16 浙江海森药业股份有限公司 一种艾维雷韦的制备方法

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US93467A (en) * 1869-08-10 Improved machine for bending car-hooks
US36684A (en) * 1862-10-14 Improvement in tailors press-board holders
US93482A (en) * 1869-08-10 Improved roofing-composition
US999366A (en) * 1910-09-30 1911-08-01 John M Gilmore Device for the manufacture of dental crowns.
DE3501247A1 (de) * 1985-01-16 1986-07-17 Bayer Ag, 5090 Leverkusen Aminoacrylsaeure-derivate
CN1232508C (zh) 2000-12-14 2005-12-21 宝洁公司 制取喹诺酮和二氮杂萘的环化方法步骤
TW200300349A (en) 2001-11-19 2003-06-01 Sankyo Co A 4-oxoqinoline derivative
US20050104233A1 (en) 2002-05-31 2005-05-19 Shinji Kato Method of substituent introduction through halogen-metal exchange reaction
US6803469B2 (en) * 2002-08-05 2004-10-12 The Procter & Gamble Company Process for preparing quinolone antibiotic intermediates
TW200409759A (en) 2002-09-25 2004-06-16 Wyeth Corp Substituted 4-(indazol-3-yl)phenols
DE60329318D1 (de) * 2002-11-20 2009-10-29 Japan Tobacco Inc 4-oxochinolinverbindungen und deren verwendung als hiv-integrase-inhibitoren
CN100375742C (zh) * 2002-11-20 2008-03-19 日本烟草产业株式会社 4-氧代喹啉化合物及其用途
EP1582523A1 (en) 2004-04-02 2005-10-05 Ludwig-Maximilians-Universität München Method of preparing organomagnesium compounds
EP1582524B1 (en) 2004-04-02 2008-08-13 Ludwig Maximilians Universität Method of preparing organomagnesium compounds
WO2005113509A1 (en) * 2004-05-20 2005-12-01 Japan Tobacco Inc. Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
US8633219B2 (en) 2004-05-21 2014-01-21 Japan Tobacco Inc. Combination therapy
WO2007063869A1 (ja) 2005-11-30 2007-06-07 Japan Tobacco Inc. 高純度キノロン化合物の製造方法
US20090233964A1 (en) * 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
KR101023635B1 (ko) 2006-03-06 2011-03-22 니뽄 다바코 산교 가부시키가이샤 4-옥소퀴놀린 화합물 제조 방법
CN101437801B (zh) 2006-03-06 2013-02-06 日本烟草产业株式会社 制备4-氧代喹啉化合物的方法
TW200811153A (en) * 2006-06-23 2008-03-01 Japan Tobacco Inc 6-(heterocyclyl-substituted benzyl)-4-oxoquinoline compound and use thereof as HIV integrase inhibitor
EP2644587A3 (en) 2006-09-12 2013-10-23 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
AP2490A (en) 2007-06-29 2012-10-04 Gilead Sciences Inc Therapeutic compositions and the use thereof
NZ582086A (en) 2007-06-29 2012-07-27 Gilead Sciences Inc Therapeutic compositions and the use thereof
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa

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AP2009004831A0 (en) 2009-04-30
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US8324244B2 (en) 2012-12-04
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