KR101565169B1 - 인테그라제 억제제의 제조를 위한 방법 및 중간체 - Google Patents

인테그라제 억제제의 제조를 위한 방법 및 중간체 Download PDF

Info

Publication number
KR101565169B1
KR101565169B1 KR1020097007377A KR20097007377A KR101565169B1 KR 101565169 B1 KR101565169 B1 KR 101565169B1 KR 1020097007377 A KR1020097007377 A KR 1020097007377A KR 20097007377 A KR20097007377 A KR 20097007377A KR 101565169 B1 KR101565169 B1 KR 101565169B1
Authority
KR
South Korea
Prior art keywords
compound
formula
salt
delete
alkyl
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.)
Expired - Fee Related
Application number
KR1020097007377A
Other languages
English (en)
Korean (ko)
Other versions
KR20090059153A (ko
Inventor
에릭 다우디
시 첸
스티븐 프페이퍼
Original Assignee
길리애드 사이언시즈, 인코포레이티드
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39092311&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR101565169(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 길리애드 사이언시즈, 인코포레이티드 filed Critical 길리애드 사이언시즈, 인코포레이티드
Publication of KR20090059153A publication Critical patent/KR20090059153A/ko
Application granted granted Critical
Publication of KR101565169B1 publication Critical patent/KR101565169B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • 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
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C227/16—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 not involving the amino or carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C41/30—Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
    • C07C51/367—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups by introduction of functional groups containing oxygen only in singly bound form
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
    • C07C51/377—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups by splitting-off hydrogen or functional groups; by hydrogenolysis of functional groups
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/18—Preparation of carboxylic acid esters by conversion of a group containing nitrogen into an ester group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D233/56—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F1/00—Compounds containing elements of Groups 1 or 11 of the Periodic Table
    • C07F1/02—Lithium compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Health & Medical Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • 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)
KR1020097007377A 2006-09-12 2007-09-11 인테그라제 억제제의 제조를 위한 방법 및 중간체 Expired - Fee Related KR101565169B1 (ko)

Applications Claiming Priority (4)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020127031758A Division KR101555089B1 (ko) 2006-09-12 2007-09-11 인테그라제 억제제의 제조를 위한 방법 및 중간체

Publications (2)

Publication Number Publication Date
KR20090059153A KR20090059153A (ko) 2009-06-10
KR101565169B1 true KR101565169B1 (ko) 2015-11-02

Family

ID=39092311

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020097007377A Expired - Fee Related KR101565169B1 (ko) 2006-09-12 2007-09-11 인테그라제 억제제의 제조를 위한 방법 및 중간체
KR1020127031758A Expired - Fee Related KR101555089B1 (ko) 2006-09-12 2007-09-11 인테그라제 억제제의 제조를 위한 방법 및 중간체

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020127031758A Expired - Fee Related KR101555089B1 (ko) 2006-09-12 2007-09-11 인테그라제 억제제의 제조를 위한 방법 및 중간체

Country Status (23)

Country Link
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)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7176220B2 (en) * 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
US20070219243A1 (en) * 2005-12-30 2007-09-20 Kearney Brian P Method for improving the pharmacokinetics of HIV integrase inhibitors
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
JP4669040B2 (ja) 2006-03-06 2011-04-13 日本たばこ産業株式会社 ４−オキソキノリン化合物の製造方法
ES2536923T3 (es) 2006-09-12 2015-05-29 Gilead Sciences, Inc. Proceso e intermedios para preparar inhibidores de la integrasa del VIH
SG182229A1 (en) * 2007-06-29 2012-07-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
WO2009006203A1 (en) * 2007-06-29 2009-01-08 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
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
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
EP2880017B1 (en) 2012-08-03 2016-10-05 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
CZ304983B6 (cs) * 2012-10-12 2015-03-11 Zentiva, K.S. Způsob výroby a nové intermediáty syntézy elvitegraviru
CZ304984B6 (cs) 2012-10-12 2015-03-11 Zentiva, K.S. Zlepšený způsob výroby a nové intermediáty syntézy elvitegraviru
EA030003B1 (ru) 2012-12-21 2018-06-29 Джилид Сайэнс, Инк. Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции
CZ307255B6 (cs) * 2013-07-11 2018-05-02 Zentiva, K.S. Nový způsob přípravy elvitegraviru
DK3019503T3 (da) 2013-07-12 2017-11-20 Gilead Sciences Inc Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner
NO2865735T3 (enExample) 2013-07-12 2018-07-21
NO2717902T3 (enExample) 2014-06-20 2018-06-23
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
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
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
CA2980362C (en) 2015-04-02 2020-02-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002048113A1 (en) 2000-12-14 2002-06-20 The Procter & Gamble Company Cyclization process step in the making of quinolones and naphthyridines
WO2004046115A1 (ja) 2002-11-20 2004-06-03 Japan Tobacco Inc. ４−オキソキノリン化合物及びそのｈｉｖインテグラーゼ阻害剤としての利用

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US36684A (en) * 1862-10-14 Improvement in tailors press-board holders
US93467A (en) * 1869-08-10 Improved machine for bending car-hooks
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
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
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
EP1582524B1 (en) 2004-04-02 2008-08-13 Ludwig Maximilians Universität Method of preparing organomagnesium compounds
EP1582523A1 (en) 2004-04-02 2005-10-05 Ludwig-Maximilians-Universität München Method of preparing organomagnesium compounds
US7531554B2 (en) * 2004-05-20 2009-05-12 Japan Tobacco Inc. 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
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
JP4669040B2 (ja) * 2006-03-06 2011-04-13 日本たばこ産業株式会社 ４−オキソキノリン化合物の製造方法
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
ES2536923T3 (es) 2006-09-12 2015-05-29 Gilead Sciences, Inc. Proceso e intermedios para preparar inhibidores de la integrasa del VIH
SG182229A1 (en) 2007-06-29 2012-07-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
WO2009006203A1 (en) 2007-06-29 2009-01-08 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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002048113A1 (en) 2000-12-14 2002-06-20 The Procter & Gamble Company Cyclization process step in the making of quinolones and naphthyridines
WO2004046115A1 (ja) 2002-11-20 2004-06-03 Japan Tobacco Inc. ４−オキソキノリン化合物及びそのｈｉｖインテグラーゼ阻害剤としての利用

Also Published As

Publication number Publication date
WO2008033836A3 (en) 2008-05-22
US20130116437A1 (en) 2013-05-09
NO342907B1 (no) 2018-08-27
CA2661943C (en) 2015-11-03
US20110160458A1 (en) 2011-06-30
JP5221544B2 (ja) 2013-06-26
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
EP2644587A3 (en) 2013-10-23
BRPI0716752A2 (pt) 2013-09-17
CN105503721A (zh) 2016-04-20
WO2008033836A2 (en) 2008-03-20
AP3004A (en) 2014-10-31
US7825252B2 (en) 2010-11-02
CN101516819A (zh) 2009-08-26
TWI411602B (zh) 2013-10-11
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
US8796459B2 (en) 2014-08-05
JP2013047248A (ja) 2013-03-07
JP2010503694A (ja) 2010-02-04
EP2069280A2 (en) 2009-06-17
MX2009002689A (es) 2009-03-26
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
KR101555089B1 (ko) 2015-09-22
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
KR20130004393A (ko) 2013-01-09
SG10201501782UA (en) 2015-05-28
TW200821283A (en) 2008-05-16
US20080125594A1 (en) 2008-05-29
CN101516819B (zh) 2013-10-16
AU2007296555B2 (en) 2012-07-12
US8324244B2 (en) 2012-12-04

Similar Documents

Publication Publication Date Title
KR101555089B1 (ko) 인테그라제 억제제의 제조를 위한 방법 및 중간체
KR101488550B1 (ko) 인테그라제 억제제 제조를 위한 방법 및 중간체
HK1187889A (en) Process and intermediates for preparing integrase inhibitors
HK1141785B (en) Process and intermediates for preparing integrase inhibitors
UA101946C2 (uk) Спосіб та інтермедіати для одержання інгібіторів інтегрази

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

A107 Divisional application of patent
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20181012

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20191028

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20191028

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000