KR101488550B1 - 인테그라제 억제제 제조를 위한 방법 및 중간체 - Google Patents

인테그라제 억제제 제조를 위한 방법 및 중간체 Download PDF

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Publication number
KR101488550B1
KR101488550B1 KR1020107007731A KR20107007731A KR101488550B1 KR 101488550 B1 KR101488550 B1 KR 101488550B1 KR 1020107007731 A KR1020107007731 A KR 1020107007731A KR 20107007731 A KR20107007731 A KR 20107007731A KR 101488550 B1 KR101488550 B1 KR 101488550B1
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South Korea
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compound
formula
salt
treatment
mixture
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English (en)
Korean (ko)
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KR20100069675A (ko
Inventor
에릭 다우디
스티븐 페이퍼
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길리애드 사이언시즈, 인코포레이티드
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    • 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
    • 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
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • 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
    • 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
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/15—Preparation of carboxylic acids or their salts, halides or anhydrides by reaction of organic compounds with carbon dioxide, e.g. Kolbe-Schmitt synthesis
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
KR1020107007731A 2007-09-11 2008-09-11 인테그라제 억제제 제조를 위한 방법 및 중간체 Expired - Fee Related KR101488550B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US97139507P 2007-09-11 2007-09-11
US60/971,395 2007-09-11
PCT/US2008/076002 WO2009036161A1 (en) 2007-09-11 2008-09-11 Process and intermediates for preparing integrase inhibitors

Publications (2)

Publication Number Publication Date
KR20100069675A KR20100069675A (ko) 2010-06-24
KR101488550B1 true KR101488550B1 (ko) 2015-02-02

Family

ID=39887255

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020107007731A Expired - Fee Related KR101488550B1 (ko) 2007-09-11 2008-09-11 인테그라제 억제제 제조를 위한 방법 및 중간체

Country Status (20)

Country Link
US (4) US20090099366A1 (https=)
EP (1) EP2190804B1 (https=)
JP (2) JP5202635B2 (https=)
KR (1) KR101488550B1 (https=)
CN (1) CN101821223B (https=)
AP (1) AP2785A (https=)
AR (1) AR068403A1 (https=)
AU (1) AU2008298943B2 (https=)
BR (1) BRPI0816694A2 (https=)
CA (1) CA2698245C (https=)
CO (1) CO6270255A2 (https=)
EA (1) EA019431B1 (https=)
ES (1) ES2562080T3 (https=)
MX (1) MX2010002783A (https=)
NZ (1) NZ583647A (https=)
PT (1) PT2190804E (https=)
TW (1) TWI419867B (https=)
UA (1) UA101956C2 (https=)
WO (1) WO2009036161A1 (https=)
ZA (1) ZA201002066B (https=)

Families Citing this family (24)

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EP2161258A3 (en) 2002-11-20 2010-04-07 Japan Tabacco Inc. 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
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
RS54047B1 (sr) 2006-03-06 2015-10-30 Japan Tobacco Inc. Postupak za dobijanje jedinjenja 4-oksohinolina
IN2014CN00532A (https=) 2006-03-06 2015-04-03 Japan Tobacco Inc
EA022099B1 (ru) 2006-09-12 2015-11-30 Джилид Сайэнс, Инк. Способы и интермедиаты для получения ингибиторов интегразы
WO2009006199A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
AR067184A1 (es) * 2007-06-29 2009-09-30 Gilead Sciences Inc Uso de 6-(3-cloro-2-fluorbencil)-1-[(2s)-1-hidroxi-3-metilbutan-2-il]-7-metoxi-4-oxo-1,4-dihidroquinolina-3-carboxilico. composicion farmaceutica
AR068403A1 (es) * 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
WO2011004389A2 (en) 2009-06-18 2011-01-13 Matrix Laboratories Ltd An improved process for the preparation of elvitegravir
CN102212032B (zh) * 2011-04-20 2013-07-31 复旦大学 一种5-羟基喹诺酮类衍生物及其制备方法和用途
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
CA2878699C (en) * 2012-08-03 2018-09-11 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
NO2865735T3 (https=) 2013-07-12 2018-07-21
SI3019503T1 (sl) 2013-07-12 2017-11-30 Gilead Sciences, Inc. Policiklične karbamoilpiridonske spojine in njihova uporaba za zdravljenje HIV infekcij
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
NO2717902T3 (https=) 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
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
JP6402259B2 (ja) 2015-04-02 2018-10-10 ギリアード サイエンシーズ， インコーポレイテッド 多環式カルバモイルピリドン化合物およびそれらの薬学的使用
CN111733133B (zh) * 2020-07-22 2020-12-01 华夏源(上海)生命科技有限公司 一种促进表皮干细胞分化和生长的方法
CN111944761B (zh) * 2020-08-23 2021-03-26 泉州伟业生物医学科技有限公司 促进表皮干细胞分化和生长的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1564210A1 (en) * 2002-11-20 2005-08-17 Japan Tobacco Inc. 4-oxoquinoline compounds and utilization thereof as hiv integrase inhibitors
WO2005113508A1 (en) 2004-05-20 2005-12-01 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound

Family Cites Families (20)

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US1564210A (en) * 1925-12-08 Obin d
DE3501247A1 (de) * 1985-01-16 1986-07-17 Bayer Ag, 5090 Leverkusen Aminoacrylsaeure-derivate
HUP0303991A3 (en) 2000-12-14 2012-09-28 Warner Chilcott Company Cyclization process step in the making of quinolones and naphthyridines
TW200300349A (en) 2001-11-19 2003-06-01 Sankyo Co A 4-oxoqinoline derivative
AU2003235447A1 (en) * 2002-05-31 2003-12-19 Banyu Pharmaceutical Co., Ltd. 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
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
EP3287130A1 (en) 2004-05-21 2018-02-28 Japan Tobacco Inc. Combinations comprising a 4-isoquinolone derivative and protease inhibitors
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
IN2014CN00532A (https=) 2006-03-06 2015-04-03 Japan Tobacco Inc
RS54047B1 (sr) 2006-03-06 2015-10-30 Japan Tobacco Inc. Postupak za dobijanje jedinjenja 4-oksohinolina
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
EA022099B1 (ru) 2006-09-12 2015-11-30 Джилид Сайэнс, Инк. Способы и интермедиаты для получения ингибиторов интегразы
WO2009006199A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
AR067184A1 (es) * 2007-06-29 2009-09-30 Gilead Sciences Inc Uso de 6-(3-cloro-2-fluorbencil)-1-[(2s)-1-hidroxi-3-metilbutan-2-il]-7-metoxi-4-oxo-1,4-dihidroquinolina-3-carboxilico. composicion farmaceutica
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
EP1564210A1 (en) * 2002-11-20 2005-08-17 Japan Tobacco Inc. 4-oxoquinoline compounds and utilization thereof as hiv integrase inhibitors
WO2005113508A1 (en) 2004-05-20 2005-12-01 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound

Also Published As

Publication number Publication date
EA019431B1 (ru) 2014-03-31
EP2190804B1 (en) 2015-11-18
ZA201002066B (en) 2010-12-29
CA2698245A1 (en) 2009-03-19
US20100292480A1 (en) 2010-11-18
CO6270255A2 (es) 2011-04-20
UA101956C2 (uk) 2013-05-27
AU2008298943A1 (en) 2009-03-19
JP2010539101A (ja) 2010-12-16
NZ583647A (en) 2012-07-27
MX2010002783A (es) 2010-03-31
AU2008298943B2 (en) 2013-10-10
PT2190804E (pt) 2016-03-15
WO2009036161A1 (en) 2009-03-19
TWI419867B (zh) 2013-12-21
US20090099366A1 (en) 2009-04-16
AP2010005187A0 (en) 2010-04-30
CN101821223B (zh) 2014-07-09
EP2190804A1 (en) 2010-06-02
US20130253200A1 (en) 2013-09-26
JP5202635B2 (ja) 2013-06-05
US20120238758A1 (en) 2012-09-20
US8759525B2 (en) 2014-06-24
EA201070256A1 (ru) 2010-12-30
US8153801B2 (en) 2012-04-10
JP2013129659A (ja) 2013-07-04
CA2698245C (en) 2015-06-16
TW200927716A (en) 2009-07-01
BRPI0816694A2 (pt) 2015-03-17
CN101821223A (zh) 2010-09-01
ES2562080T3 (es) 2016-03-02
HK1141785A1 (zh) 2010-11-19
US8440831B2 (en) 2013-05-14
KR20100069675A (ko) 2010-06-24
AR068403A1 (es) 2009-11-18
AP2785A (en) 2013-10-31

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