EA201590018A1 - Способ и промежуточные соединения для получения ингибиторов интегразы - Google Patents

Способ и промежуточные соединения для получения ингибиторов интегразы

Info

Publication number
EA201590018A1
EA201590018A1 EA201590018A EA201590018A EA201590018A1 EA 201590018 A1 EA201590018 A1 EA 201590018A1 EA 201590018 A EA201590018 A EA 201590018A EA 201590018 A EA201590018 A EA 201590018A EA 201590018 A1 EA201590018 A1 EA 201590018A1
Authority
EA
Eurasian Patent Office
Prior art keywords
integrases
intermediate connections
obtaining inhibitors
inhibitors
obtaining
Prior art date
Application number
EA201590018A
Other languages
English (en)
Other versions
EA026089B1 (ru
Inventor
Доминика Псион
Кэрри Томаси
Марк Чарльз Уиткомб
Эрик Д. Доуди
Вэньи Фу
Патрисия Маклеод
Original Assignee
Джилид Сайэнс, Инк.
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
Application filed by Джилид Сайэнс, Инк. filed Critical Джилид Сайэнс, Инк.
Publication of EA201590018A1 publication Critical patent/EA201590018A1/ru
Publication of EA026089B1 publication Critical patent/EA026089B1/ru

Links

Classifications

    • 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
    • C07C43/257—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings
    • C07C43/29—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/27—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
    • C07C45/30—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation with halogen containing compounds, e.g. hypohalogenation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C07C45/46—Friedel-Crafts reactions
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/84—Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/12—Preparation of carboxylic acid esters from asymmetrical anhydrides
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Quinoline Compounds (AREA)

Abstract

В изобретении предложены способы синтеза и синтетические промежуточные соединения, которые могут быть использованы для получения 4-оксохинолоновых соединений, обладающих полезной способностью ингибировать интегразу.
EA201590018A 2012-08-03 2013-08-01 Способ и промежуточные соединения для получения ингибиторов интегразы EA026089B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261679475P 2012-08-03 2012-08-03
PCT/US2013/053295 WO2014022707A1 (en) 2012-08-03 2013-08-01 Process and intermediates for preparing integrase inhibitors

Publications (2)

Publication Number Publication Date
EA201590018A1 true EA201590018A1 (ru) 2015-05-29
EA026089B1 EA026089B1 (ru) 2017-02-28

Family

ID=48980354

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590018A EA026089B1 (ru) 2012-08-03 2013-08-01 Способ и промежуточные соединения для получения ингибиторов интегразы

Country Status (18)

Country Link
US (1) US8877931B2 (ru)
EP (1) EP2880017B1 (ru)
JP (1) JP6147856B2 (ru)
KR (1) KR20150040340A (ru)
CN (1) CN104520275B (ru)
AU (1) AU2013296289B2 (ru)
BR (1) BR112015002275A2 (ru)
CA (1) CA2878699C (ru)
EA (1) EA026089B1 (ru)
ES (1) ES2608860T3 (ru)
HK (2) HK1209415A1 (ru)
IL (1) IL236618A (ru)
IN (1) IN2015DN01688A (ru)
MX (1) MX337094B (ru)
NZ (1) NZ630199A (ru)
PT (1) PT2880017T (ru)
SG (1) SG11201500812QA (ru)
WO (1) WO2014022707A1 (ru)

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CN111303152B (zh) 2012-12-21 2023-04-11 吉利德科学公司 多环-氨基甲酰基吡啶酮化合物及其药物用途
NO2865735T3 (ru) 2013-07-12 2018-07-21
DK3019503T3 (da) 2013-07-12 2017-11-20 Gilead Sciences Inc Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner
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
NO2717902T3 (ru) 2014-06-20 2018-06-23
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
EP3466490B1 (en) 2015-04-02 2020-10-21 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
EP4036096A4 (en) * 2019-09-24 2023-08-09 Asymchem Laboratories (Tianjin) Co., Ltd. CONTINUOUS MANUFACTURING PROCESS FOR BENZYLZINC HALIDE AND DERIVATIVES THEREOF
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

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SE9904108D0 (sv) * 1999-11-15 1999-11-15 New Pharma Research Ab Nya föreningar
PL207394B1 (pl) 2000-12-14 2010-12-31 Procter & Gamble Sposób wytwarzania chinolonów i naftyrydyn
TW200300349A (en) 2001-11-19 2003-06-01 Sankyo Co A 4-oxoqinoline derivative
EP1510510A1 (en) 2002-05-31 2005-03-02 Banyu Pharmaceutical Co., Ltd. Method of substituent introduction through halogen-metal exchange reaction
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TW200409759A (en) 2002-09-25 2004-06-16 Wyeth Corp Substituted 4-(indazol-3-yl)phenols
TR200401663T1 (tr) 2002-11-20 2005-04-21 Japan Tobacco Inc. 4-oksokuinolin bileşiği ve bunun HIV integraz inhibitörü olarak kullanımı.
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
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
WO2005113509A1 (en) 2004-05-20 2005-12-01 Japan Tobacco Inc. Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
EP2229945A1 (en) 2004-05-21 2010-09-22 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-HIV agents
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
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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
ES2531190T3 (es) 2006-03-06 2015-03-11 Japan Tobacco Inc Método para producir un compuesto de 4-oxoquinolina
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KR101565169B1 (ko) 2006-09-12 2015-11-02 길리애드 사이언시즈, 인코포레이티드 인테그라제 억제제의 제조를 위한 방법 및 중간체
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AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa

Also Published As

Publication number Publication date
AU2013296289A1 (en) 2015-02-19
IN2015DN01688A (ru) 2015-07-03
CN104520275A (zh) 2015-04-15
ES2608860T3 (es) 2017-04-17
CA2878699A1 (en) 2014-02-06
PT2880017T (pt) 2016-12-14
MX337094B (es) 2016-02-10
KR20150040340A (ko) 2015-04-14
IL236618A (en) 2017-04-30
EP2880017A1 (en) 2015-06-10
JP6147856B2 (ja) 2017-06-14
CA2878699C (en) 2018-09-11
IL236618A0 (en) 2015-02-26
US20140039194A1 (en) 2014-02-06
SG11201500812QA (en) 2015-04-29
EA026089B1 (ru) 2017-02-28
NZ630199A (en) 2016-12-23
AU2013296289B2 (en) 2017-10-05
WO2014022707A1 (en) 2014-02-06
JP2015524822A (ja) 2015-08-27
HK1209748A1 (en) 2016-04-08
HK1209415A1 (en) 2016-04-01
US8877931B2 (en) 2014-11-04
CN104520275B (zh) 2016-11-02
BR112015002275A2 (pt) 2017-07-04
MX2015001506A (es) 2015-04-08
EP2880017B1 (en) 2016-10-05

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU