ZA201002066B - Process and intermediates for preparing integrase inhibitors - Google Patents
Process and intermediates for preparing integrase inhibitorsInfo
- Publication number
- ZA201002066B ZA201002066B ZA2010/02066A ZA201002066A ZA201002066B ZA 201002066 B ZA201002066 B ZA 201002066B ZA 2010/02066 A ZA2010/02066 A ZA 2010/02066A ZA 201002066 A ZA201002066 A ZA 201002066A ZA 201002066 B ZA201002066 B ZA 201002066B
- Authority
- ZA
- South Africa
- Prior art keywords
- intermediates
- integrase inhibitors
- preparing integrase
- preparing
- inhibitors
- Prior art date
Links
- 229940124524 integrase inhibitor Drugs 0.000 title 1
- 239000002850 integrase inhibitor Substances 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
Classifications
-
- 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
Landscapes
- 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)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Bioinformatics & Cheminformatics (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)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97139507P | 2007-09-11 | 2007-09-11 | |
| PCT/US2008/076002 WO2009036161A1 (en) | 2007-09-11 | 2008-09-11 | Process and intermediates for preparing integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA201002066B true ZA201002066B (en) | 2010-12-29 |
Family
ID=39887255
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA2010/02066A ZA201002066B (en) | 2007-09-11 | 2010-03-24 | Process and intermediates for preparing integrase inhibitors |
Country Status (20)
| Country | Link |
|---|---|
| US (4) | US8153801B2 (enExample) |
| EP (1) | EP2190804B1 (enExample) |
| JP (2) | JP5202635B2 (enExample) |
| KR (1) | KR101488550B1 (enExample) |
| CN (1) | CN101821223B (enExample) |
| AP (1) | AP2785A (enExample) |
| AR (1) | AR068403A1 (enExample) |
| AU (1) | AU2008298943B2 (enExample) |
| BR (1) | BRPI0816694A2 (enExample) |
| CA (1) | CA2698245C (enExample) |
| CO (1) | CO6270255A2 (enExample) |
| EA (1) | EA019431B1 (enExample) |
| ES (1) | ES2562080T3 (enExample) |
| MX (1) | MX2010002783A (enExample) |
| NZ (1) | NZ583647A (enExample) |
| PT (1) | PT2190804E (enExample) |
| TW (1) | TWI419867B (enExample) |
| UA (1) | UA101956C2 (enExample) |
| WO (1) | WO2009036161A1 (enExample) |
| ZA (1) | ZA201002066B (enExample) |
Families Citing this family (24)
| 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 |
| 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 |
| US9089574B2 (en) | 2011-11-30 | 2015-07-28 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
| EP2880017B1 (en) | 2012-08-03 | 2016-10-05 | 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 |
| EA030003B1 (ru) | 2012-12-21 | 2018-06-29 | Джилид Сайэнс, Инк. | Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции |
| NO2865735T3 (enExample) | 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 |
| NO2717902T3 (enExample) | 2014-06-20 | 2018-06-23 | ||
| 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 |
| 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 |
| CA2980362C (en) | 2015-04-02 | 2020-02-25 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| 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 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| US7176220B2 (en) * | 2002-11-20 | 2007-02-13 | Japan Tobacco Inc. | 4-oxoquinoline compound and use thereof as pharmaceutical agent |
| 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 |
| 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 |
| 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 |
| 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 |
-
2008
- 2008-09-10 AR ARP080103928A patent/AR068403A1/es unknown
- 2008-09-11 TW TW097134842A patent/TWI419867B/zh not_active IP Right Cessation
- 2008-09-11 CA CA2698245A patent/CA2698245C/en not_active Expired - Fee Related
- 2008-09-11 AP AP2010005187A patent/AP2785A/xx active
- 2008-09-11 BR BRPI0816694 patent/BRPI0816694A2/pt not_active IP Right Cessation
- 2008-09-11 PT PT88302559T patent/PT2190804E/pt unknown
- 2008-09-11 KR KR1020107007731A patent/KR101488550B1/ko not_active Expired - Fee Related
- 2008-09-11 AU AU2008298943A patent/AU2008298943B2/en not_active Ceased
- 2008-09-11 WO PCT/US2008/076002 patent/WO2009036161A1/en not_active Ceased
- 2008-09-11 NZ NZ583647A patent/NZ583647A/en not_active IP Right Cessation
- 2008-09-11 JP JP2010524261A patent/JP5202635B2/ja not_active Expired - Fee Related
- 2008-09-11 CN CN200880106554.2A patent/CN101821223B/zh not_active Expired - Fee Related
- 2008-09-11 US US12/676,553 patent/US8153801B2/en active Active
- 2008-09-11 MX MX2010002783A patent/MX2010002783A/es active IP Right Grant
- 2008-09-11 EA EA201070256A patent/EA019431B1/ru not_active IP Right Cessation
- 2008-09-11 EP EP08830255.9A patent/EP2190804B1/en active Active
- 2008-09-11 US US12/208,952 patent/US20090099366A1/en not_active Abandoned
- 2008-09-11 ES ES08830255.9T patent/ES2562080T3/es active Active
- 2008-11-09 UA UAA201003978A patent/UA101956C2/uk unknown
-
2010
- 2010-03-24 ZA ZA2010/02066A patent/ZA201002066B/en unknown
- 2010-04-05 CO CO10037836A patent/CO6270255A2/es active IP Right Grant
-
2012
- 2012-03-06 US US13/413,518 patent/US8440831B2/en active Active
-
2013
- 2013-02-12 JP JP2013024589A patent/JP2013129659A/ja not_active Withdrawn
- 2013-04-23 US US13/868,836 patent/US8759525B2/en active Active
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