JP2015524822A5 - - Google Patents
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- JP2015524822A5 JP2015524822A5 JP2015525605A JP2015525605A JP2015524822A5 JP 2015524822 A5 JP2015524822 A5 JP 2015524822A5 JP 2015525605 A JP2015525605 A JP 2015525605A JP 2015525605 A JP2015525605 A JP 2015525605A JP 2015524822 A5 JP2015524822 A5 JP 2015524822A5
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- JP
- Japan
- Prior art keywords
- compound
- formula
- salt
- converting
- item
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 58
- 238000000034 method Methods 0.000 claims description 37
- 150000003839 salts Chemical class 0.000 claims description 22
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 6
- 239000002841 Lewis acid Substances 0.000 claims description 4
- 230000010933 acylation Effects 0.000 claims description 4
- 238000005917 acylation reaction Methods 0.000 claims description 4
- 150000007517 lewis acids Chemical class 0.000 claims description 4
- OIFBSDVPJOWBCH-UHFFFAOYSA-N Diethyl carbonate Chemical compound CCOC(=O)OCC OIFBSDVPJOWBCH-UHFFFAOYSA-N 0.000 claims description 2
- -1 acetyl halide Chemical class 0.000 claims description 2
- 150000004703 alkoxides Chemical class 0.000 claims description 2
- VSCWAEJMTAWNJL-UHFFFAOYSA-K aluminium trichloride Chemical compound Cl[Al](Cl)Cl VSCWAEJMTAWNJL-UHFFFAOYSA-K 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 229910052751 metal Inorganic materials 0.000 claims description 2
- 239000002184 metal Substances 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 0 CC(C1C(OC)=CC(*)=C(Cc(cccc2Cl)c2F)C1)=O Chemical compound CC(C1C(OC)=CC(*)=C(Cc(cccc2Cl)c2F)C1)=O 0.000 description 2
- YZMVLKJJJCMVGX-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline-2,4-dione Chemical class C1=CC=C2NC(=O)CC(=O)C2=C1 YZMVLKJJJCMVGX-UHFFFAOYSA-N 0.000 description 1
- RLCJXIYWSSMZDH-UHFFFAOYSA-N CC(c(c(OC)c1)cc(Cc(cccc2Cl)c2F)c1OC)=O Chemical compound CC(c(c(OC)c1)cc(Cc(cccc2Cl)c2F)c1OC)=O RLCJXIYWSSMZDH-UHFFFAOYSA-N 0.000 description 1
- FKHOOEDRXRLSTH-UHFFFAOYSA-N COc1cc(OC)c(Cc2cccc(Cl)c2F)cc1 Chemical compound COc1cc(OC)c(Cc2cccc(Cl)c2F)cc1 FKHOOEDRXRLSTH-UHFFFAOYSA-N 0.000 description 1
- 239000000543 intermediate Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261679475P | 2012-08-03 | 2012-08-03 | |
| US61/679,475 | 2012-08-03 | ||
| PCT/US2013/053295 WO2014022707A1 (en) | 2012-08-03 | 2013-08-01 | Process and intermediates for preparing integrase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015524822A JP2015524822A (ja) | 2015-08-27 |
| JP2015524822A5 true JP2015524822A5 (OSRAM) | 2016-10-06 |
| JP6147856B2 JP6147856B2 (ja) | 2017-06-14 |
Family
ID=48980354
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015525605A Expired - Fee Related JP6147856B2 (ja) | 2012-08-03 | 2013-08-01 | インテグラーゼインヒビターを調製するためのプロセスおよび中間体 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8877931B2 (OSRAM) |
| EP (1) | EP2880017B1 (OSRAM) |
| JP (1) | JP6147856B2 (OSRAM) |
| KR (1) | KR20150040340A (OSRAM) |
| CN (1) | CN104520275B (OSRAM) |
| AU (1) | AU2013296289B2 (OSRAM) |
| BR (1) | BR112015002275A2 (OSRAM) |
| CA (1) | CA2878699C (OSRAM) |
| EA (1) | EA026089B1 (OSRAM) |
| ES (1) | ES2608860T3 (OSRAM) |
| IL (1) | IL236618A (OSRAM) |
| IN (1) | IN2015DN01688A (OSRAM) |
| MX (1) | MX337094B (OSRAM) |
| NZ (1) | NZ630199A (OSRAM) |
| PT (1) | PT2880017T (OSRAM) |
| SG (1) | SG11201500812QA (OSRAM) |
| WO (1) | WO2014022707A1 (OSRAM) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3067358T3 (da) | 2012-12-21 | 2019-11-04 | Gilead Sciences Inc | Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse |
| NO2865735T3 (OSRAM) | 2013-07-12 | 2018-07-21 | ||
| PL3019503T3 (pl) | 2013-07-12 | 2018-01-31 | Gilead Sciences Inc | Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv |
| 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 (OSRAM) | 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 |
| EP3277691B1 (en) | 2015-04-02 | 2019-01-30 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| CA3160068A1 (en) * | 2019-09-24 | 2021-04-01 | Asymchem Laboratories (Tianjin) Co., Ltd. | Continuous preparation method for benzylzinc halide and derivative 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 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9904108D0 (sv) * | 1999-11-15 | 1999-11-15 | New Pharma Research Ab | Nya föreningar |
| DK1343766T3 (da) | 2000-12-14 | 2005-10-31 | Procter & Gamble | Procestrin med cyklisering ved fremstilling af quinoloner og naphthyridiner |
| 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 |
| AR042095A1 (es) | 2002-11-20 | 2005-06-08 | Japan Tobacco Inc | Compuesto 4-oxoquinolina y aplicacion del mismo como inhibidor de integrasa de vih |
| 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 |
| 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 |
| WO2005112930A1 (en) | 2004-05-21 | 2005-12-01 | 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 |
| US20090233964A1 (en) | 2005-12-30 | 2009-09-17 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| US8420821B2 (en) | 2006-03-06 | 2013-04-16 | Japan Tobacco Inc. | Process for production of 4-oxoquinoline compound |
| AU2007223260C1 (en) | 2006-03-06 | 2011-02-03 | Japan Tobacco Inc. | Method for producing 4-oxoquinoline compound |
| 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 |
| MX2009002689A (es) | 2006-09-12 | 2009-03-26 | Gilead Sciences Inc | Proceso e intermediarios para preparar inhibidores de integrasa. |
| KR20100028656A (ko) | 2007-06-29 | 2010-03-12 | 길리애드 사이언시즈, 인코포레이티드 | 치료 조성물 및 그의 용도 |
| EP2167088A1 (en) | 2007-06-29 | 2010-03-31 | 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 |
-
2013
- 2013-08-01 US US13/956,905 patent/US8877931B2/en active Active
- 2013-08-01 MX MX2015001506A patent/MX337094B/es active IP Right Grant
- 2013-08-01 PT PT137482295T patent/PT2880017T/pt unknown
- 2013-08-01 BR BR112015002275A patent/BR112015002275A2/pt not_active IP Right Cessation
- 2013-08-01 JP JP2015525605A patent/JP6147856B2/ja not_active Expired - Fee Related
- 2013-08-01 IN IN1688DEN2015 patent/IN2015DN01688A/en unknown
- 2013-08-01 CA CA2878699A patent/CA2878699C/en not_active Expired - Fee Related
- 2013-08-01 ES ES13748229.5T patent/ES2608860T3/es active Active
- 2013-08-01 SG SG11201500812QA patent/SG11201500812QA/en unknown
- 2013-08-01 EP EP13748229.5A patent/EP2880017B1/en active Active
- 2013-08-01 KR KR20157005620A patent/KR20150040340A/ko not_active Abandoned
- 2013-08-01 EA EA201590018A patent/EA026089B1/ru not_active IP Right Cessation
- 2013-08-01 AU AU2013296289A patent/AU2013296289B2/en not_active Ceased
- 2013-08-01 NZ NZ630199A patent/NZ630199A/en not_active IP Right Cessation
- 2013-08-01 WO PCT/US2013/053295 patent/WO2014022707A1/en not_active Ceased
- 2013-08-01 CN CN201380041287.6A patent/CN104520275B/zh not_active Expired - Fee Related
-
2015
- 2015-01-11 IL IL236618A patent/IL236618A/en not_active IP Right Cessation
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