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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- Japan
- Prior art keywords
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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 (cg-RX-API-DMAC10.html) | 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)
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AP2015008510A0 (en) | 2012-12-21 | 2015-06-30 | Gilead Sciences Inc | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| PL3252058T3 (pl) | 2013-07-12 | 2021-07-19 | Gilead Sciences, Inc. | Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv |
| NO2865735T3 (cg-RX-API-DMAC10.html) | 2013-07-12 | 2018-07-21 | ||
| 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 |
| NO2717902T3 (cg-RX-API-DMAC10.html) | 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 |
| TWI738321B (zh) | 2014-12-23 | 2021-09-01 | 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 |
| ES2718410T3 (es) | 2015-04-02 | 2019-07-01 | Gilead Sciences Inc | Compuestos de carbamoilpiridonas policíclicos y su utilización farmacéutica |
| WO2021056193A1 (zh) * | 2019-09-24 | 2021-04-01 | 凯莱英医药集团（天津）股份有限公司 | 一种苄基卤化锌及其衍生物的连续制备方法 |
| 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 |
| MXPA03005338A (es) | 2000-12-14 | 2003-10-06 | Procter & Gamble | Etapa de ciclizacion en el procedimiento de elaboracion de quinolonas y naftiridinas. |
| 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 |
| EP3406596A1 (en) | 2002-11-20 | 2018-11-28 | Japan Tobacco Inc. | 4-oxoquinoline compound and use thereof as hiv integrase inhibitor |
| 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 |
| WO2005113509A1 (en) | 2004-05-20 | 2005-12-01 | Japan Tobacco Inc. | Novel 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 |
| US8420821B2 (en) | 2006-03-06 | 2013-04-16 | Japan Tobacco Inc. | Process for production of 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 |
| CA2661943C (en) | 2006-09-12 | 2015-11-03 | Gilead Sciences, Inc. | Process and intermediates for preparing integrase inhibitors |
| CN103480000A (zh) | 2007-06-29 | 2014-01-01 | 吉里德科学公司 | 治疗用组合物和方法 |
| 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 |
-
2013
- 2013-08-01 MX MX2015001506A patent/MX337094B/es active IP Right Grant
- 2013-08-01 US US13/956,905 patent/US8877931B2/en active Active
- 2013-08-01 AU AU2013296289A patent/AU2013296289B2/en not_active Ceased
- 2013-08-01 CN CN201380041287.6A patent/CN104520275B/zh not_active Expired - Fee Related
- 2013-08-01 CA CA2878699A patent/CA2878699C/en not_active Expired - Fee Related
- 2013-08-01 JP JP2015525605A patent/JP6147856B2/ja not_active Expired - Fee Related
- 2013-08-01 EP EP13748229.5A patent/EP2880017B1/en active Active
- 2013-08-01 EA EA201590018A patent/EA026089B1/ru not_active IP Right Cessation
- 2013-08-01 NZ NZ630199A patent/NZ630199A/en not_active IP Right Cessation
- 2013-08-01 IN IN1688DEN2015 patent/IN2015DN01688A/en unknown
- 2013-08-01 PT PT137482295T patent/PT2880017T/pt unknown
- 2013-08-01 SG SG11201500812QA patent/SG11201500812QA/en unknown
- 2013-08-01 ES ES13748229.5T patent/ES2608860T3/es active Active
- 2013-08-01 KR KR20157005620A patent/KR20150040340A/ko not_active Abandoned
- 2013-08-01 WO PCT/US2013/053295 patent/WO2014022707A1/en not_active Ceased
- 2013-08-01 BR BR112015002275A patent/BR112015002275A2/pt not_active IP Right Cessation
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2015
- 2015-01-11 IL IL236618A patent/IL236618A/en not_active IP Right Cessation