JP2017105793A5 - - Google Patents
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- Publication number
- JP2017105793A5 JP2017105793A5 JP2017006285A JP2017006285A JP2017105793A5 JP 2017105793 A5 JP2017105793 A5 JP 2017105793A5 JP 2017006285 A JP2017006285 A JP 2017006285A JP 2017006285 A JP2017006285 A JP 2017006285A JP 2017105793 A5 JP2017105793 A5 JP 2017105793A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- following formula
- pharmaceutical composition
- salt
- formula
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 31
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 208000030507 AIDS Diseases 0.000 claims 1
- AXRYRYVKAWYZBR-UHFFFAOYSA-N Atazanavir Natural products C=1C=C(C=2N=CC=CC=2)C=CC=1CN(NC(=O)C(NC(=O)OC)C(C)(C)C)CC(O)C(NC(=O)C(NC(=O)OC)C(C)(C)C)CC1=CC=CC=C1 AXRYRYVKAWYZBR-UHFFFAOYSA-N 0.000 claims 1
- 108010019625 Atazanavir Sulfate Proteins 0.000 claims 1
- XQSPYNMVSIKCOC-NTSWFWBYSA-N Emtricitabine Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1O[C@@H](CO)SC1 XQSPYNMVSIKCOC-NTSWFWBYSA-N 0.000 claims 1
- 108010002459 HIV Integrase Proteins 0.000 claims 1
- KJHKTHWMRKYKJE-SUGCFTRWSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O KJHKTHWMRKYKJE-SUGCFTRWSA-N 0.000 claims 1
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 claims 1
- 229960004748 abacavir Drugs 0.000 claims 1
- MCGSCOLBFJQGHM-SCZZXKLOSA-N abacavir Chemical compound C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 MCGSCOLBFJQGHM-SCZZXKLOSA-N 0.000 claims 1
- 229960003277 atazanavir Drugs 0.000 claims 1
- AXRYRYVKAWYZBR-GASGPIRDSA-N atazanavir Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)[C@@H](O)CN(CC=1C=CC(=CC=1)C=1N=CC=CC=1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C1=CC=CC=C1 AXRYRYVKAWYZBR-GASGPIRDSA-N 0.000 claims 1
- 229960005107 darunavir Drugs 0.000 claims 1
- CJBJHOAVZSMMDJ-HEXNFIEUSA-N darunavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1[C@@H]2CCO[C@@H]2OC1)C1=CC=CC=C1 CJBJHOAVZSMMDJ-HEXNFIEUSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960000366 emtricitabine Drugs 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229960001627 lamivudine Drugs 0.000 claims 1
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims 1
- 229960004525 lopinavir Drugs 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- YIBOMRUWOWDFLG-ONEGZZNKSA-N rilpivirine Chemical compound CC1=CC(\C=C\C#N)=CC(C)=C1NC1=CC=NC(NC=2C=CC(=CC=2)C#N)=N1 YIBOMRUWOWDFLG-ONEGZZNKSA-N 0.000 claims 1
- 229960002814 rilpivirine Drugs 0.000 claims 1
- 229960000311 ritonavir Drugs 0.000 claims 1
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims 1
- 229960004556 tenofovir Drugs 0.000 claims 1
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361883463P | 2013-09-27 | 2013-09-27 | |
| US61/883,463 | 2013-09-27 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516931A Division JP6081662B2 (ja) | 2013-09-27 | 2014-09-26 | Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017105793A JP2017105793A (ja) | 2017-06-15 |
| JP2017105793A5 true JP2017105793A5 (enExample) | 2017-09-07 |
| JP6550083B2 JP6550083B2 (ja) | 2019-07-24 |
Family
ID=52744477
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516931A Expired - Fee Related JP6081662B2 (ja) | 2013-09-27 | 2014-09-26 | Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
| JP2017006285A Expired - Fee Related JP6550083B2 (ja) | 2013-09-27 | 2017-01-18 | Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516931A Expired - Fee Related JP6081662B2 (ja) | 2013-09-27 | 2014-09-26 | Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
Country Status (31)
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013361401C1 (en) | 2012-12-21 | 2018-08-09 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| NO2865735T3 (enExample) | 2013-07-12 | 2018-07-21 | ||
| EP3252058B1 (en) | 2013-07-12 | 2021-01-20 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their use for the treatment of hiv infections |
| CN105744936B (zh) * | 2013-09-27 | 2019-07-30 | 默沙东公司 | 可用作hiv整合酶抑制剂的取代喹嗪衍生物 |
| WO2015089847A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
| 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 (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 |
| EP3757105B1 (en) | 2014-08-22 | 2024-07-24 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative having integrase inhibitory activity |
| 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 |
| WO2016154527A1 (en) * | 2015-03-26 | 2016-09-29 | Merck Sharp & Dohme Corp. | Phosphate-substituted quinolizine derivatives useful as hiv integrase inhibitors |
| ES2718410T3 (es) | 2015-04-02 | 2019-07-01 | Gilead Sciences Inc | Compuestos de carbamoilpiridonas policíclicos y su utilización farmacéutica |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| WO2017106071A1 (en) | 2015-12-15 | 2017-06-22 | Merck Sharp & Dohme Corp. | Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors |
| WO2018057408A1 (en) * | 2016-09-21 | 2018-03-29 | Merck Sharp & Dohme Corp. | Drug delivery system for the delivery of integrase inhibitors |
| JOP20190130A1 (ar) | 2016-12-02 | 2019-06-02 | Merck Sharp & Dohme | مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv) |
| US10786488B2 (en) | 2017-01-26 | 2020-09-29 | Merck Sharp & Dohme Corp. | Substituted quinolizine derivatives useful as HIV integrase inhibitors |
| JP2019016012A (ja) * | 2017-07-03 | 2019-01-31 | 東芝テック株式会社 | プリンタ装置及びプログラム |
| EP3752144B1 (en) | 2018-02-15 | 2022-12-28 | Merck Sharp & Dohme LLC | Tricyclic heterocycle compounds useful as hiv integrase inhibitors |
| MY203593A (en) | 2018-05-31 | 2024-07-05 | Shionogi & Co | Polycyclic pyridone derivative |
| WO2019230858A1 (ja) | 2018-05-31 | 2019-12-05 | 塩野義製薬株式会社 | 多環性カルバモイルピリドン誘導体 |
| MX2021011394A (es) | 2019-03-22 | 2021-10-13 | Gilead Sciences Inc | Compuestos de carbamoilpiridona triciclica puenteada y su uso farmaceutico. |
| US20200398978A1 (en) | 2019-06-20 | 2020-12-24 | Bell Helicopter Textron Inc. | Low-drag rotor blade extension |
| EP3833657B1 (en) | 2019-07-31 | 2022-07-27 | Advanced Biodesign | Aminothiolester compounds and uses thereof |
| CN112521386B (zh) * | 2019-09-19 | 2023-05-26 | 周雨恬 | 具有抗病毒作用的多环吡啶酮化合物及其药物组合和用途 |
| WO2021107066A1 (ja) | 2019-11-28 | 2021-06-03 | 塩野義製薬株式会社 | インテグラーゼ阻害剤及び抗ｈｉｖ薬を組み合わせることを特徴とするｈｉｖ感染症の予防及び治療用医薬 |
| JP7453399B2 (ja) | 2020-02-24 | 2024-03-19 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖ感染症を治療するための四環式化合物及びその使用 |
| WO2022072520A1 (en) | 2020-09-30 | 2022-04-07 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| PT4196479T (pt) | 2021-01-19 | 2024-01-03 | Gilead Sciences Inc | Compostos de piridotriazinas substituídos e suas utilizações |
| FR3119314B1 (fr) | 2021-01-29 | 2025-01-10 | Advanced Biodesign | Nanocapsule lipidique comprenant au moins un composé aminothiolester ou un de ses dérivés pharmaceutiquement acceptable |
| TW202446773A (zh) | 2022-04-06 | 2024-12-01 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
| WO2025229179A1 (en) | 2024-05-03 | 2025-11-06 | Advanced Biodesign | Use of aminothiolester compounds in combination with hypomethylating agents (hma) for the prevention and treatment of cancer |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1115724A1 (en) * | 1998-09-21 | 2001-07-18 | Shire Biochem Inc. | Quinolizinones as integrin inhibitors |
| GB0110832D0 (en) | 2001-05-03 | 2001-06-27 | Virogen Ltd | Antiviral compounds |
| ES2572030T3 (es) | 2001-08-10 | 2017-07-19 | Shionogi & Co., Ltd. | Agente antiviral |
| DE60209381T2 (de) | 2001-10-26 | 2006-10-05 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase |
| ATE355064T1 (de) | 2001-10-26 | 2006-03-15 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| DE60315796T2 (de) | 2002-01-17 | 2008-06-05 | Merck & Co., Inc. | Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen |
| WO2004024078A2 (en) | 2002-09-11 | 2004-03-25 | Merck & Co., Inc. | Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors |
| AU2003292437A1 (en) | 2002-12-27 | 2004-07-22 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | Tetrahydro-4h-pyrido(1,2-a)pyrimidines and related compounds useful as hiv integrase inhibitors |
| US7135467B2 (en) | 2003-01-13 | 2006-11-14 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7037908B2 (en) | 2003-04-24 | 2006-05-02 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| JP2006232849A (ja) * | 2003-08-13 | 2006-09-07 | Japan Tobacco Inc | 含窒素縮合環化合物及びそのｈｉｖインテグラーゼ阻害剤としての利用 |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| AR046938A1 (es) | 2003-12-12 | 2006-01-04 | Merck & Co Inc | Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares |
| TW200526635A (en) | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
| CN1930161A (zh) | 2004-03-09 | 2007-03-14 | P·安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
| CN1930160B (zh) | 2004-03-09 | 2011-11-16 | 默沙东公司 | Hiv整合酶抑制剂 |
| US7273859B2 (en) | 2004-05-12 | 2007-09-25 | Bristol-Myers Squibb Company | HIV integrase inhibitors: cyclic pyrimidinone compounds |
| US7115601B2 (en) | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7157447B2 (en) | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7192948B2 (en) | 2004-05-28 | 2007-03-20 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7173022B2 (en) | 2004-05-28 | 2007-02-06 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7745459B2 (en) | 2004-09-21 | 2010-06-29 | Japan Tobacco Inc. | Quinolizinone compound and use thereof as HIV integrase inhibitor |
| WO2006033422A1 (ja) * | 2004-09-21 | 2006-03-30 | Japan Tobacco Inc. | キノリジノン化合物、およびそのｈｉｖインテグラーゼ阻害剤としての利用 |
| US20060066414A1 (en) | 2004-09-28 | 2006-03-30 | Rockwell Scientific Licensing, Llc | Method and apparatus for changing the polarization of a signal |
| WO2006066414A1 (en) * | 2004-12-23 | 2006-06-29 | Virochem Pharma Inc. | Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase |
| EP1852434B1 (en) * | 2005-02-21 | 2011-07-13 | Shionogi Co., Ltd. | Bicyclic carbamoylpyridone derivative having hiv integrase inhibiting activity |
| CA2600832C (en) | 2005-03-31 | 2011-12-13 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
| UA96568C2 (en) * | 2005-04-28 | 2011-11-25 | Глаксосмиткляйн Ллк | Polycyclic carbamoyl pyridone derivative as hiv-integrase inhibitor |
| DK3372281T3 (da) | 2005-04-28 | 2021-09-27 | Viiv Healthcare Co | Polycyklisk carbamoylpyridon-derivat med HIV-integrase-hæmmende aktivitet |
| JP2006342115A (ja) | 2005-06-10 | 2006-12-21 | Shionogi & Co Ltd | Ｈｉｖインテグラーゼ阻害活性を有する多環性化合物 |
| US7494984B2 (en) | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
| US7897592B2 (en) | 2005-11-15 | 2011-03-01 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7902182B2 (en) | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8039458B2 (en) | 2005-11-17 | 2011-10-18 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7897593B2 (en) | 2006-05-30 | 2011-03-01 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7893055B2 (en) | 2006-06-28 | 2011-02-22 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2011025683A1 (en) | 2009-08-26 | 2011-03-03 | Merck Sharp & Dohme Corp. | Hiv integrase inhibitors |
| AU2010305805B2 (en) | 2009-10-13 | 2014-04-03 | Elanco Animal Health Ireland Limited | Macrocyclic integrase inhibitors |
| CA2787691C (en) | 2010-01-27 | 2018-07-17 | Glaxosmithkline Llc | Combinations for use in the inhibition of hiv-1 |
| JP5739517B2 (ja) | 2010-04-02 | 2015-06-24 | ヤンセン・アールアンドデイ・アイルランド | 大環状インテグラーゼ阻害剤 |
| CN105744936B (zh) * | 2013-09-27 | 2019-07-30 | 默沙东公司 | 可用作hiv整合酶抑制剂的取代喹嗪衍生物 |
-
2014
- 2014-09-26 CN CN201480064591.7A patent/CN105744936B/zh not_active Expired - Fee Related
- 2014-09-26 ES ES14849935T patent/ES2768658T3/es active Active
- 2014-09-26 SG SG11201602217XA patent/SG11201602217XA/en unknown
- 2014-09-26 PE PE2016000401A patent/PE20160501A1/es unknown
- 2014-09-26 UA UAA201604645A patent/UA117499C2/uk unknown
- 2014-09-26 BR BR112016006651A patent/BR112016006651B8/pt not_active IP Right Cessation
- 2014-09-26 EA EA201690669A patent/EA030695B1/ru not_active IP Right Cessation
- 2014-09-26 EP EP14849935.3A patent/EP3049081B1/en active Active
- 2014-09-26 JP JP2016516931A patent/JP6081662B2/ja not_active Expired - Fee Related
- 2014-09-26 MA MA38922A patent/MA38922A3/fr unknown
- 2014-09-26 AP AP2016009157A patent/AP2016009157A0/en unknown
- 2014-09-26 HK HK16109802.1A patent/HK1221648A1/zh unknown
- 2014-09-26 KR KR1020177034018A patent/KR102102516B1/ko not_active Expired - Fee Related
- 2014-09-26 CA CA2924829A patent/CA2924829C/en not_active Expired - Fee Related
- 2014-09-26 AU AU2014324829A patent/AU2014324829B2/en not_active Ceased
- 2014-09-26 MX MX2016003860A patent/MX367057B/es active IP Right Grant
- 2014-09-26 US US15/025,038 patent/US9861620B2/en active Active
- 2014-09-26 MD MDA20160044A patent/MD4794B1/ro not_active IP Right Cessation
- 2014-09-26 WO PCT/US2014/057572 patent/WO2015048363A1/en not_active Ceased
- 2014-09-26 KR KR1020167010927A patent/KR101809392B1/ko not_active Expired - Fee Related
- 2014-09-26 TN TN2016000090A patent/TN2016000090A1/en unknown
-
2016
- 2016-03-03 IL IL244438A patent/IL244438B/en active IP Right Grant
- 2016-03-11 ZA ZA2016/01708A patent/ZA201601708B/en unknown
- 2016-03-18 SV SV2016005171A patent/SV2016005171A/es unknown
- 2016-03-18 NI NI201600040A patent/NI201600040A/es unknown
- 2016-03-22 GT GT201600056A patent/GT201600056A/es unknown
- 2016-03-22 PH PH12016500553A patent/PH12016500553B1/en unknown
- 2016-03-23 DO DO2016000069A patent/DOP2016000069A/es unknown
- 2016-03-24 CL CL2016000698A patent/CL2016000698A1/es unknown
- 2016-03-27 SA SA516370826A patent/SA516370826B1/ar unknown
- 2016-03-28 CR CR20160140A patent/CR20160140A/es unknown
- 2016-04-25 EC ECIEPI201616726A patent/ECSP16016726A/es unknown
-
2017
- 2017-01-18 JP JP2017006285A patent/JP6550083B2/ja not_active Expired - Fee Related
- 2017-10-05 US US15/725,407 patent/US10201533B2/en active Active
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