EA016475B1 - Азольные соединения для применения в качестве fxr модуляторов - Google Patents
Азольные соединения для применения в качестве fxr модуляторов Download PDFInfo
- Publication number
- EA016475B1 EA016475B1 EA201070148A EA201070148A EA016475B1 EA 016475 B1 EA016475 B1 EA 016475B1 EA 201070148 A EA201070148 A EA 201070148A EA 201070148 A EA201070148 A EA 201070148A EA 016475 B1 EA016475 B1 EA 016475B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- cyclopropyl
- dichlorophenyl
- ylmethoxy
- compound
- isoxazol
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94997407P | 2007-07-16 | 2007-07-16 | |
| PCT/US2008/069719 WO2009012125A1 (en) | 2007-07-16 | 2008-07-11 | Compounds and methods for modulating fxr |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201070148A1 EA201070148A1 (ru) | 2010-06-30 |
| EA016475B1 true EA016475B1 (ru) | 2012-05-30 |
Family
ID=39855171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201070148A EA016475B1 (ru) | 2007-07-16 | 2008-07-11 | Азольные соединения для применения в качестве fxr модуляторов |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US8153624B2 (enExample) |
| EP (1) | EP2178851B1 (enExample) |
| JP (1) | JP5373788B2 (enExample) |
| KR (1) | KR101157334B1 (enExample) |
| CN (1) | CN101743232B (enExample) |
| AR (1) | AR067540A1 (enExample) |
| AT (1) | ATE539065T1 (enExample) |
| AU (1) | AU2008276236B2 (enExample) |
| BR (1) | BRPI0814571A2 (enExample) |
| CA (1) | CA2693406C (enExample) |
| CL (1) | CL2008002051A1 (enExample) |
| CO (1) | CO6270212A2 (enExample) |
| CY (1) | CY1112298T1 (enExample) |
| DK (1) | DK2178851T3 (enExample) |
| DO (1) | DOP2010000018A (enExample) |
| EA (1) | EA016475B1 (enExample) |
| EC (1) | ECSP109879A (enExample) |
| ES (1) | ES2376176T3 (enExample) |
| HR (1) | HRP20120048T1 (enExample) |
| IL (1) | IL202234A0 (enExample) |
| MA (1) | MA31683B1 (enExample) |
| MX (1) | MX2010000502A (enExample) |
| PE (1) | PE20090809A1 (enExample) |
| PL (1) | PL2178851T3 (enExample) |
| PT (1) | PT2178851E (enExample) |
| RS (1) | RS52216B (enExample) |
| SI (1) | SI2178851T1 (enExample) |
| SV (1) | SV2010003458A (enExample) |
| TN (1) | TN2010000028A1 (enExample) |
| TW (1) | TW200906823A (enExample) |
| WO (1) | WO2009012125A1 (enExample) |
Families Citing this family (82)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2289883A1 (en) | 2009-08-19 | 2011-03-02 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| CU24152B1 (es) * | 2010-12-20 | 2016-02-29 | Irm Llc | 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr |
| JP2014500319A (ja) * | 2010-12-20 | 2014-01-09 | アイアールエム・リミテッド・ライアビリティ・カンパニー | ファルネソイドｘ受容体を調節するための組成物および方法 |
| CN103370315A (zh) * | 2010-12-20 | 2013-10-23 | Irm责任有限公司 | 用于调控法尼醇x受体的组合物和方法 |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
| US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| CA2905242C (en) | 2013-03-15 | 2016-11-29 | Pfizer Inc. | Indole compounds that activate ampk |
| HRP20201953T1 (hr) | 2013-09-11 | 2021-04-30 | Institut National De La Santé Et De La Recherche Médicale (Inserm) | Postupci i farmaceutski pripravci za liječenje virusne infekcije hepatitisom b |
| JP6424231B2 (ja) * | 2013-11-05 | 2018-11-14 | ノバルティス アーゲー | ファルネソイドｘ受容体をモジュレートするための組成物および方法 |
| CN104045635A (zh) * | 2014-06-23 | 2014-09-17 | 华东理工大学 | 3,4,5-三取代异恶唑类化合物及其用途 |
| EP3006939A1 (en) | 2014-10-06 | 2016-04-13 | Gilead Sciences, Inc. | Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| EP3034501A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| EP3034499A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| SG11201706347SA (en) | 2015-02-06 | 2017-09-28 | Intercept Pharmaceuticals Inc | Pharmaceutical compositions for combination therapy |
| TWI698430B (zh) | 2015-02-13 | 2020-07-11 | 南北兄弟藥業投資有限公司 | 三環化合物及其在藥物中的應用 |
| AU2016242861B2 (en) | 2015-03-31 | 2020-08-20 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| CA2981507A1 (en) | 2015-04-07 | 2016-10-13 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions for combination therapy |
| CN106946867B (zh) * | 2016-01-06 | 2019-11-12 | 广州市恒诺康医药科技有限公司 | Fxr受体调节剂及其制备方法和用途 |
| CN107021958A (zh) * | 2016-02-01 | 2017-08-08 | 山东轩竹医药科技有限公司 | Fxr受体激动剂 |
| TW201733582A (zh) | 2016-03-28 | 2017-10-01 | 大日本住友製藥股份有限公司 | Fxr促效劑及arb之組合醫藥 |
| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189663A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
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| US10138228B2 (en) | 2016-05-18 | 2018-11-27 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use therof |
| US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017201150A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| PT3730487T (pt) | 2016-06-13 | 2022-07-22 | Gilead Sciences Inc | Derivados de azetidina como moduladores de fxr (nr1h4) |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| TW201808283A (zh) | 2016-08-05 | 2018-03-16 | 廣東東陽光藥業有限公司 | 含氮三環化合物及其在藥物中的應用 |
| US11091482B2 (en) | 2016-08-23 | 2021-08-17 | Ardelyx, Inc. | Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as FXR activators |
| WO2018039386A1 (en) * | 2016-08-23 | 2018-03-01 | Ardelyx, Inc. | Hormone receptor modulators for treating metabolic conditions and disorders |
| EP3512514A1 (en) * | 2016-09-14 | 2019-07-24 | Novartis AG | Novel regimes of fxr agonists |
| BR112019006651A2 (pt) | 2016-10-04 | 2019-07-02 | Enanta Pharm Inc | análogos de isoxazol como agonistas de fxr e métodos de uso do mesmo |
| WO2018081285A1 (en) | 2016-10-26 | 2018-05-03 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof |
| CN108017636A (zh) * | 2016-11-04 | 2018-05-11 | 合帕吉恩治疗公司 | 作为fxr调节剂的含氮杂环化合物 |
| CN108218852A (zh) * | 2016-12-15 | 2018-06-29 | 宁波百纳西药业有限公司 | 一种螺环化合物、其制备方法、组合物及用途 |
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| JP2020515564A (ja) | 2017-03-30 | 2020-05-28 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物 |
| HRP20220026T1 (hr) * | 2017-04-12 | 2022-04-01 | Il Dong Pharmaceutical Co., Ltd. | Derivati izoksazola kao agonisti nuklearnog receptora i njihove uporabe |
| CN109265471B (zh) * | 2017-06-30 | 2021-06-04 | 轩竹生物科技有限公司 | Fxr受体激动剂 |
| CN109320509B (zh) * | 2017-07-31 | 2022-02-08 | 轩竹生物科技股份有限公司 | Fxr受体激动剂 |
| CN111655680B (zh) | 2017-09-14 | 2024-03-05 | 阿德利克斯股份有限公司 | 用于治疗代谢突变和纤维化病状及病症的激素受体调节剂 |
| KR102732835B1 (ko) | 2017-11-01 | 2024-11-22 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 가교된 비시클릭 화합물 |
| ES2944657T3 (es) * | 2017-11-01 | 2023-06-23 | Bristol Myers Squibb Co | Compuestos de alqueno como moduladores del receptor farnesoide X |
| KR102731925B1 (ko) | 2017-11-01 | 2024-11-18 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 멀티시클릭 화합물 |
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| JP7228595B2 (ja) | 2017-11-01 | 2023-02-24 | ブリストル－マイヤーズ スクイブ カンパニー | ファルネソイドｘ受容体モジュレーターとしてのスピロ環化合物 |
| US10689391B2 (en) | 2017-12-12 | 2020-06-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| EP3730491B1 (en) * | 2017-12-22 | 2022-07-20 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Isoxazole derivative, preparation method therefor, and use thereof |
| CN110128432B (zh) | 2018-02-02 | 2021-03-02 | 广东东阳光药业有限公司 | 含氮三环化合物及其在药物中的应用 |
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| CN110452235B (zh) * | 2018-05-08 | 2023-02-17 | 中国科学院上海药物研究所 | 一类含氟异噁唑类化合物及其制备方法、药物组合物和用途 |
| US20210244744A1 (en) * | 2018-08-30 | 2021-08-12 | Terns Pharmaceuticals, Inc. | Treating liver disorders |
| CN121081472A (zh) | 2018-12-13 | 2025-12-09 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| DK3911647T3 (da) | 2019-01-15 | 2024-02-26 | Gilead Sciences Inc | Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| KR20210130757A (ko) | 2019-02-15 | 2021-11-01 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 치환된 비시클릭 화합물 |
| JP7550777B2 (ja) | 2019-02-15 | 2024-09-13 | ブリストル－マイヤーズ スクイブ カンパニー | ファルネソイドｘ受容体モジュレータとして有用な置換アミド化合物 |
| AR118050A1 (es) | 2019-02-15 | 2021-09-15 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x |
| EA202192244A1 (ru) | 2019-02-15 | 2022-01-24 | Бристол-Маерс Сквибб Компани | Замещенные амидные соединения, применимые в качестве модуляторов фарнезоидного x-рецептора |
| CN113439078B (zh) | 2019-02-19 | 2024-04-23 | 吉利德科学公司 | Fxr激动剂的固体形式 |
| SG11202111502XA (en) | 2019-04-19 | 2021-11-29 | Shanghai Institute Of Materia Medica Chinese Academy Of Sciences | Fxr small molecule agonist and preparation method therefor and use thereof |
| US11555032B2 (en) | 2019-05-13 | 2023-01-17 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| AU2020284135A1 (en) | 2019-05-30 | 2022-01-06 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions comprising a FXR agonist and a fibrate for use in the treatment of cholestatic liver disease |
| CA3139291A1 (en) | 2019-07-18 | 2021-01-21 | Jacky Vonderscher | Method for decreasing adverse-effects of interferon |
| EP4028008A4 (en) | 2019-09-12 | 2023-09-13 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| EP4054567A4 (en) * | 2019-11-08 | 2024-01-10 | Terns Pharmaceuticals, Inc. | TREATMENT OF LIVER DISEASES |
| WO2021108974A1 (en) | 2019-12-03 | 2021-06-10 | Gannex Pharma Co., Ltd | Compounds for modulating activity of fxr and uses thereof |
| EP4090327B1 (en) | 2020-01-15 | 2025-03-05 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of fxr agonists for treating an infection by hepatitis d virus |
| MX2022014238A (es) * | 2020-05-13 | 2023-04-11 | Terns Pharmaceuticals Inc | Tratamiento combinado de trastornos hepáticos. |
| WO2022046779A1 (en) | 2020-08-25 | 2022-03-03 | Eli Lilly And Company | Polymorphs of an ssao inhibitor |
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| US20220135540A1 (en) * | 2020-10-15 | 2022-05-05 | Eli Lilly And Company | Polymorphs of an fxr agonist |
| MX2023008365A (es) | 2021-01-14 | 2023-10-04 | Enyo Pharma | Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv. |
| US20240216364A1 (en) | 2021-04-28 | 2024-07-04 | Enyo Pharma | Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment |
| TW202327589A (zh) | 2021-11-11 | 2023-07-16 | 美商拓臻製藥公司 | 肝病之組合療法 |
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| CN115850152B (zh) * | 2022-12-20 | 2025-10-31 | 河北鼎泰制药有限公司 | 一种杂质A-7-imp3的制备方法及其用途 |
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| WO2004048349A1 (en) * | 2002-11-22 | 2004-06-10 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| WO2007092751A2 (en) * | 2006-02-03 | 2007-08-16 | Eli Lilly And Company | Compounds and methods for modulating fx-receptors |
| WO2007140174A2 (en) * | 2006-05-24 | 2007-12-06 | Eli Lilly And Company | Compounds and methods for modulating fxr |
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| EP1285914B1 (en) | 2001-08-13 | 2007-12-19 | PheneX Pharmaceuticals AG | Nr1h4 nuclear receptor binding compounds |
| JP4541883B2 (ja) | 2002-07-09 | 2010-09-08 | ブリストル−マイヤーズ スクイブ カンパニー | 抗糖尿病薬および抗肥満症薬として有用な置換へテロ環誘導体、並びに方法 |
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2008
- 2008-07-03 TW TW097125064A patent/TW200906823A/zh unknown
- 2008-07-11 EA EA201070148A patent/EA016475B1/ru not_active IP Right Cessation
- 2008-07-11 AU AU2008276236A patent/AU2008276236B2/en not_active Ceased
- 2008-07-11 AT AT08781651T patent/ATE539065T1/de active
- 2008-07-11 MX MX2010000502A patent/MX2010000502A/es active IP Right Grant
- 2008-07-11 CN CN2008800247651A patent/CN101743232B/zh active Active
- 2008-07-11 PL PL08781651T patent/PL2178851T3/pl unknown
- 2008-07-11 DK DK08781651.8T patent/DK2178851T3/da active
- 2008-07-11 WO PCT/US2008/069719 patent/WO2009012125A1/en not_active Ceased
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004048349A1 (en) * | 2002-11-22 | 2004-06-10 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| WO2007092751A2 (en) * | 2006-02-03 | 2007-08-16 | Eli Lilly And Company | Compounds and methods for modulating fx-receptors |
| WO2007140174A2 (en) * | 2006-05-24 | 2007-12-06 | Eli Lilly And Company | Compounds and methods for modulating fxr |
| WO2007140183A1 (en) * | 2006-05-24 | 2007-12-06 | Eli Lilly And Company | Fxr agonists |
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