ECSP034504A - Derivados de acido oxazolil-arilpropionico y su uso como agonista ppar - Google Patents
Derivados de acido oxazolil-arilpropionico y su uso como agonista pparInfo
- Publication number
- ECSP034504A ECSP034504A EC2003004504A ECSP034504A ECSP034504A EC SP034504 A ECSP034504 A EC SP034504A EC 2003004504 A EC2003004504 A EC 2003004504A EC SP034504 A ECSP034504 A EC SP034504A EC SP034504 A ECSP034504 A EC SP034504A
- Authority
- EC
- Ecuador
- Prior art keywords
- alkyl
- unsubstituted
- substituted
- arilpropionic
- oxazolil
- Prior art date
Links
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 title abstract 2
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- -1 thiophene-2,5-diyl Chemical group 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000005493 quinolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
Classifications
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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
-
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D413/10—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 carbon chain containing aromatic rings
-
- 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
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
Abstract
Los compuestos representados por la siguiente fórmula estructural (I) (Gráfico) y las sales, solvatos e hidratos farmacéuticamente aceptables de los mismos en la que n es 2, 3 ó 4 y W es CH2, CH(OH), C(O) o O; R1 es un arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o t-butilo no sustituido o sustituido; R2 es H, alquilo, haloalquilo o fenilo; Y es un tiofen-2,5- diilo o fenileno no sustituido o sustituido; R3 es alquilo o haloalquilo; R4 es un grupo fenilo, naftilo, 1, 2, 3, 4-tetrahidronaftilo, quinolilo, piridilo o benzo (1, 3) dioxol-5-ilo sustituido o no sustituido; y R5 es H, alquilo o aminoalquilo; son útiles para modular un receptor activado por proliferador de peroxisoma, particularmente en el tratamiento de la diabetes mellitus.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22723400P | 2000-08-23 | 2000-08-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP034504A true ECSP034504A (es) | 2003-04-25 |
Family
ID=22852309
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2003004504A ECSP034504A (es) | 2000-08-23 | 2003-03-06 | Derivados de acido oxazolil-arilpropionico y su uso como agonista ppar |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US6930120B2 (es) |
| EP (1) | EP1313716B1 (es) |
| JP (1) | JP2004506721A (es) |
| KR (1) | KR20030027054A (es) |
| CN (1) | CN1471517A (es) |
| AT (1) | ATE361283T1 (es) |
| AU (1) | AU2001284659A1 (es) |
| BR (1) | BR0113409A (es) |
| CA (1) | CA2418104A1 (es) |
| CY (1) | CY1107679T1 (es) |
| CZ (1) | CZ2003482A3 (es) |
| DE (1) | DE60128239T2 (es) |
| DK (1) | DK1313716T3 (es) |
| EA (1) | EA200300286A1 (es) |
| EC (1) | ECSP034504A (es) |
| ES (1) | ES2286137T3 (es) |
| HU (1) | HUP0300857A3 (es) |
| IL (1) | IL154110A0 (es) |
| MX (1) | MXPA03001558A (es) |
| NO (1) | NO20030729L (es) |
| NZ (1) | NZ523804A (es) |
| PL (1) | PL360744A1 (es) |
| PT (1) | PT1313716E (es) |
| SK (1) | SK1872003A3 (es) |
| WO (1) | WO2002016331A1 (es) |
| ZA (1) | ZA200300570B (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002018355A1 (en) | 2000-08-23 | 2002-03-07 | Eli Lilly And Company | Oxazolyl-aryloxyacetic acid derivatives and their use as ppar agonists |
| JP2004506722A (ja) * | 2000-08-23 | 2004-03-04 | イーライ・リリー・アンド・カンパニー | ペルオキシソーム増殖因子活性化受容体の調節方法 |
| DK1392295T3 (da) | 2001-05-15 | 2006-10-02 | Hoffmann La Roche | Carboxylsyre-substituerede oxazol-derivater til anvendelse som PPAR-alpha og -gamma-aktivatorer i behandlingen af diabetes |
| KR100459917B1 (ko) * | 2001-12-14 | 2004-12-03 | (주)바이오뉴트리젠 | 페놀릭산 유도체 및 이를 포함하는 혈중 지질 농도 관련질환의 예방 및 치료용 조성물 |
| US6833380B2 (en) | 2002-03-07 | 2004-12-21 | Warner-Lambert Company, Llc | Compounds that modulate PPAR activity and methods of preparation |
| US6867224B2 (en) | 2002-03-07 | 2005-03-15 | Warner-Lambert Company | Compounds that modulate PPAR activity and methods of preparation |
| PL374818A1 (en) | 2002-07-03 | 2005-10-31 | F.Hoffmann-La Roche Ag | Oxazole derivatives and their use as insulin sensitizers |
| EP1537091B1 (en) | 2002-08-30 | 2010-10-06 | F. Hoffmann-La Roche AG | Novel 2-arylthiazole compounds as pparalpha and ppargamma agonists |
| BR0314261A (pt) | 2002-09-12 | 2005-07-26 | Hoffmann La Roche | Compostos, processo de preparação de um composto, composição farmacêutica que compreende o mesmo, utilização de um composto, método para tratamento e/ou profilaxia de enfermidades e utilização e/ou método de tratamento |
| AR041481A1 (es) * | 2002-10-07 | 2005-05-18 | Hoffmann La Roche | Derivados de acido arilpropionico-oxazol y su uso como agonistas de ppar |
| KR100699614B1 (ko) * | 2002-11-08 | 2007-03-23 | 에프. 호프만-라 로슈 아게 | 퍼옥시좀 증식자 활성화된 수용체 작용제로서의 치환된4-알콕시옥사졸 유도체 |
| DE60323130D1 (de) | 2002-11-25 | 2008-10-02 | Hoffmann La Roche | Indolderivaten |
| DE10308355A1 (de) * | 2003-02-27 | 2004-12-23 | Aventis Pharma Deutschland Gmbh | Aryl-cycloalkyl substituierte Alkansäurederivate, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel |
| US7244763B2 (en) | 2003-04-17 | 2007-07-17 | Warner Lambert Company Llc | Compounds that modulate PPAR activity and methods of preparation |
| EP1658273B1 (en) * | 2003-08-20 | 2007-01-03 | Eli Lilly And Company | Compounds, methods and formulations for the oral delivery of a glucagon like peptide (glp)-1 compound or an melanocortin 4 receptor (mc4) agonist peptide |
| US20070293423A1 (en) * | 2003-08-20 | 2007-12-20 | Eli Lilly And Company | Compounds, Methods and Formulations for the Oral Delivery of a Glucagon-Like Peptide (Glp)-1 Compound or a Melanocortin-4 Receptor (Mc4) Agonist Peptide |
| WO2005100318A1 (en) * | 2004-04-14 | 2005-10-27 | Ranbaxy Laboratories Limited | Alkanoic acids and their esters as antidiabetic agents |
| JPWO2006057448A1 (ja) * | 2004-11-26 | 2008-06-05 | 武田薬品工業株式会社 | アリールアルカン酸誘導体 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5089514A (en) * | 1990-06-14 | 1992-02-18 | Pfizer Inc. | 3-coxazolyl [phenyl, chromanyl or benzofuranyl]-2-hydroxypropionic acid derivatives and analogs as hypoglycemic agents |
| US5232945A (en) * | 1992-07-20 | 1993-08-03 | Pfizer Inc. | 3-aryl-2-hydroxypropionic acid derivatives and analogs as antihypertensives |
| US6062509A (en) | 1994-12-23 | 2000-05-16 | Hexcel Corporation | Retrofit centerline luggage bin assemblies compatible with existing aircraft bin supports |
| US5902726A (en) * | 1994-12-23 | 1999-05-11 | Glaxo Wellcome Inc. | Activators of the nuclear orphan receptor peroxisome proliferator-activated receptor gamma |
| CA2245529A1 (en) | 1996-02-02 | 1997-08-07 | Soumya P. Sahoo | Antidiabetic agents |
| GB9604242D0 (en) | 1996-02-28 | 1996-05-01 | Glaxo Wellcome Inc | Chemical compounds |
| KR20000068151A (ko) * | 1996-08-19 | 2000-11-25 | 미즈노 마사루 | 프로피온산 유도체 및 그의 용도 |
| AU3275999A (en) | 1998-03-10 | 1999-09-27 | Ono Pharmaceutical Co. Ltd. | Carboxylic acid derivatives and drugs containing the same as the active ingredient |
| US6417212B1 (en) | 1999-08-27 | 2002-07-09 | Eli Lilly & Company | Modulators of peroxisome proliferator activated receptors |
| JP4316787B2 (ja) | 2000-01-11 | 2009-08-19 | 壽製薬株式会社 | エーテル又はアミド誘導体、その製法並びにそれを含有する糖尿病治療剤、 |
| JP2004506722A (ja) | 2000-08-23 | 2004-03-04 | イーライ・リリー・アンド・カンパニー | ペルオキシソーム増殖因子活性化受容体の調節方法 |
| WO2002018355A1 (en) | 2000-08-23 | 2002-03-07 | Eli Lilly And Company | Oxazolyl-aryloxyacetic acid derivatives and their use as ppar agonists |
-
2001
- 2001-08-23 HU HU0300857A patent/HUP0300857A3/hu unknown
- 2001-08-23 EA EA200300286A patent/EA200300286A1/ru unknown
- 2001-08-23 US US10/343,476 patent/US6930120B2/en not_active Expired - Fee Related
- 2001-08-23 PL PL01360744A patent/PL360744A1/xx not_active Application Discontinuation
- 2001-08-23 KR KR10-2003-7002472A patent/KR20030027054A/ko not_active Withdrawn
- 2001-08-23 IL IL15411001A patent/IL154110A0/xx unknown
- 2001-08-23 ES ES01963733T patent/ES2286137T3/es not_active Expired - Lifetime
- 2001-08-23 CA CA002418104A patent/CA2418104A1/en not_active Abandoned
- 2001-08-23 DK DK01963733T patent/DK1313716T3/da active
- 2001-08-23 AU AU2001284659A patent/AU2001284659A1/en not_active Abandoned
- 2001-08-23 DE DE60128239T patent/DE60128239T2/de not_active Expired - Lifetime
- 2001-08-23 EP EP01963733A patent/EP1313716B1/en not_active Expired - Lifetime
- 2001-08-23 NZ NZ523804A patent/NZ523804A/en unknown
- 2001-08-23 SK SK187-2003A patent/SK1872003A3/sk not_active Application Discontinuation
- 2001-08-23 BR BR0113409-4A patent/BR0113409A/pt not_active IP Right Cessation
- 2001-08-23 CZ CZ2003482A patent/CZ2003482A3/cs unknown
- 2001-08-23 PT PT01963733T patent/PT1313716E/pt unknown
- 2001-08-23 AT AT01963733T patent/ATE361283T1/de not_active IP Right Cessation
- 2001-08-23 CN CNA018177387A patent/CN1471517A/zh active Pending
- 2001-08-23 MX MXPA03001558A patent/MXPA03001558A/es unknown
- 2001-08-23 JP JP2002521432A patent/JP2004506721A/ja not_active Withdrawn
- 2001-08-23 WO PCT/US2001/022616 patent/WO2002016331A1/en not_active Ceased
-
2003
- 2003-01-21 ZA ZA200300570A patent/ZA200300570B/en unknown
- 2003-02-14 NO NO20030729A patent/NO20030729L/no not_active Application Discontinuation
- 2003-03-06 EC EC2003004504A patent/ECSP034504A/es unknown
-
2005
- 2005-02-09 US US11/054,226 patent/US7345070B2/en not_active Expired - Fee Related
-
2007
- 2007-06-19 CY CY20071100810T patent/CY1107679T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO20030729D0 (no) | 2003-02-14 |
| ZA200300570B (en) | 2004-04-21 |
| DK1313716T3 (da) | 2007-08-27 |
| HUP0300857A3 (en) | 2007-03-28 |
| US20040097590A1 (en) | 2004-05-20 |
| EA200300286A1 (ru) | 2003-08-28 |
| US20050245584A1 (en) | 2005-11-03 |
| NZ523804A (en) | 2004-09-24 |
| NO20030729L (no) | 2003-04-02 |
| WO2002016331A1 (en) | 2002-02-28 |
| AU2001284659A1 (en) | 2002-03-04 |
| MXPA03001558A (es) | 2003-06-06 |
| JP2004506721A (ja) | 2004-03-04 |
| EP1313716B1 (en) | 2007-05-02 |
| PL360744A1 (en) | 2004-09-20 |
| HUP0300857A2 (hu) | 2003-10-28 |
| PT1313716E (pt) | 2007-07-11 |
| CZ2003482A3 (cs) | 2003-05-14 |
| CY1107679T1 (el) | 2013-04-18 |
| SK1872003A3 (en) | 2003-07-01 |
| CA2418104A1 (en) | 2002-02-28 |
| BR0113409A (pt) | 2003-07-01 |
| ATE361283T1 (de) | 2007-05-15 |
| US6930120B2 (en) | 2005-08-16 |
| IL154110A0 (en) | 2003-07-31 |
| US7345070B2 (en) | 2008-03-18 |
| CN1471517A (zh) | 2004-01-28 |
| ES2286137T3 (es) | 2007-12-01 |
| DE60128239T2 (de) | 2008-01-10 |
| KR20030027054A (ko) | 2003-04-03 |
| EP1313716A1 (en) | 2003-05-28 |
| DE60128239D1 (de) | 2007-06-14 |
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